Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
44417940 81268 0 None - 1 Human 6.0 pEC50 = 6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 7 2 3 5.8 CCCc1cc(N)c2cc(NCCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216372 81268 0 None - 1 Human 6.0 pEC50 = 6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 7 2 3 5.8 CCCc1cc(N)c2cc(NCCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
137644041 157891 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationPartial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
CHEMBL4090568 157891 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationPartial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
137644041 157891 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationPartial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
CHEMBL4090568 157891 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationPartial agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
10150552 81167 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 385 4 2 3 5.1 CCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216324 81167 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 385 4 2 3 5.1 CCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417944 141266 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 4 2 3 6.1 CC(C)(C)Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386284 141266 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 4 2 3 6.1 CC(C)(C)Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417894 80157 1 None -8 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 387 5 1 3 4.9 CN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214984 80157 1 None -8 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 387 5 1 3 4.9 CN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417921 80698 0 None -9 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215662 80698 0 None -9 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417925 81038 0 None -10 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 532 7 2 4 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NC(=O)c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215981 81038 0 None -10 2 Rat 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 532 7 2 4 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NC(=O)c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417875 80367 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 407 6 2 3 6.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(-c4ccccc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215204 80367 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 407 6 2 3 6.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(-c4ccccc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417823 165208 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 401 6 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL424721 165208 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 401 6 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417903 141224 0 None -67 2 Rat 5.9 pEC50 = 5.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 455 6 1 3 6.6 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCCC1 10.1016/j.bmcl.2006.08.006
CHEMBL386046 141224 0 None -67 2 Rat 5.9 pEC50 = 5.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 455 6 1 3 6.6 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCCC1 10.1016/j.bmcl.2006.08.006
44207909 16505 1 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL1242923 16505 1 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
44207909 16505 1 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL1242923 16505 1 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human mAChR1 receptor expressed in F1pIn CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
15133403 204617 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 371 3 2 3 4.8 Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL87370 204617 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 371 3 2 3 4.8 Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018999 80692 1 None -70 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 6 1 3 5.7 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL215648 80692 1 None -70 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 6 1 3 5.7 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
22018957 82016 0 None -281 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 468 5 2 4 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC4(CCNC4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217502 82016 0 None -281 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 468 5 2 4 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC4(CCNC4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
22018919 141016 1 None -14 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 7 1 3 5.7 CCCN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL384848 141016 1 None -14 2 Rat 6.9 pEC50 = 6.9 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 7 1 3 5.7 CCCN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417998 81969 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 6 2 3 5.9 CCCc1cc(NC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217262 81969 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 6 2 3 5.9 CCCc1cc(NC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018944 81782 0 None -151 2 Rat 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 439 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3C4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217078 81782 0 None -151 2 Rat 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 439 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3C4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417962 81660 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 4 2 3 5.6 CC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216565 81660 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 4 2 3 5.6 CC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417846 81673 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 359 6 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(CC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216580 81673 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 359 6 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(CC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
25110804 95033 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 458 5 1 6 4.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257280 95033 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 458 5 1 6 4.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44454966 154875 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 432 7 1 4 5.5 Cc1ccc2c(c1)nc(C)n2C1CCN(CCCc2cccc(NC(=O)C(C)C)c2)CC1 10.1016/j.bmcl.2008.01.010
CHEMBL403730 154875 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 432 7 1 4 5.5 Cc1ccc2c(c1)nc(C)n2C1CCN(CCCc2cccc(NC(=O)C(C)C)c2)CC1 10.1016/j.bmcl.2008.01.010
44417917 81670 0 None -70 2 Rat 5.8 pEC50 = 5.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 489 6 1 3 6.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL216576 81670 0 None -70 2 Rat 5.8 pEC50 = 5.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 489 6 1 3 6.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
44418009 81437 1 None -48 2 Rat 5.8 pEC50 = 5.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL216455 81437 1 None -48 2 Rat 5.8 pEC50 = 5.8 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417930 81874 0 None -63 2 Rat 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 453 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217207 81874 0 None -63 2 Rat 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 453 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
44455444 94589 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 460 8 1 5 4.9 CO[C@H]1CN(CCCc2cccc(NC(=O)C3CC3)c2)CC[C@@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL255112 94589 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 460 8 1 5 4.9 CO[C@H]1CN(CCCc2cccc(NC(=O)C3CC3)c2)CC[C@@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44455414 96955 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL269939 96955 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44455417 96999 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 462 5 1 6 4.5 COC(=O)Nc1ccc2c(c1)C[C@@H](CN1CC[C@@H](n3c(C)nc4cc(C)ccc43)[C@H](OC)C1)C2 10.1016/j.bmcl.2008.01.010
CHEMBL270151 96999 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 462 5 1 6 4.5 COC(=O)Nc1ccc2c(c1)C[C@@H](CN1CC[C@@H](n3c(C)nc4cc(C)ccc43)[C@H](OC)C1)C2 10.1016/j.bmcl.2008.01.010
24952417 91070 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 407 4 1 3 5.8 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403854 91070 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 407 4 1 3 5.8 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
24952419 91080 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403864 91080 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417867 140969 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 349 5 2 3 4.6 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384550 140969 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 349 5 2 3 4.6 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018896 141150 0 None -16 2 Rat 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 428 5 2 4 4.4 NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385612 141150 0 None -16 2 Rat 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 428 5 2 4 4.4 NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
10150954 141003 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 6 2 3 5.8 CCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384765 141003 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 6 2 3 5.8 CCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
24808474 91077 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403861 91077 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417956 96190 0 None -3 2 Rat 7.6 pEC50 = 7.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL263686 96190 0 None -3 2 Rat 7.6 pEC50 = 7.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417947 140967 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 411 4 2 3 5.8 Nc1cc(C2CCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL384547 140967 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 411 4 2 3 5.8 Nc1cc(C2CCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
10310316 80693 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 439 6 1 3 6.1 CCCc1cc(N2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215649 80693 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 439 6 1 3 6.1 CCCc1cc(N2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
24952765 91082 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 402 4 1 4 4.8 Cc1nc2cc(F)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403866 91082 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 402 4 1 4 4.8 Cc1nc2cc(F)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
10173787 82012 0 None 13 2 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 453 7 2 3 6.8 CCCc1cc(NC2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217480 82012 0 None 13 2 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 453 7 2 3 6.8 CCCc1cc(NC2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018932 79881 0 None -53 2 Rat 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.8 CC1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214125 79881 0 None -53 2 Rat 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.8 CC1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417843 81535 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 457 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(I)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216510 81535 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 457 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(I)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417886 141154 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 453 6 1 3 6.5 CCCc1cc(N2CCCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385619 141154 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 453 6 1 3 6.5 CCCc1cc(N2CCCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
16049789 168442 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 3 2 3 5.8 CC(C)(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL439358 168442 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 3 2 3 5.8 CC(C)(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44455368 95173 0 None 831 2 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 511 5 1 5 5.0 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257906 95173 0 None 831 2 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 511 5 1 5 5.0 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
24952418 91072 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 398 4 1 4 5.0 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403856 91072 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 398 4 1 4 5.0 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
59135478 91074 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 471 5 2 4 6.1 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403858 91074 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 471 5 2 4 6.1 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
59135482 91078 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403862 91078 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
59135474 91079 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403863 91079 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
22018997 141164 0 None -5 2 Rat 7.5 pEC50 = 7.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 485 6 3 4 4.3 CNC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385661 141164 0 None -5 2 Rat 7.5 pEC50 = 7.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 485 6 3 4 4.3 CNC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44417992 82031 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 6 1 3 5.9 CCCc1cc(N(C)C)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217575 82031 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 6 1 3 5.9 CCCc1cc(N(C)C)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10173726 80418 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 449 5 2 3 6.7 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215258 80418 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 449 5 2 3 6.7 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417857 141112 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 376 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc([N+](=O)[O-])cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385389 141112 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 376 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc([N+](=O)[O-])cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10150955 80492 1 None -104 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 413 5 1 3 5.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215331 80492 1 None -104 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 413 5 1 3 5.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417888 79980 1 None -16 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 373 5 2 3 4.9 CNc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214541 79980 1 None -16 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 373 5 2 3 4.9 CNc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417999 81780 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 7 2 3 6.3 CCCc1cc(NCC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217061 81780 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 7 2 3 6.3 CCCc1cc(NCC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018856 80180 0 None -173 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 6 1 3 6.2 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCC1 10.1016/j.bmcl.2006.08.006
CHEMBL215082 80180 0 None -173 2 Rat 6.5 pEC50 = 6.5 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 6 1 3 6.2 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCC1 10.1016/j.bmcl.2006.08.006
44417995 82015 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 414 6 1 3 5.9 CCCc1cc(OC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217495 82015 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 414 6 1 3 5.9 CCCc1cc(OC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417847 82009 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 373 7 2 3 5.4 CCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
CHEMBL217462 82009 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 373 7 2 3 5.4 CCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
44417821 80132 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 421 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214888 80132 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 421 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)ccc2n1 10.1016/j.bmcl.2006.08.008
10126754 81131 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 402 5 3 3 5.1 CCCc1cc(N)c2cc(NC(=O)NCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216145 81131 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 402 5 3 3 5.1 CCCc1cc(N)c2cc(NC(=O)NCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44455443 95254 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 474 6 1 5 4.9 CO[C@@H]1CN(C[C@@H]2Cc3ccc(NC(=O)C(C)C)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL258260 95254 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 474 6 1 5 4.9 CO[C@@H]1CN(C[C@@H]2Cc3ccc(NC(=O)C(C)C)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
24952056 91073 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 437 5 2 4 5.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403857 91073 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 437 5 2 4 5.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417845 141342 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141342 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018945 141179 0 None -199 2 Rat 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.7 CC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385748 141179 0 None -199 2 Rat 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 427 5 1 3 5.7 CC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44417966 160959 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 5 2 3 6.0 CCC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL412831 160959 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 413 5 2 3 6.0 CCC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018914 80488 0 None -87 2 Rat 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 470 6 2 4 4.5 CC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL215316 80488 0 None -87 2 Rat 6.4 pEC50 = 6.4 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 470 6 2 4 4.5 CC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
59135486 91076 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 505 5 2 4 6.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403860 91076 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 505 5 2 4 6.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417975 141316 0 None -2 2 Rat 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 440 5 2 4 4.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CN4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL386548 141316 0 None -2 2 Rat 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 440 5 2 4 4.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CN4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417945 141253 0 None -16 2 Rat 7.3 pEC50 = 7.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 508 7 3 5 3.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NS(=O)(=O)O)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL386211 141253 0 None -16 2 Rat 7.3 pEC50 = 7.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 508 7 3 5 3.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NS(=O)(=O)O)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417838 81171 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216342 81171 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
44417877 80710 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 373 6 2 3 5.5 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215696 80710 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 373 6 2 3 5.5 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
59135492 91081 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 418 4 1 4 5.4 Cc1nc2cc(C#N)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403865 91081 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 418 4 1 4 5.4 Cc1nc2cc(C#N)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417911 82013 1 None -14 2 Rat 7.3 pEC50 = 7.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 399 5 1 3 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217487 82013 1 None -14 2 Rat 7.3 pEC50 = 7.3 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 399 5 1 3 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417915 140845 0 None 1 2 Rat 6.2 pEC50 = 6.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 471 6 1 5 5.0 COC(=O)C1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL383884 140845 0 None 1 2 Rat 6.2 pEC50 = 6.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 471 6 1 5 5.0 COC(=O)C1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
24952055 91075 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 515 5 2 4 6.2 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403859 91075 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 515 5 2 4 6.2 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417845 141342 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141342 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417845 141342 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141342 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417864 79865 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 389 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(OC(C)=O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214020 79865 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 389 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(OC(C)=O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417979 81720 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 433 4 2 3 6.2 Nc1cc(-c2ccccc2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL216817 81720 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 433 4 2 3 6.2 Nc1cc(-c2ccccc2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
44417948 141205 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 425 4 2 3 6.1 Nc1cc(C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL385941 141205 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 425 4 2 3 6.1 Nc1cc(C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
44455367 95172 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 389 4 0 4 4.3 CO[C@@H]1CN(CC2Cc3ccccc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257905 95172 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at MCHR1 by cAMP assayAntagonist activity at MCHR1 by cAMP assay
ChEMBL 389 4 0 4 4.3 CO[C@@H]1CN(CC2Cc3ccccc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
59135471 91068 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 451 4 1 3 5.9 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403852 91068 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP productionAntagonist activity at human MCHR1 expressed in CHOK1 cells assessed as inhibition of MCH/forskolin-stimulated cAMP production
ChEMBL 451 4 1 3 5.9 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44417973 140931 0 None -5 2 Rat 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 5 1 4 4.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CO4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL384362 140931 0 None -5 2 Rat 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 441 5 1 4 4.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CO4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417844 141043 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 345 5 2 3 4.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384994 141043 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 345 5 2 3 4.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417874 141117 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 377 6 2 4 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(SC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385398 141117 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 377 6 2 4 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(SC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417982 82086 1 None -3 2 Rat 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 359 4 2 3 4.4 Nc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL217751 82086 1 None -3 2 Rat 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 359 4 2 3 4.4 Nc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417848 141078 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 8 2 3 5.8 CCCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
CHEMBL385221 141078 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 8 2 3 5.8 CCCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
44417832 141208 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 415 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385957 141208 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 415 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417976 165378 1 None -9 2 Rat 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 7 1 3 5.7 CCN(CC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL425098 165378 1 None -9 2 Rat 6.1 pEC50 = 6.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 415 7 1 3 5.7 CCN(CC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417959 81369 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 7 2 3 6.2 CCCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216428 81369 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 427 7 2 3 6.2 CCCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018964 141126 0 None -89 2 Rat 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 498 7 2 4 5.2 CC(C)C(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385452 141126 0 None -89 2 Rat 7.1 pEC50 = 7.1 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing rat MCH-R1
ChEMBL 498 7 2 4 5.2 CC(C)C(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44418003 82042 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217614 82042 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
44417873 81033 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215965 81033 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 387 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44418002 82139 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 409 5 2 3 5.2 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Br)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217845 82139 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 409 5 2 3 5.2 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Br)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
9799244 80158 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214985 80158 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10127348 141273 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 439 4 2 3 6.5 Nc1cc(C2CCCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL386320 141273 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 439 4 2 3 6.5 Nc1cc(C2CCCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
44417856 80413 0 None - 1 Human 6.0 pEC50 = 6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)c(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215241 80413 0 None - 1 Human 6.0 pEC50 = 6 Functional
Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1Stimulation of IP3-coupled mobilization of calcium in HEK293 cells expressing MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)c(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
11994411 987 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 10.1021/jm060814b
1306 987 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 10.1021/jm060814b
CHEMBL214523 987 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 10.1021/jm060814b
4033 1860 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2006.07.008
9826520 1860 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2006.07.008
CHEMBL214957 1860 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2006.07.008
4033 1860 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.003
9826520 1860 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.003
CHEMBL214957 1860 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.003
10004545 74588 4 None 1 5 Mouse 9.2 pIC50 = 9.2 Functional
Antagonist activity at mouse MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at mouse MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74588 4 None 1 5 Mouse 9.2 pIC50 = 9.2 Functional
Antagonist activity at mouse MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at mouse MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
11995648 81972 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 446 4 0 6 5.4 CN(C)Cc1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1 10.1021/jm060572f
CHEMBL217269 81972 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 446 4 0 6 5.4 CN(C)Cc1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1 10.1021/jm060572f
11994912 82464 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 487 4 0 5 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCCC1)=C2 10.1021/jm060814b
CHEMBL218077 82464 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 487 4 0 5 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCCC1)=C2 10.1021/jm060814b
10004545 74588 4 None -1 5 Rat 9.1 pIC50 = 9.1 Functional
Antagonist activity at rat MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at rat MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74588 4 None -1 5 Rat 9.1 pIC50 = 9.1 Functional
Antagonist activity at rat MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at rat MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
10004545 74588 4 None -1 5 Rhesus macaque 9.1 pIC50 = 9.1 Functional
Antagonist activity at rhesus monkey MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at rhesus monkey MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74588 4 None -1 5 Rhesus macaque 9.1 pIC50 = 9.1 Functional
Antagonist activity at rhesus monkey MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilizationAntagonist activity at rhesus monkey MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
11994412 141167 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 473 4 0 5 6.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCC1)=C2 10.1021/jm060814b
CHEMBL385690 141167 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 473 4 0 5 6.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCC1)=C2 10.1021/jm060814b
11993893 141279 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 486 4 0 6 6.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCCCC3)ccc2c1 10.1021/jm060572f
CHEMBL386349 141279 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 486 4 0 6 6.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCCCC3)ccc2c1 10.1021/jm060572f
11995024 140890 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 477 4 0 6 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCCC3)cc2c1 10.1021/jm060814b
CHEMBL384133 140890 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 477 4 0 6 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCCC3)cc2c1 10.1021/jm060814b
11995242 80390 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 472 4 0 6 5.9 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCCC3)ccc2c1 10.1021/jm060572f
CHEMBL215235 80390 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 472 4 0 6 5.9 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCCC3)ccc2c1 10.1021/jm060572f
44416336 79638 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 477 8 0 8 4.6 COc1ccc(-c2cc3ncn(-c4ccc(OCCN5CCCC5)c(OC)c4)c(=O)c3s2)cc1 10.1016/j.bmcl.2006.07.008
CHEMBL213008 79638 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 477 8 0 8 4.6 COc1ccc(-c2cc3ncn(-c4ccc(OCCN5CCCC5)c(OC)c4)c(=O)c3s2)cc1 10.1016/j.bmcl.2006.07.008
44442095 93853 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 381 6 2 5 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250516 93853 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 381 6 2 5 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11994413 80093 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 449 4 0 5 5.4 CN(C)CC1CCc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2C1 10.1021/jm060814b
CHEMBL214806 80093 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 449 4 0 5 5.4 CN(C)CC1CCc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2C1 10.1021/jm060814b
11994784 81866 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 461 4 0 6 6.1 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2oc(CN3CCCC3)cc2c1 10.1021/jm060814b
CHEMBL217178 81866 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 461 4 0 6 6.1 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2oc(CN3CCCC3)cc2c1 10.1021/jm060814b
11994786 82166 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 474 4 0 6 5.9 Cn1c(CN2CCCC2)cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1021/jm060814b
CHEMBL217887 82166 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 474 4 0 6 5.9 Cn1c(CN2CCCC2)cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1021/jm060814b
10004545 74588 4 None -1 5 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization by aequorin assayAntagonist activity at human MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization by aequorin assay
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74588 4 None -1 5 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization by aequorin assayAntagonist activity at human MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization by aequorin assay
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
44416314 79540 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 465 7 0 7 4.7 COc1cc(-n2cnc3cc(-c4ccc(F)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212657 79540 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 465 7 0 7 4.7 COc1cc(-n2cnc3cc(-c4ccc(F)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
11994913 80127 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 475 4 0 5 6.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCC1)C2 10.1021/jm060814b
CHEMBL214871 80127 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 475 4 0 5 6.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCC1)C2 10.1021/jm060814b
11994659 81125 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 451 4 0 6 6.0 CN(C)Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2s1 10.1021/jm060814b
CHEMBL216117 81125 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 451 4 0 6 6.0 CN(C)Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2s1 10.1021/jm060814b
11993894 82137 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 562 5 0 6 7.7 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccccc4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL217843 82137 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 562 5 0 6 7.7 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccccc4)CC3)ccc2c1 10.1021/jm060572f
11994780 82084 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 518 6 0 7 5.9 COC[C@H]1CCCN1Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C 10.1021/jm060814b
CHEMBL217733 82084 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 518 6 0 7 5.9 COC[C@H]1CCCN1Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C 10.1021/jm060814b
11995244 80148 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 583 7 0 7 7.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(CCN4CCCC4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL214944 80148 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 583 7 0 7 7.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(CCN4CCCC4)CC3)ccc2c1 10.1021/jm060572f
44416857 79817 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 450 5 1 7 4.8 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCCO 10.1016/j.bmcl.2006.07.054
CHEMBL213813 79817 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 450 5 1 7 4.8 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCCO 10.1016/j.bmcl.2006.07.054
11553871 80690 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 3 0 7 4.7 CN(C)c1nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2n1C 10.1016/j.bmcl.2006.07.054
CHEMBL215643 80690 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 3 0 7 4.7 CN(C)c1nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2n1C 10.1016/j.bmcl.2006.07.054
44416316 168709 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 515 7 0 7 5.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)c(Cl)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL441368 168709 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 515 7 0 7 5.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)c(Cl)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44416837 140996 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 489 5 0 7 5.5 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCN1CCCC1 10.1016/j.bmcl.2006.07.054
CHEMBL384724 140996 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 489 5 0 7 5.5 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCN1CCCC1 10.1016/j.bmcl.2006.07.054
10225681 79913 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3cc(-c4ccccc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL214276 79913 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3cc(-c4ccccc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44414475 77706 0 None - 1 Human 8.0 pIC50 = 8 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL210069 77706 0 None - 1 Human 8.0 pIC50 = 8 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44417150 79808 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 527 5 0 8 6.2 COc1ccc(-n2c(N(C)C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL213766 79808 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 527 5 0 8 6.2 COc1ccc(-n2c(N(C)C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44416976 81050 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 465 5 1 8 4.2 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCO 10.1016/j.bmcl.2006.07.054
CHEMBL216005 81050 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 465 5 1 8 4.2 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCO 10.1016/j.bmcl.2006.07.054
23027411 196833 0 None 30 4 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577912 196833 0 None 30 4 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
44430471 86364 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 541 5 0 7 4.2 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232209 86364 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 541 5 0 7 4.2 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOC2)C1 10.1016/j.bmcl.2007.02.012
44430460 86784 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 567 4 0 6 6.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232858 86784 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 567 4 0 6 6.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2007.02.012
44430463 148855 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 511 5 0 6 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL394560 148855 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 511 5 0 6 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CC2)C1 10.1016/j.bmcl.2007.02.012
70688018 74479 0 None 1 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 428 5 1 3 5.6 O=C(Nc1ccc2c(c1)OCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031574 74479 0 None 1 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 428 5 1 3 5.6 O=C(Nc1ccc2c(c1)OCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
18436085 74524 0 None 2 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1cc2cc(CN3CCCC3)cnc2cc1NC(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031730 74524 0 None 2 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1cc2cc(CN3CCCC3)cnc2cc1NC(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
44394824 123736 0 None - 1 Human 8.0 pIC50 = 8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5cccc(Cl)c5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL363464 123736 0 None - 1 Human 8.0 pIC50 = 8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5cccc(Cl)c5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
10025637 65238 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL183215 65238 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
44416751 81694 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 476 3 1 7 4.4 CN1CCN(c2nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3[nH]2)CC1 10.1016/j.bmcl.2006.07.054
CHEMBL216649 81694 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 476 3 1 7 4.4 CN1CCN(c2nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3[nH]2)CC1 10.1016/j.bmcl.2006.07.054
44416350 141407 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 453 7 0 8 4.7 COc1cc(-n2cnc3cc(-c4cccs4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL387195 141407 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 453 7 0 8 4.7 COc1cc(-n2cnc3cc(-c4cccs4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
45485029 196806 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 CCc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577714 196806 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 CCc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
54581468 60246 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccc(F)cc2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760068 60246 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccc(F)cc2)cc1 10.1016/j.bmcl.2011.02.046
45267576 194947 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 4 1 4 5.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL564286 194947 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 4 1 4 5.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
70687479 73148 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3cccc(F)c3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016785 73148 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3cccc(F)c3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
57402044 68487 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3ccc(Cl)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922251 68487 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3ccc(Cl)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
23532179 68489 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.4 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922253 68489 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.4 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
57395050 68499 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 419 3 1 2 5.3 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCCCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922265 68499 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 419 3 1 2 5.3 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCCCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
44394800 121829 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 373 6 2 6 4.0 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OC(F)(F)O4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL359995 121829 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 373 6 2 6 4.0 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OC(F)(F)O4)c2n1 10.1016/j.bmcl.2004.07.034
44394676 123101 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 297 6 2 5 3.0 CC(CNCc1ccoc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL361878 123101 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 297 6 2 5 3.0 CC(CNCc1ccoc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394890 130917 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 299 6 2 4 3.4 CC(CNCC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL369116 130917 0 None - 1 Human 7.0 pIC50 = 7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 299 6 2 4 3.4 CC(CNCC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11189610 165213 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 430 5 1 5 4.6 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL424728 165213 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 430 5 1 5 4.6 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
20817821 76491 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 431 4 1 4 5.4 Cn1c(=O)cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL206953 76491 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 431 4 1 4 5.4 Cn1c(=O)cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
23120540 194455 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL561134 194455 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
127031907 138583 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccccc2Cl)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3786923 138583 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccccc2Cl)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
57398576 68485 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 254 0 1 1 3.4 CC1c2c([nH]c3ccccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922249 68485 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 254 0 1 1 3.4 CC1c2c([nH]c3ccccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
57402045 68488 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3c(Cl)cccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922252 68488 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3c(Cl)cccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
10202381 68501 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 C[C@@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@@H]2CCN(CCN3CCOCC3)C[C@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922267 68501 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 C[C@@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@@H]2CCN(CCN3CCOCC3)C[C@H]21 10.1016/j.bmcl.2011.09.110
44418006 81984 0 None - 1 Human 6.0 pIC50 = 6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 505 10 5 4 3.5 N=C(N)NCCC[C@@H](NC(=O)Cc1csc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217349 81984 0 None - 1 Human 6.0 pIC50 = 6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 505 10 5 4 3.5 N=C(N)NCCC[C@@H](NC(=O)Cc1csc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11973799 82036 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 410 5 1 5 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL217593 82036 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 410 5 1 5 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
11188955 80042 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 406 6 2 5 4.4 CC(C)Nc1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
CHEMBL214678 80042 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 406 6 2 5 4.4 CC(C)Nc1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
3114950 37521 29 None -2 2 Human 5.0 pIC50 = 5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 318 3 0 4 2.8 O=[N+]([O-])c1cc(S(=O)(=O)N2CCCCCC2)ccc1Cl nan
CHEMBL1458112 37521 29 None -2 2 Human 5.0 pIC50 = 5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 318 3 0 4 2.8 O=[N+]([O-])c1cc(S(=O)(=O)N2CCCCCC2)ccc1Cl nan
54586331 60245 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760065 60245 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2011.02.046
11526309 188619 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 508 8 1 5 5.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(OC(F)(F)F)cc3)o2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL511480 188619 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 508 8 1 5 5.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(OC(F)(F)F)cc3)o2)CC1 10.1016/j.bmcl.2008.07.079
44417983 81734 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1ccnc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL216935 81734 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1ccnc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
70689520 73104 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 521 6 1 6 4.8 Cc1nc(N2CCN(C(=O)C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016715 73104 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 521 6 1 6 4.8 Cc1nc(N2CCN(C(=O)C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11837128 71771 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 360 5 1 4 4.4 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2ccccc2o1 10.1021/jm050598r
CHEMBL197849 71771 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 360 5 1 4 4.4 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2ccccc2o1 10.1021/jm050598r
44562404 176380 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 408 6 1 3 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462347 176380 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 408 6 1 3 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.07.079
44410878 77739 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 475 5 1 7 4.2 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL210273 77739 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 475 5 1 7 4.2 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2006.02.044
44592257 178403 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 433 10 0 6 3.9 COc1cc(-n2ccnc(CCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL470840 178403 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 433 10 0 6 3.9 COc1cc(-n2ccnc(CCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
58062385 125343 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 9 2 4 3.7 CC1(CNCc2ccc3c(c2)C[C@H](NC(=O)c2ccc(OCC4CC4)cn2)C3)CC1 nan
CHEMBL3648387 125343 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 9 2 4 3.7 CC1(CNCc2ccc3c(c2)C[C@H](NC(=O)c2ccc(OCC4CC4)cn2)C3)CC1 nan
4062524 32391 6 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 501 7 1 5 4.8 Cc1ccc(CN2C(=O)c3ccccc3Sc3ccc(C(=O)NCCCN4CCOCC4)cc32)cc1 nan
CHEMBL1412874 32391 6 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 501 7 1 5 4.8 Cc1ccc(CN2C(=O)c3ccccc3Sc3ccc(C(=O)NCCCN4CCOCC4)cc32)cc1 nan
46846317 58826 0 None -15 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 362 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cccc(Cl)c3)c2=O)cc1 nan
CHEMBL1699198 58826 0 None -15 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 362 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cccc(Cl)c3)c2=O)cc1 nan
46846319 58881 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 6 4.8 COc1cc(OC)cc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)c1 nan
CHEMBL1701679 58881 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 6 4.8 COc1cc(OC)cc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)c1 nan
24856242 35060 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 355 4 0 3 4.7 CN(C)C1=NC[C@H](Cc2ccccc2)N1CC1CCC(C(C)(C)C)CC1 nan
CHEMBL1436519 35060 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 355 4 0 3 4.7 CN(C)C1=NC[C@H](Cc2ccccc2)N1CC1CCC(C(C)(C)C)CC1 nan
49866089 16054 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 481 7 1 4 6.6 Cc1nc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2[nH]1 10.1016/j.bmcl.2010.07.086
CHEMBL1224389 16054 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 481 7 1 4 6.6 Cc1nc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2[nH]1 10.1016/j.bmcl.2010.07.086
44405481 71491 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 364 4 2 5 3.7 Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL196972 71491 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 364 4 2 5 3.7 Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
70691720 73191 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 442 5 2 5 4.6 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017594 73191 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 442 5 2 5 4.6 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
23120586 195052 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL565105 195052 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
2729098 80069 2 None 11 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
CHEMBL214726 80069 2 None 11 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
11563383 70156 0 None 173 2 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL194691 70156 0 None 173 2 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
52917998 60293 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760234 60293 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44430477 86776 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 569 6 0 7 5.0 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232823 86776 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 569 6 0 7 5.0 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44430476 151762 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 555 5 0 7 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL396957 151762 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 555 5 0 7 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
23593464 64356 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64356 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
18436117 74529 0 None 162 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 435 5 1 3 6.4 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
CHEMBL2031735 74529 0 None 162 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 435 5 1 3 6.4 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
53324076 56400 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 420 9 0 6 3.9 COc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642476 56400 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 420 9 0 6 3.9 COc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1 10.1016/j.bmc.2010.12.002
21108056 67723 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 452 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914629 67723 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 452 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57391028 67728 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914634 67728 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
9910346 64386 0 None -12 3 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at rat MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818901 64386 0 None -12 3 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at rat MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
10070016 71104 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 408 4 1 7 3.4 COc1ccc2oc(O)c/c(=N\C3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm050598r
CHEMBL196208 71104 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 408 4 1 7 3.4 COc1ccc2oc(O)c/c(=N\C3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm050598r
11775399 63015 0 None -2 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL179501 63015 0 None -2 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0490890
11495754 71573 0 None 588 2 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL197245 71573 0 None 588 2 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
57404360 72785 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 6 1 6 4.2 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C[C@@H]1c1cc(F)c(F)cc1F 10.1016/j.bmcl.2012.02.010
CHEMBL2011534 72785 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 6 1 6 4.2 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C[C@@H]1c1cc(F)c(F)cc1F 10.1016/j.bmcl.2012.02.010
49865653 15851 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223709 15851 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
49865678 15869 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 497 9 2 6 5.7 COc1ccc(-n2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2010.07.086
CHEMBL1223767 15869 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 497 9 2 6 5.7 COc1ccc(-n2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2010.07.086
10183297 92867 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL245231 92867 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1021/jm060383x
44394909 66684 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 504 10 3 6 4.6 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCOCC1 10.1016/j.bmcl.2004.07.077
CHEMBL187093 66684 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 504 10 3 6 4.6 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCOCC1 10.1016/j.bmcl.2004.07.077
44394856 65788 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 380 6 3 6 3.1 Nc1ccc2cccc(OCCCNC(=O)Nc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184080 65788 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 380 6 3 6 3.1 Nc1ccc2cccc(OCCCNC(=O)Nc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
46850893 59396 0 None -3 2 Human 6.0 pIC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 5.0 COc1ccc(Oc2c(Cl)cnn(-c3cc(Cl)cc(Cl)c3)c2=O)cc1 nan
CHEMBL1723963 59396 0 None -3 2 Human 6.0 pIC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 5.0 COc1ccc(Oc2c(Cl)cnn(-c3cc(Cl)cc(Cl)c3)c2=O)cc1 nan
46172926 59011 0 None -10 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.4 CCOc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1706758 59011 0 None -10 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.4 CCOc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
46861572 125332 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 390 7 0 3 3.9 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCC3)cc2C1 nan
CHEMBL3648376 125332 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 390 7 0 3 3.9 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCC3)cc2C1 nan
46172933 59536 0 None -3 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 314 3 1 5 3.4 O=c1c(Oc2ccc(O)cc2)c(Cl)cnn1-c1ccccc1 nan
CHEMBL1729376 59536 0 None -3 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 314 3 1 5 3.4 O=c1c(Oc2ccc(O)cc2)c(Cl)cnn1-c1ccccc1 nan
3247171 23111 1 None -1 3 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 579 7 0 5 4.9 COC(=O)[C@@]1(Cc2ccc(F)cc2)[C@H]2c3cc(C(=O)N(C)C)n(Cc4ccccc4)c3C[C@H]2CN1C(=O)c1ccccc1 nan
CHEMBL1332346 23111 1 None -1 3 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 579 7 0 5 4.9 COC(=O)[C@@]1(Cc2ccc(F)cc2)[C@H]2c3cc(C(=O)N(C)C)n(Cc4ccccc4)c3C[C@H]2CN1C(=O)c1ccccc1 nan
23603500 21612 6 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 421 9 1 5 4.0 CCN(CC)CCNC(=O)CCc1c(C)nc2c(c(C)nn2-c2ccc(C)cc2)c1C nan
CHEMBL1319565 21612 6 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 421 9 1 5 4.0 CCN(CC)CCNC(=O)CCc1c(C)nc2c(c(C)nn2-c2ccc(C)cc2)c1C nan
49866035 16039 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 498 8 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224305 16039 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 498 8 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417961 81651 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 525 11 5 3 3.9 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL216564 81651 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 525 11 5 3 3.9 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
44394866 123817 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 397 9 2 4 4.9 CCCNc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363683 123817 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 397 9 2 4 4.9 CCCNc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
16438224 51999 12 None - 1 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 416 8 1 4 4.4 COc1ccc(C(CNC(=O)COc2ccc(Cl)c(C)c2)N2CCCCC2)cc1 nan
CHEMBL1589201 51999 12 None - 1 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 416 8 1 4 4.4 COc1ccc(C(CNC(=O)COc2ccc(Cl)c(C)c2)N2CCCCC2)cc1 nan
54580459 60244 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 504 11 1 6 4.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760063 60244 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 504 11 1 6 4.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(OC)c2)cc1 10.1016/j.bmcl.2011.02.046
46846318 59314 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 408 5 0 5 3.3 O=C(C1CCCCN1Cc1ccccc1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1720892 59314 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 408 5 0 5 3.3 O=C(C1CCCCN1Cc1ccccc1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
58062375 125350 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 6 0 4 3.9 CN1CCCC1c1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cn1)C2 nan
CHEMBL3648394 125350 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 6 0 4 3.9 CN1CCCC1c1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cn1)C2 nan
44394807 65871 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 425 4 1 5 4.0 CC(C)(C)c1ccc(S(=O)(=O)N2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL184482 65871 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 425 4 1 5 4.0 CC(C)(C)c1ccc(S(=O)(=O)N2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
44405646 96412 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 511 6 1 9 3.5 O=C(CN1CCOCC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL265540 96412 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 511 6 1 9 3.5 O=C(CN1CCOCC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
70691649 73093 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 6 1 7 3.9 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016703 73093 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 6 1 7 3.9 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
58062307 125336 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 420 7 1 4 3.3 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CC[C@H](O)C3)cc2C1 nan
CHEMBL3648380 125336 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 420 7 1 4 3.3 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CC[C@H](O)C3)cc2C1 nan
11562129 70718 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195250 70718 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44562442 178600 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 505 7 1 4 5.9 CC(c1ccn(-c2ccc(C(F)(F)F)cc2)c1)N1CCC(NC(=O)COc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472379 178600 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 505 7 1 4 5.9 CC(c1ccn(-c2ccc(C(F)(F)F)cc2)c1)N1CCC(NC(=O)COc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2008.07.079
58062320 125331 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 422 11 1 4 3.8 COCCCNCc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
CHEMBL3648375 125331 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 422 11 1 4 3.8 COCCCNCc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
46188959 121235 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 427 6 1 6 3.8 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.05.008
CHEMBL3589135 121235 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 427 6 1 6 3.8 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.05.008
44442151 93559 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cc(C#N)ccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248673 93559 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cc(C#N)ccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
2810388 42238 5 None - 1 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 380 4 1 3 4.9 O=C(NCc1cccnc1)c1cc(-c2ccc(Cl)cc2)oc1C(F)(F)F nan
CHEMBL1499675 42238 5 None - 1 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 380 4 1 3 4.9 O=C(NCc1cccnc1)c1cc(-c2ccc(Cl)cc2)oc1C(F)(F)F nan
44414520 79846 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213932 79846 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
11547011 141070 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 455 5 0 6 5.0 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(C)c1 10.1016/j.bmcl.2006.05.075
CHEMBL385141 141070 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 455 5 0 6 5.0 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(C)c1 10.1016/j.bmcl.2006.05.075
11610423 165455 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL425518 165455 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2006.05.075
52918016 60307 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 555 11 1 5 5.1 COc1ccc([C@H]2CN(CCCN(C)S(=O)(=O)c3ccccc3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760250 60307 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 555 11 1 5 5.1 COc1ccc([C@H]2CN(CCCN(C)S(=O)(=O)c3ccccc3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
18436082 74526 0 None 57 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 459 5 1 3 6.5 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1Cl)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031732 74526 0 None 57 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 459 5 1 3 6.5 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1Cl)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
70689612 73242 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 539 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017744 73242 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 539 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11635674 200154 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of MCH-stimulated G-protein/[35S]GTPcS binding in CHO cells expressing human MCH1 receptorInhibition of MCH-stimulated G-protein/[35S]GTPcS binding in CHO cells expressing human MCH1 receptor
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607121 200154 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of MCH-stimulated G-protein/[35S]GTPcS binding in CHO cells expressing human MCH1 receptorInhibition of MCH-stimulated G-protein/[35S]GTPcS binding in CHO cells expressing human MCH1 receptor
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
11496313 71953 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL198361 71953 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44416956 79820 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 541 6 0 8 6.2 COc1ccc(Cn2c(N(C)C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL213824 79820 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 541 6 0 8 6.2 COc1ccc(Cn2c(N(C)C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44416995 82665 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 465 5 1 8 4.2 CN(C)c1nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2n1CCO 10.1016/j.bmcl.2006.07.054
CHEMBL218186 82665 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 465 5 1 8 4.2 CN(C)c1nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2n1CCO 10.1016/j.bmcl.2006.07.054
44416348 80809 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 462 7 1 8 4.2 COc1cc(-n2cnc3cc(-c4ccc(N)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL215862 80809 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 462 7 1 8 4.2 COc1cc(-n2cnc3cc(-c4ccc(N)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44414589 79739 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 473 4 0 7 4.0 CN(C)C1CCN(c2ccc(-c3coc4cc(C5=CCC6OCCOC6C5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213459 79739 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 473 4 0 7 4.0 CN(C)C1CCN(c2ccc(-c3coc4cc(C5=CCC6OCCOC6C5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
45484995 196832 0 None 1 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577904 196832 0 None 1 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
11713742 93117 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 552 8 2 6 4.3 O=C(CCN1CCCCC1)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL246464 93117 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 552 8 2 6 4.3 O=C(CCN1CCCCC1)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
11570031 73136 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 529 7 1 7 4.9 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016774 73136 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 529 7 1 7 4.9 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44397202 66873 0 None -12 2 Mouse 6.9 pIC50 = 6.9 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 398 6 1 6 2.8 COc1cc(OC)cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187916 66873 0 None -12 2 Mouse 6.9 pIC50 = 6.9 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 398 6 1 6 2.8 COc1cc(OC)cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
127032787 138615 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 445 6 0 5 4.9 Cc1oc(-c2ccccc2)nc1C(=O)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787237 138615 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 445 6 0 5 4.9 Cc1oc(-c2ccccc2)nc1C(=O)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
10319824 66731 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 417 8 2 4 3.9 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL187288 66731 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 417 8 2 4 3.9 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN(C)C 10.1016/j.bmcl.2004.07.077
46835812 59204 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 424 5 0 5 5.7 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC(F)(F)F)cc3)c2=O)cc1 nan
CHEMBL1716158 59204 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 424 5 0 5 5.7 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC(F)(F)F)cc3)c2=O)cc1 nan
5810215 26184 9 None -2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 460 7 2 6 4.3 COc1cc(/C=C(\C#N)C(=O)Nc2ccc(C(=O)O)cc2)ccc1OC(=O)c1cccc(F)c1 nan
CHEMBL1359426 26184 9 None -2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 460 7 2 6 4.3 COc1cc(/C=C(\C#N)C(=O)Nc2ccc(C(=O)O)cc2)ccc1OC(=O)c1cccc(F)c1 nan
45269336 194298 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL559801 194298 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
58062364 125334 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 418 9 1 3 4.6 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC3(C)CC3)cc2C1 nan
CHEMBL3648378 125334 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 418 9 1 3 4.6 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC3(C)CC3)cc2C1 nan
5091342 51506 6 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 501 7 1 5 4.8 Cc1ccccc1CN1C(=O)c2ccccc2Sc2ccc(C(=O)NCCCN3CCOCC3)cc21 nan
CHEMBL1585038 51506 6 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 501 7 1 5 4.8 Cc1ccccc1CN1C(=O)c2ccccc2Sc2ccc(C(=O)NCCCN3CCOCC3)cc21 nan
45273642 194771 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 398 5 1 5 4.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
CHEMBL563096 194771 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 398 5 1 5 4.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
44562545 188504 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cnc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL510193 188504 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cnc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
46835786 59264 0 None -8 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cc(C)ccc3C)c2=O)cc1 nan
CHEMBL1718965 59264 0 None -8 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cc(C)ccc3C)c2=O)cc1 nan
58062388 125329 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 448 9 1 4 4.2 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC3CCOCC3)cc2C1 nan
CHEMBL3648373 125329 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 448 9 1 4 4.2 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC3CCOCC3)cc2C1 nan
44416363 79950 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 465 7 0 7 4.8 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)oc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL214427 79950 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 465 7 0 7 4.8 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)oc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
1479656 59460 13 None -9 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C)c3C)c2=O)cc1 nan
CHEMBL1726382 59460 13 None -9 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C)c3C)c2=O)cc1 nan
24856245 45855 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 335 7 1 3 4.8 CCC(C)CCN1C(Nc2ccccc2)=NC[C@@H]1Cc1ccccc1 nan
CHEMBL1533829 45855 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 335 7 1 3 4.8 CCC(C)CCN1C(Nc2ccccc2)=NC[C@@H]1Cc1ccccc1 nan
2982342 54857 8 None 2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 306 6 1 4 4.2 CCOc1ccc([N+](=O)[O-])cc1CNC1CCCCCCC1 nan
CHEMBL1342885 54857 8 None 2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 306 6 1 4 4.2 CCOc1ccc([N+](=O)[O-])cc1CNC1CCCCCCC1 nan
CHEMBL1617311 54857 8 None 2 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 306 6 1 4 4.2 CCOc1ccc([N+](=O)[O-])cc1CNC1CCCCCCC1 nan
11995644 81942 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3ccccc3Cl)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL217228 81942 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3ccccc3Cl)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
44416297 96517 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 525 8 0 9 4.0 COc1cc(-n2cnc3cc(-c4ccc(S(C)(=O)=O)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL266415 96517 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 525 8 0 9 4.0 COc1cc(-n2cnc3cc(-c4ccc(S(C)(=O)=O)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44394592 65416 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 376 5 2 5 3.4 CC(=O)Nc1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL183468 65416 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 376 5 2 5 3.4 CC(=O)Nc1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
45382326 59510 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2cnn(-c3ccc(C)cc3)c(=O)c2Cl)cc1 nan
CHEMBL1728485 59510 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2cnn(-c3ccc(C)cc3)c(=O)c2Cl)cc1 nan
16191617 50448 1 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 419 7 1 5 4.3 COc1cccc(CC2(CO)CCCN(Cc3c(C)cc(C)cc3-n3cccn3)C2)c1 nan
CHEMBL1576145 50448 1 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 419 7 1 5 4.3 COc1cccc(CC2(CO)CCCN(Cc3c(C)cc(C)cc3-n3cccn3)C2)c1 nan
44442153 93600 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c(C#N)cccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248863 93600 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c(C#N)cccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
46835820 59486 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 364 6 0 5 4.7 CCc1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
CHEMBL1727473 59486 0 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 364 6 0 5 4.7 CCc1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
2386953 54966 3 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 2 0 1 5.7 FC(F)(F)c1cccc(C[n+]2c3n(c4ccc(C(F)(F)F)cc42)CCCCC3)c1 nan
CHEMBL1339438 54966 3 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 2 0 1 5.7 FC(F)(F)c1cccc(C[n+]2c3n(c4ccc(C(F)(F)F)cc42)CCCCC3)c1 nan
CHEMBL1618129 54966 3 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 2 0 1 5.7 FC(F)(F)c1cccc(C[n+]2c3n(c4ccc(C(F)(F)F)cc42)CCCCC3)c1 nan
23027035 196860 0 None 9 4 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1ccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)cc1 10.1016/j.bmcl.2009.09.003
CHEMBL578170 196860 0 None 9 4 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1ccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)cc1 10.1016/j.bmcl.2009.09.003
11583049 141404 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)cc2o1 10.1021/jm060683e
CHEMBL387178 141404 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)cc2o1 10.1021/jm060683e
44430459 86722 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 525 4 0 6 5.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232662 86722 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 525 4 0 6 5.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCCC2)C1 10.1016/j.bmcl.2007.02.012
16718619 121238 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.05.008
CHEMBL3589154 121238 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.05.008
70691736 73239 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 541 6 1 7 4.8 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017741 73239 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 541 6 1 7 4.8 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70693807 73240 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 555 6 1 7 4.3 Cc1nc(N2CCC(N3CCOCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017742 73240 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 555 6 1 7 4.3 Cc1nc(N2CCC(N3CCOCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
10369833 92121 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 533 10 2 3 6.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1 10.1021/jm060381c
CHEMBL243338 92121 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 533 10 2 3 6.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1 10.1021/jm060381c
44414481 138358 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 480 4 0 6 5.1 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5cnccc5C(F)(F)F)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL378283 138358 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 480 4 0 6 5.1 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5cnccc5C(F)(F)F)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
54580457 60240 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760059 60240 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
10456385 91694 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242054 91694 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccccc2)CC1 10.1021/jm060381c
44394606 66902 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 351 6 2 6 3.1 CC(CNCc1ccc2c(c1)OCO2)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL188058 66902 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 351 6 2 6 3.1 CC(CNCc1ccc2c(c1)OCO2)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44397008 66553 0 None -2 2 Mouse 6.9 pIC50 = 6.9 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 368 5 1 5 2.8 COc1cccc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186469 66553 0 None -2 2 Mouse 6.9 pIC50 = 6.9 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 368 5 1 5 2.8 COc1cccc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
16756405 92421 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 392 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)c(C)c3)CC2)c1 10.1021/jm060383x
CHEMBL244004 92421 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 392 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)c(C)c3)CC2)c1 10.1021/jm060383x
9955811 65825 0 None 10 2 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 458 8 3 4 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184292 65825 0 None 10 2 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 458 8 3 4 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
10377822 126290 1 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 5 1 3 4.0 CCC(CC)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL365459 126290 1 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 5 1 3 4.0 CCC(CC)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
135519896 71739 4 None - 1 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 343 3 2 6 3.2 C/N=c1\scc(-c2ccc(F)cc2)n1/N=C/c1ccc(O)c(O)c1 nan
CHEMBL1977747 71739 4 None - 1 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 343 3 2 6 3.2 C/N=c1\scc(-c2ccc(F)cc2)n1/N=C/c1ccc(O)c(O)c1 nan
90666255 108864 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 494 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C(C)C)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219264 108864 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 494 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C(C)C)cc3)CC2)c1 10.1039/C1MD00015B
3338232 39189 7 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 391 7 1 3 6.3 CC(NCCC1(Cc2ccccc2Cl)CCOC(C)(C)C1)c1cccs1 nan
CHEMBL1471999 39189 7 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 391 7 1 3 6.3 CC(NCCC1(Cc2ccccc2Cl)CCOC(C)(C)C1)c1cccs1 nan
22254604 123345 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 2 1 3 3.8 CC1CCCCC1Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL362713 123345 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 2 1 3 3.8 CC1CCCCC1Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
952248 46280 17 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 3 2 2 3.4 Cc1cccc(NC(=S)NC(=O)Cc2ccccc2)c1C nan
CHEMBL1537947 46280 17 None -1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 3 2 2 3.4 Cc1cccc(NC(=S)NC(=O)Cc2ccccc2)c1C nan
46846336 59456 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 374 5 0 6 4.6 COc1ccc(Oc2c(-c3ccco3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1726190 59456 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 374 5 0 6 4.6 COc1ccc(Oc2c(-c3ccco3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
11592099 93056 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 554 8 2 6 3.8 O=C(NCCN1CCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(Cl)c1 10.1016/j.bmcl.2006.11.068
CHEMBL246258 93056 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 554 8 2 6 3.8 O=C(NCCN1CCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(Cl)c1 10.1016/j.bmcl.2006.11.068
44410904 171880 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL448110 171880 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11974131 141442 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 431 4 1 7 2.8 N#Cc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL387417 141442 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 431 4 1 7 2.8 N#Cc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
90666251 108860 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 596 7 1 5 7.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C(F)(F)F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219260 108860 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 596 7 1 5 7.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C(F)(F)F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
45382325 59130 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 312 3 0 4 4.0 Cc1ccc(-n2ncc(Cl)c(Oc3ccccc3)c2=O)cc1 nan
CHEMBL1712328 59130 0 None 1 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 312 3 0 4 4.0 Cc1ccc(-n2ncc(Cl)c(Oc3ccccc3)c2=O)cc1 nan
44405431 71592 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 368 4 2 3 4.9 Cc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1C 10.1016/j.bmcl.2005.08.049
CHEMBL197283 71592 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 368 4 2 3 4.9 Cc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1C 10.1016/j.bmcl.2005.08.049
46892535 125328 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 432 7 0 3 5.1 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCCCCC3)cc2C1 nan
CHEMBL3648372 125328 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 432 7 0 3 5.1 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCCCCC3)cc2C1 nan
54579973 60303 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 470 9 1 4 5.6 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760245 60303 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 470 9 1 4 5.6 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
18436120 74515 0 None 123 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 442 5 1 4 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)nc1 10.1021/jm201596h
CHEMBL2031721 74515 0 None 123 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 442 5 1 4 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)nc1 10.1021/jm201596h
70693734 73115 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 528 8 1 7 5.1 Cc1nc(N2CCC(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016726 73115 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 528 8 1 7 5.1 Cc1nc(N2CCC(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70687551 73255 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 499 6 2 6 3.8 Cc1nc(N2CCC(NS(C)(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017757 73255 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 499 6 2 6 3.8 Cc1nc(N2CCC(NS(C)(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70691738 73260 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 543 8 2 7 4.2 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017762 73260 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 543 8 2 7 4.2 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
24857598 18914 12 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium releaseAntagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium release
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289283 18914 12 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium releaseAntagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium release
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
11655872 71358 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL196567 71358 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
10027853 71503 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197026 71503 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
50908737 18930 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCH-1 receptorAntagonist activity at MCH-1 receptor
ChEMBL 385 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289395 18930 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCH-1 receptorAntagonist activity at MCH-1 receptor
ChEMBL 385 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
54587368 60249 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 521 10 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(N(C)C)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760077 60249 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 521 10 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(N(C)C)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
57404359 72782 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 474 6 1 6 4.0 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C[C@@H]1c1cc(F)ccc1F 10.1016/j.bmcl.2012.02.010
CHEMBL2011528 72782 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 474 6 1 6 4.0 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C[C@@H]1c1cc(F)ccc1F 10.1016/j.bmcl.2012.02.010
127033672 138479 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 463 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)cn4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785819 138479 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 463 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)cn4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
89690365 137634 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769550 137634 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
16755969 91869 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 10 2 3 6.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL242902 91869 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 10 2 3 6.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44394764 122640 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 7 2 4 4.1 CC(C)c1ccc(C(=O)NCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
CHEMBL361262 122640 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 7 2 4 4.1 CC(C)c1ccc(C(=O)NCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
9895868 69224 0 None -61 3 Human 6.9 pIC50 = 6.9 Functional
Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 induced calcium flux stably expressed in HEK293 cells (n=6)Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 induced calcium flux stably expressed in HEK293 cells (n=6)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193438 69224 0 None -61 3 Human 6.9 pIC50 = 6.9 Functional
Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 induced calcium flux stably expressed in HEK293 cells (n=6)Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 induced calcium flux stably expressed in HEK293 cells (n=6)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
16756640 92833 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cc(Cl)cc(Cl)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL245008 92833 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cc(Cl)cc(Cl)c4)c3)CC2)c1 10.1021/jm060383x
11994910 79989 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 542 7 1 6 6.1 O=C(NCCCN1CCCC1)c1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2c1 10.1021/jm060814b
CHEMBL214571 79989 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 542 7 1 6 6.1 O=C(NCCCN1CCCC1)c1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2c1 10.1021/jm060814b
70681198 73211 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 509 9 3 7 3.5 Cc1nc(NCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017614 73211 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 509 9 3 7 3.5 Cc1nc(NCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
46850887 59371 0 None -5 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 353 4 0 6 3.6 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C#N)c3)c2=O)cc1 nan
CHEMBL1723067 59371 0 None -5 2 Human 4.9 pIC50 = 4.9 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 353 4 0 6 3.6 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C#N)c3)c2=O)cc1 nan
49865868 15985 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 460 7 2 5 6.1 Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224079 15985 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 460 7 2 5 6.1 Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
58062381 125330 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 420 8 1 3 4.9 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC(C)(C)C)cc2C1 nan
CHEMBL3648374 125330 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 420 8 1 3 4.9 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CNCC(C)(C)C)cc2C1 nan
58062316 125339 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 450 8 1 4 4.6 CN(C(=O)c1ccc(OC[C@@H]2CCCO2)cc1)[C@@H]1Cc2ccc(CNCC(C)(C)C)cc2C1 nan
CHEMBL3648383 125339 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 450 8 1 4 4.6 CN(C(=O)c1ccc(OC[C@@H]2CCCO2)cc1)[C@@H]1Cc2ccc(CNCC(C)(C)C)cc2C1 nan
10255474 123141 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2ccc(Nc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL362094 123141 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2ccc(Nc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
11510669 188700 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 448 7 1 5 4.2 N#Cc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL512180 188700 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 448 7 1 5 4.2 N#Cc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
70693795 73197 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 497 6 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(N4CCCC4)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017600 73197 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 497 6 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(N4CCCC4)cc3)cc12 10.1016/j.bmcl.2012.03.049
45382320 59664 0 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 428 9 0 6 4.6 CCOc1ccc(CCOc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1OCC nan
CHEMBL1734525 59664 0 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 428 9 0 6 4.6 CCOc1ccc(CCOc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1OCC nan
70687470 73099 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 3.7 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016710 73099 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 3.7 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
49865977 16027 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 456 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224231 16027 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 456 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
58062334 125333 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 392 8 0 3 4.2 CCN(C)Cc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
CHEMBL3648377 125333 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 392 8 0 3 4.2 CCN(C)Cc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
58062344 125346 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 465 10 1 5 4.4 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CNCC4(C)CCOCC4)cc3C2)nc1 nan
CHEMBL3648390 125346 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 465 10 1 5 4.4 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CNCC4(C)CCOCC4)cc3C2)nc1 nan
70691333 77603 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 453 9 1 4 5.5 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL2096766 77603 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 453 9 1 4 5.5 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm0490890
135693566 23544 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 461 7 1 6 4.3 COCCNC1=N[C@@H](c2cccc(C(F)(F)F)c2)C(C(=O)OC)=C(C)N1Cc1ccccc1 nan
CHEMBL1335685 23544 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 461 7 1 6 4.3 COCCNC1=N[C@@H](c2cccc(C(F)(F)F)c2)C(C(=O)OC)=C(C)N1Cc1ccccc1 nan
11539632 70202 0 None -1412 11 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 70202 0 None -1412 11 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
44414432 77569 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 411 4 0 5 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL209542 77569 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 411 4 0 5 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
90666094 108826 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 546 7 1 5 6.7 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3218997 108826 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 546 7 1 5 6.7 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
44430468 91915 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 537 5 0 7 4.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(Cc2ccoc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL243045 91915 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 537 5 0 7 4.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(Cc2ccoc2)C1 10.1016/j.bmcl.2007.02.012
127031622 138647 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 498 8 0 7 4.6 O=C(c1nnc(-c2ccc(OC(F)F)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787639 138647 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 498 8 0 7 4.6 O=C(c1nnc(-c2ccc(OC(F)F)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
11511776 188701 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 507 8 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(OC(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL512185 188701 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 507 8 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(OC(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
70681213 73241 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 6 5.5 Cc1nc(N2CCC(N3CCCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017743 73241 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 6 5.5 Cc1nc(N2CCC(N3CCCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11520239 3562 4 None - 1 Human 7.8 pIC50 = 7.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
1313 3562 4 None - 1 Human 7.8 pIC50 = 7.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
CHEMBL185271 3562 4 None - 1 Human 7.8 pIC50 = 7.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
4219492 71078 1 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196091 71078 1 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
44417043 80946 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 433 4 2 6 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(NC3CC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL215932 80946 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 433 4 2 6 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(NC3CC3)nc2c1 10.1016/j.bmcl.2006.07.054
44417067 141448 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 3 1 7 4.5 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCOCC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL387438 141448 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 3 1 7 4.5 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCOCC3)nc2c1 10.1016/j.bmcl.2006.07.054
54584908 60300 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 505 9 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2Cc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760242 60300 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 505 9 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2Cc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
127031909 138609 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1noc(-c2ccccc2)n1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787166 138609 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1noc(-c2ccccc2)n1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
70685336 73092 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCN(C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016702 73092 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCN(C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44394683 66857 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 313 6 2 5 3.4 CC(CNCc1ccsc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL187847 66857 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 313 6 2 5 3.4 CC(CNCc1ccsc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
46850894 59033 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 464 4 0 5 5.7 COc1ccc(Oc2c(Cl)cnn(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)c2=O)cc1 nan
CHEMBL1707830 59033 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 464 4 0 5 5.7 COc1ccc(Oc2c(Cl)cnn(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)c2=O)cc1 nan
2827417 54208 9 None -1 4 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 11 2 4 2.0 C#CC(CO)N(CCN(Cc1ccccc1)C(C#C)CO)Cc1ccccc1 nan
CHEMBL1609915 54208 9 None -1 4 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 11 2 4 2.0 C#CC(CO)N(CCN(Cc1ccccc1)C(C#C)CO)Cc1ccccc1 nan
3732471 38637 7 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 435 4 1 4 4.2 COC(=O)C(O)(c1ccc(N(C)C(=O)c2ccc(Cl)c(Cl)c2)cc1)C(F)(F)F nan
CHEMBL1467280 38637 7 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 435 4 1 4 4.2 COC(=O)C(O)(c1ccc(N(C)C(=O)c2ccc(Cl)c(Cl)c2)cc1)C(F)(F)F nan
54585833 60283 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 494 9 1 5 5.0 COc1ccc([C@H]2CN(Cc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760222 60283 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 494 9 1 5 5.0 COc1ccc([C@H]2CN(Cc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
54585862 60291 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 469 9 2 4 4.6 COc1ccc([C@H]2CN(CCCC3CCNCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760230 60291 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 469 9 2 4 4.6 COc1ccc([C@H]2CN(CCCC3CCNCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
49865654 15852 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 467 8 2 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccccc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223710 15852 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 467 8 2 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccccc3)CC2)c1 10.1016/j.bmcl.2010.07.086
70689526 73145 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 558 7 2 7 5.8 Cc1nc(N2CCC(O)(C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016782 73145 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 558 7 2 7 5.8 Cc1nc(N2CCC(O)(C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
1129890 55850 14 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 490 9 1 4 5.2 CCCC(CCC)C(=O)Nc1ccc2c(c1)N(C(=O)CCN1CCN(C)CC1)c1ccccc1CC2 nan
CHEMBL1578660 55850 14 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 490 9 1 4 5.2 CCCC(CCC)C(=O)Nc1ccc2c(c1)N(C(=O)CCN1CCN(C)CC1)c1ccccc1CC2 nan
CHEMBL1625981 55850 14 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 490 9 1 4 5.2 CCCC(CCC)C(=O)Nc1ccc2c(c1)N(C(=O)CCN1CCN(C)CC1)c1ccccc1CC2 nan
70681116 73101 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 493 6 1 6 4.1 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016712 73101 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 493 6 1 6 4.1 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44416255 79624 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 448 7 0 8 4.0 COc1cc(-n2cnc3cc(-c4cccnc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212963 79624 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 448 7 0 8 4.0 COc1cc(-n2cnc3cc(-c4cccnc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
2766793 49793 12 None 2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 355 6 0 7 3.0 CCOC(=O)C(C)On1c(-c2ccccc2)nc2ccc([N+](=O)[O-])cc21 nan
CHEMBL1569862 49793 12 None 2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 355 6 0 7 3.0 CCOC(=O)C(C)On1c(-c2ccccc2)nc2ccc([N+](=O)[O-])cc21 nan
4439874 51197 2 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 382 4 1 3 4.7 O=C(NC1CCCCCCC1)C1c2ccccc2C(=O)N1Cc1cccs1 nan
CHEMBL1582511 51197 2 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 382 4 1 3 4.7 O=C(NC1CCCCCCC1)C1c2ccccc2C(=O)N1Cc1cccs1 nan
46835815 58992 0 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 408 4 0 4 6.1 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(Cl)c(Cl)c3)c2=O)cc1 nan
CHEMBL1705920 58992 0 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 408 4 0 4 6.1 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(Cl)c(Cl)c3)c2=O)cc1 nan
2709719 26193 7 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 394 7 1 3 3.5 CN(c1ccccc1)S(=O)(=O)c1ccc(C(=O)NCCc2ccccc2)cc1 nan
CHEMBL1359489 26193 7 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 394 7 1 3 3.5 CN(c1ccccc1)S(=O)(=O)c1ccc(C(=O)NCCc2ccccc2)cc1 nan
23027245 195442 0 None 10 5 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL567791 195442 0 None 10 5 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
11683903 82003 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 454 5 1 7 3.1 COc1cc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2cc1F 10.1021/jm060683e
CHEMBL217442 82003 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 454 5 1 7 3.1 COc1cc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2cc1F 10.1021/jm060683e
71226964 128646 0 None -5 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3670638 128646 0 None -5 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11599186 73137 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016775 73137 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
16718619 121238 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3589154 121238 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
4033 1860 42 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
9826520 1860 42 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
CHEMBL214957 1860 42 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
60150483 73190 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 462 5 2 5 5.0 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017593 73190 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 462 5 2 5 5.0 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70685409 73246 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 575 6 1 7 4.5 Cc1nc(N2CCC(N3CCCS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017748 73246 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 575 6 1 7 4.5 Cc1nc(N2CCC(N3CCCS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11583744 71365 0 None 1 3 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196581 71365 0 None 1 3 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
10005009 165812 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL427540 165812 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
54586330 60241 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 542 10 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760060 60241 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 542 10 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.02.046
11374857 79794 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 472 6 1 7 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(OC(F)F)cc2o1 10.1021/jm060683e
CHEMBL213715 79794 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 472 6 1 7 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(OC(F)F)cc2o1 10.1021/jm060683e
70681114 73097 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 1 6 4.3 Cc1nc(N2CCN(C(=O)CC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016708 73097 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 1 6 4.3 Cc1nc(N2CCN(C(=O)CC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
54582960 60294 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 10 0 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)N(C)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760235 60294 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 10 0 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)N(C)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44394639 66358 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL185558 66358 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
2948187 52582 10 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 350 2 1 5 4.8 Clc1ccc(C2CC(c3cccs3)n3ncnc3N2)cc1Cl nan
CHEMBL1595687 52582 10 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 350 2 1 5 4.8 Clc1ccc(C2CC(c3cccs3)n3ncnc3N2)cc1Cl nan
20854116 25205 6 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 539 7 1 5 5.2 O=C(NCCCN1CCOCC1)c1ccc2c(c1)N(Cc1c(F)cccc1Cl)C(=O)c1ccccc1S2 nan
CHEMBL1350024 25205 6 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 539 7 1 5 5.2 O=C(NCCCN1CCOCC1)c1ccc2c(c1)N(Cc1c(F)cccc1Cl)C(=O)c1ccccc1S2 nan
11611530 134269 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 421 3 1 5 4.8 Cn1ccc2ccc(CN3CCC(/N=c4\cc(O)oc5ccc(Cl)cc45)CC3)cc21 10.1021/jm050598r
CHEMBL371877 134269 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 421 3 1 5 4.8 Cn1ccc2ccc(CN3CCC(/N=c4\cc(O)oc5ccc(Cl)cc45)CC3)cc21 10.1021/jm050598r
70695853 73107 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 426 5 2 6 3.6 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016718 73107 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 426 5 2 6 3.6 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11553316 71275 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ocnc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL196350 71275 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ocnc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
45269335 194779 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 388 4 1 6 3.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563156 194779 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 388 4 1 6 3.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
11155432 82061 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 461 8 1 6 4.0 Cc1nc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL217712 82061 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 461 8 1 6 4.0 Cc1nc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
16190353 24474 6 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 445 9 0 5 4.0 CCCCN(C)C(=O)c1nc2ccccn2c1CN1CCN(C/C=C/c2ccccc2)CC1 nan
CHEMBL1343746 24474 6 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 445 9 0 5 4.0 CCCCN(C)C(=O)c1nc2ccccn2c1CN1CCN(C/C=C/c2ccccc2)CC1 nan
786990 51691 11 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 338 4 0 3 4.0 Cc1cc(C(=O)N2CCC(Cc3ccccc3)CC2)ccc1[N+](=O)[O-] nan
CHEMBL1586617 51691 11 None 1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 338 4 0 3 4.0 Cc1cc(C(=O)N2CCC(Cc3ccccc3)CC2)ccc1[N+](=O)[O-] nan
11640515 80083 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL214768 80083 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
11640515 80083 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1021/jm060683e
CHEMBL214768 80083 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1021/jm060683e
22254551 124511 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
22254551 124511 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.034
22254551 124511 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364377 124511 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL364377 124511 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL364377 124511 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.035
17596249 33070 9 None 1 3 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 433 3 0 4 2.9 Cc1ccc(Cl)cc1N1CCN(C(=O)c2ccc3c(c2)CCN3S(C)(=O)=O)CC1 nan
CHEMBL1418691 33070 9 None 1 3 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 433 3 0 4 2.9 Cc1ccc(Cl)cc1N1CCN(C(=O)c2ccc3c(c2)CCN3S(C)(=O)=O)CC1 nan
10041636 122666 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL361305 122666 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
21940008 64379 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818809 64379 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
9910346 64386 0 None -12 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL1818901 64386 0 None -12 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11676220 56399 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccc(Cl)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642475 56399 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccc(Cl)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11505089 193129 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 568 8 1 4 6.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL538936 193129 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 568 8 1 4 6.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
70685407 73238 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 491 5 1 6 4.5 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017740 73238 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 491 5 1 6 4.5 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
54585377 60250 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccccc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760078 60250 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccccc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
54585378 60251 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 512 9 1 4 5.7 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(Cl)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760079 60251 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 512 9 1 4 5.7 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(Cl)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
54582958 60287 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc([C@H]2CN(CCc3cccc(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760226 60287 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc([C@H]2CN(CCc3cccc(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
70695929 73253 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 590 6 1 7 4.0 Cc1nc(N2CCC(N3CCN(C)S3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017755 73253 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 590 6 1 7 4.0 Cc1nc(N2CCC(N3CCN(C)S3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44394959 66859 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL187854 66859 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44394907 165428 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 422 8 3 3 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL425359 165428 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 422 8 3 3 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
46172924 59291 0 None -6 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C(C)C)c3)c2=O)cc1 nan
CHEMBL1720022 59291 0 None -6 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C(C)C)c3)c2=O)cc1 nan
1479652 51437 13 None -7 3 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1584538 51437 13 None -7 3 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
46172940 59270 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 344 3 0 4 4.4 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(F)cc3C)c2=O)cc1 nan
CHEMBL1719118 59270 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 344 3 0 4 4.4 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(F)cc3C)c2=O)cc1 nan
11974230 165448 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 438 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL425448 165448 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 438 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
800280 46404 10 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 304 3 2 1 4.7 Cc1ccc(N=C(S)NCc2ccc(Cl)cc2)c(C)c1 nan
CHEMBL1539046 46404 10 None - 1 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 304 3 2 1 4.7 Cc1ccc(N=C(S)NCc2ccc(Cl)cc2)c(C)c1 nan
58062315 125344 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 433 8 0 4 4.5 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CN4C[C@@H]5CC[C@H]4C5)cc3C2)nc1 nan
CHEMBL3648388 125344 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 433 8 0 4 4.5 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CN4C[C@@H]5CC[C@H]4C5)cc3C2)nc1 nan
22254571 66620 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 268 3 1 3 3.6 Nc1ccc2cccc(OCC3CC4CCC3C4)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186750 66620 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 268 3 1 3 3.6 Nc1ccc2cccc(OCC3CC4CCC3C4)c2n1 10.1016/j.bmcl.2004.07.032
46172927 59403 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 348 3 0 4 4.3 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(F)cc3F)c2=O)cc1 nan
CHEMBL1724285 59403 0 None -1 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 348 3 0 4 4.3 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(F)cc3F)c2=O)cc1 nan
53317307 56403 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 440 8 0 5 5.0 O=c1cc(OCc2ccc3ccccc3c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642479 56403 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 440 8 0 5 5.0 O=c1cc(OCc2ccc3ccccc3c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
44438741 93378 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 496 9 1 6 4.5 COC(C)(C)CCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL247688 93378 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 496 9 1 6 4.5 COC(C)(C)CCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
660602 54878 8 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 8 2 3 3.3 O=C(CCN(CCO)Cc1ccccc1)Nc1ccc(Br)cc1 nan
CHEMBL1314041 54878 8 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 8 2 3 3.3 O=C(CCN(CCO)Cc1ccccc1)Nc1ccc(Br)cc1 nan
CHEMBL1617460 54878 8 None -2 2 Human 4.8 pIC50 = 4.8 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 376 8 2 3 3.3 O=C(CCN(CCO)Cc1ccccc1)Nc1ccc(Br)cc1 nan
58062386 125347 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 419 7 0 4 4.1 CN(C(=O)c1ccc(OCC2CC2)cn1)[C@@H]1Cc2ccc(CN3CCCCC3)cc2C1 nan
CHEMBL3648391 125347 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 419 7 0 4 4.1 CN(C(=O)c1ccc(OCC2CC2)cn1)[C@@H]1Cc2ccc(CN3CCCCC3)cc2C1 nan
44417883 79939 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 485 9 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)c1cccc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL214383 79939 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 485 9 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)c1cccc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
89691096 138934 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assay
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794306 138934 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assay
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
23593474 64357 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818784 64357 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
11559625 56406 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 364 8 0 5 3.4 CN(C)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642484 56406 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 364 8 0 5 3.4 CN(C)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
70687473 73112 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCC(C(=O)N(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016723 73112 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCC(C(=O)N(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70685410 73249 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 569 6 1 7 5.7 Cc1nc(N2CCC(N3CC(C)(C)OC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017751 73249 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 569 6 1 7 5.7 Cc1nc(N2CCC(N3CC(C)(C)OC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
46933537 15872 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 485 8 2 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223770 15872 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 485 8 2 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417850 81231 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216362 81231 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
57391574 68496 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 412 3 1 1 6.0 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CCc3ccccc3)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922260 68496 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 412 3 1 1 6.0 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CCc3ccccc3)CC21 10.1016/j.bmcl.2011.09.110
57403783 68497 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 406 2 1 2 5.4 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CC3CCCCO3)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922261 68497 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 406 2 1 2 5.4 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CC3CCCCO3)CC21 10.1016/j.bmcl.2011.09.110
46850892 59686 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 442 5 0 5 4.0 O=C(C1CCCCN1Cc1ccc(Cl)cc1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1735215 59686 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 442 5 0 5 4.0 O=C(C1CCCCN1Cc1ccc(Cl)cc1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
70695854 73108 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 440 6 1 6 4.2 COC1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016719 73108 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 440 6 1 6 4.2 COC1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
44388559 60380 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 469 10 2 6 4.7 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ncn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL176081 60380 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 469 10 2 6 4.7 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ncn(CCN3CCCC3)c2c1 10.1021/jm0490890
44417970 97758 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2cn1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL274326 97758 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2cn1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
70695916 73208 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 382 6 3 5 3.6 Cc1nc(NCCO)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017611 73208 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 382 6 3 5 3.6 Cc1nc(NCCO)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44405518 139816 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 390 4 2 3 5.4 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5ccccc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL380782 139816 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 390 4 2 3 5.4 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5ccccc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
46172915 59198 0 None -2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.4 CCOc1ccc(Oc2cnn(-c3ccc(C)cc3)c(=O)c2Cl)cc1 nan
CHEMBL1715946 59198 0 None -2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.4 CCOc1ccc(Oc2cnn(-c3ccc(C)cc3)c(=O)c2Cl)cc1 nan
24892611 55587 3 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 587 10 0 8 3.9 CCOC(=O)N1CCN(S(=O)(=O)c2ccc(C(=O)N(CCCN(C)C)c3nc4ccc(CC)cc4s3)cc2)CC1 nan
CHEMBL1538063 55587 3 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 587 10 0 8 3.9 CCOC(=O)N1CCN(S(=O)(=O)c2ccc(C(=O)N(CCCN(C)C)c3nc4ccc(CC)cc4s3)cc2)CC1 nan
CHEMBL1623531 55587 3 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 587 10 0 8 3.9 CCOC(=O)N1CCN(S(=O)(=O)c2ccc(C(=O)N(CCCN(C)C)c3nc4ccc(CC)cc4s3)cc2)CC1 nan
49865928 16004 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 513 9 2 5 6.4 CC(C)C(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224153 16004 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 513 9 2 5 6.4 CC(C)C(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
12005269 39962 5 None 2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 453 4 2 4 3.9 Cc1ccc(N2C(=O)C3C4C=CC(CN=C(S)Nc5ccc(Cl)cc5)(O4)C3C2=O)cc1 nan
CHEMBL1480448 39962 5 None 2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 453 4 2 4 3.9 Cc1ccc(N2C(=O)C3C4C=CC(CN=C(S)Nc5ccc(Cl)cc5)(O4)C3C2=O)cc1 nan
11560917 123521 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 424 4 1 5 5.7 O=c1cc(NC2CCN(Cc3ccc4sccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL363139 123521 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 424 4 1 5 5.7 O=c1cc(NC2CCN(Cc3ccc4sccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44405519 72011 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 5 4.1 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL198588 72011 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 5 4.1 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
11995343 79999 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 600 7 0 9 4.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(CCN4CCOCC4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL214604 79999 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 600 7 0 9 4.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(CCN4CCOCC4)CC3)ccc2c1 10.1021/jm060572f
1314 3657 18 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm8016199
9865843 3657 18 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm8016199
CHEMBL178707 3657 18 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm8016199
56598528 138527 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 450 8 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC(OC)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786350 138527 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 450 8 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC(OC)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
89690574 137784 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771182 137784 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
24780883 56404 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 404 8 0 5 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642482 56404 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 404 8 0 5 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCCC2)cc1 10.1016/j.bmc.2010.12.002
44557554 194727 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 528 10 2 4 5.8 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL562847 194727 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 528 10 2 4 5.8 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
70681217 73258 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 493 7 2 6 4.0 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017760 73258 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 493 7 2 6 4.0 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
11705240 132279 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370120 132279 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44416871 80071 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 482 3 0 6 6.7 Cc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL214733 80071 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 482 3 0 6 6.7 Cc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44416296 79951 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 472 7 0 8 4.5 COc1cc(-n2cnc3cc(-c4ccc(C#N)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL214429 79951 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 472 7 0 8 4.5 COc1cc(-n2cnc3cc(-c4ccc(C#N)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
16755970 91868 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 525 11 2 3 6.4 CCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
CHEMBL242901 91868 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 525 11 2 3 6.4 CCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
16756284 150942 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 521 9 2 3 6.3 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCCC2)CC1 10.1021/jm060381c
CHEMBL396234 150942 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 521 9 2 3 6.3 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCCC2)CC1 10.1021/jm060381c
44394572 66166 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 287 4 1 5 1.9 CC(CN1CCOCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL185236 66166 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 287 4 1 5 1.9 CC(CN1CCOCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44405415 72209 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 394 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2C 10.1016/j.bmcl.2005.08.049
CHEMBL199222 72209 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 394 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2C 10.1016/j.bmcl.2005.08.049
11975326 80082 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 406 4 1 6 2.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccccc2o1 10.1021/jm060683e
CHEMBL214767 80082 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 406 4 1 6 2.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccccc2o1 10.1021/jm060683e
58062298 125345 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 437 10 1 5 3.8 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CNC[C@@H]4CCCO4)cc3C2)nc1 nan
CHEMBL3648389 125345 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 437 10 1 5 3.8 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc(CNC[C@@H]4CCCO4)cc3C2)nc1 nan
44410944 76684 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 456 4 1 5 5.3 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207257 76684 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 456 4 1 5 5.3 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44394855 66929 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 490 12 3 5 5.6 CCOc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCN(CC)CC 10.1016/j.bmcl.2004.07.077
CHEMBL188179 66929 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 490 12 3 5 5.6 CCOc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCN(CC)CC 10.1016/j.bmcl.2004.07.077
135515070 20913 1 None -3 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 353 3 2 5 4.2 CCc1ccc(C2CC(c3ccccc3Cl)Nc3nc(N)nn32)cc1 nan
CHEMBL1312413 20913 1 None -3 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 353 3 2 5 4.2 CCc1ccc(C2CC(c3ccccc3Cl)Nc3nc(N)nn32)cc1 nan
11464405 80070 18 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1021/jm060683e
CHEMBL214731 80070 18 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1021/jm060683e
70687537 73189 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 526 6 2 6 5.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017592 73189 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 526 6 2 6 5.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
58062333 125335 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 406 9 1 3 4.6 CC[C@H](C)NCc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
CHEMBL3648379 125335 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 406 9 1 3 4.6 CC[C@H](C)NCc1ccc2c(c1)C[C@H](N(C)C(=O)c1ccc(OCC3CC3)cc1)C2 nan
44438748 148953 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 527 10 1 7 4.5 CC(C)CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL394639 148953 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 527 10 1 7 4.5 CC(C)CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
11842385 37882 3 None -2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 292 5 1 3 4.7 Cc1ccc(NC(Cc2cc(C)no2)c2ccccc2)cc1 nan
CHEMBL1461182 37882 3 None -2 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 292 5 1 3 4.7 Cc1ccc(NC(Cc2cc(C)no2)c2ccccc2)cc1 nan
44416232 79674 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 448 7 0 8 4.0 COc1cc(-n2cnc3cc(-c4ccncc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL213154 79674 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 448 7 0 8 4.0 COc1cc(-n2cnc3cc(-c4ccncc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
11995025 168264 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 491 4 0 6 7.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCCCC3)cc2c1 10.1021/jm060814b
CHEMBL437914 168264 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 491 4 0 6 7.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCCCC3)cc2c1 10.1021/jm060814b
11993892 141073 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 469 4 0 7 5.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(Cn3ccnc3)ccc2c1 10.1021/jm060572f
CHEMBL385171 141073 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 469 4 0 7 5.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(Cn3ccnc3)ccc2c1 10.1021/jm060572f
9821717 196851 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 389 5 2 5 3.3 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL578049 196851 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 389 5 2 5 3.3 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
57522703 76008 0 None 1 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059410 76008 0 None 1 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
16006978 79648 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells assessed by inhibition of MCH-stimulated G protein-GTP-gamma-[35S] bindingAntagonist activity against human MCHR1 expressed in CHO cells assessed by inhibition of MCH-stimulated G protein-GTP-gamma-[35S] binding
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213052 79648 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells assessed by inhibition of MCH-stimulated G protein-GTP-gamma-[35S] bindingAntagonist activity against human MCHR1 expressed in CHO cells assessed by inhibition of MCH-stimulated G protein-GTP-gamma-[35S] binding
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
11995347 80480 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 478 4 1 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CCCC1)O2 10.1021/jm060572f
CHEMBL215286 80480 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 478 4 1 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CCCC1)O2 10.1021/jm060572f
23027806 195521 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 5 2 5 3.6 Cc1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc(N(C)C)c1C 10.1016/j.bmcl.2009.09.003
CHEMBL568208 195521 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 5 2 5 3.6 Cc1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)nc(N(C)C)c1C 10.1016/j.bmcl.2009.09.003
18436094 74521 0 None 53 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031727 74521 0 None 53 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11994660 96092 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 493 4 1 7 5.5 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CC[C@@H](O)C3)cc2c1 10.1021/jm060814b
CHEMBL262945 96092 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 493 4 1 7 5.5 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CC[C@@H](O)C3)cc2c1 10.1021/jm060814b
23027679 196859 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 389 5 2 5 3.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL578166 196859 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 389 5 2 5 3.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
44417021 80067 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 421 3 1 6 4.7 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL214716 80067 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 421 3 1 6 4.7 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44416337 79948 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 515 7 0 7 5.6 COc1cc(-n2cnc3cc(-c4ccc(C(F)(F)F)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL214416 79948 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 515 7 0 7 5.6 COc1cc(-n2cnc3cc(-c4ccc(C(F)(F)F)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
18436038 76006 0 None -1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059408 76006 0 None -1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
11994911 141444 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 447 4 0 5 5.7 CN(C)CC1=Cc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2CC1 10.1021/jm060814b
CHEMBL387419 141444 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 447 4 0 5 5.7 CN(C)CC1=Cc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc2CC1 10.1021/jm060814b
9932896 74163 0 None 1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2029372 74163 0 None 1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
57398088 67725 0 None 2 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914631 67725 0 None 2 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
9932896 74163 0 None 1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2029372 74163 0 None 1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
45485062 195482 0 None 10 5 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
CHEMBL567993 195482 0 None 10 5 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3ncc(C)c(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
57521365 2567 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
8587 2567 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
CHEMBL2059420 2567 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
44414309 138347 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 489 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Br)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL378230 138347 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 489 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Br)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44414497 178555 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL472083 178555 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL534717 178555 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44414497 178555 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm8016199
CHEMBL472083 178555 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm8016199
CHEMBL534717 178555 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm8016199
23120512 193628 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551470 193628 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
24963343 72787 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 362 5 1 6 2.3 N[C@@H]1CCN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C1 10.1016/j.bmcl.2012.02.010
CHEMBL2011537 72787 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 362 5 1 6 2.3 N[C@@H]1CCN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C1 10.1016/j.bmcl.2012.02.010
16739324 149215 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 471 3 0 6 3.8 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL394823 149215 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 471 3 0 6 3.8 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
71226400 128648 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3670640 128648 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
71227163 138525 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCCO4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3786346 138525 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCCO4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
127031338 138529 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccc(Cl)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3786375 138529 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccc(Cl)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
71226277 138576 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCOC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786841 138576 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCOC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
57403784 68498 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922262 68498 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
23532181 68500 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CCN3CCOCC3)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922266 68500 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 421 3 1 3 4.1 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(CCN3CCOCC3)CC21 10.1016/j.bmcl.2011.09.110
70681214 73244 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 489 5 1 5 4.8 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017746 73244 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 489 5 1 5 4.8 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44469273 195871 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 394 10 1 4 4.3 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL570296 195871 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 394 10 1 4 4.3 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
10436090 65859 0 None 776 2 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL184438 65859 0 None 776 2 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
44394609 123354 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 545 10 2 5 7.6 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)c1cccc(Cl)c1 10.1016/j.bmcl.2004.07.034
CHEMBL362768 123354 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 545 10 2 5 7.6 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)c1cccc(Cl)c1 10.1016/j.bmcl.2004.07.034
44394792 124207 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 405 7 2 5 3.9 Nc1ccc2cccc(OCCCNC(=O)c3cccc(OC(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL364210 124207 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 405 7 2 5 3.9 Nc1ccc2cccc(OCCCNC(=O)c3cccc(OC(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
16659240 81788 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 474 9 6 3 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217079 81788 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 474 9 6 3 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
22348155 76217 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
CHEMBL206314 76217 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
22348261 76695 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 421 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)cc(=O)n2C 10.1016/j.bmcl.2006.02.044
CHEMBL207300 76695 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 421 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)cc(=O)n2C 10.1016/j.bmcl.2006.02.044
22348066 165266 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 436 4 2 7 4.3 N#Cc1c(O)nc2ccc(Cl)cc2c1NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2006.02.044
CHEMBL424865 165266 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 436 4 2 7 4.3 N#Cc1c(O)nc2ccc(Cl)cc2c1NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2006.02.044
11995141 80727 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 510 6 0 7 6.0 CCC(C)c1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
CHEMBL215782 80727 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 510 6 0 7 6.0 CCC(C)c1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
45485004 196753 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 489 6 3 5 5.3 CNc1nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)ncc1C 10.1016/j.bmcl.2009.09.003
CHEMBL577259 196753 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 489 6 3 5 5.3 CNc1nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)ncc1C 10.1016/j.bmcl.2009.09.003
127033096 138636 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 409 7 0 8 2.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cn4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787492 138636 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 409 7 0 8 2.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cn4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
57393331 68490 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.4 CC1c2c([nH]c3cc(C(F)(F)F)ccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922254 68490 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.4 CC1c2c([nH]c3cc(C(F)(F)F)ccc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
57391572 68491 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 268 0 1 1 3.7 Cc1ccc2[nH]c3c(c2c1)C(C)C1CN(C)CCC1C3 10.1016/j.bmcl.2011.09.110
CHEMBL1922255 68491 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 268 0 1 1 3.7 Cc1ccc2[nH]c3c(c2c1)C(C)C1CN(C)CCC1C3 10.1016/j.bmcl.2011.09.110
16756637 92757 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)cc4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244578 92757 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)cc4)c3)CC2)c1 10.1021/jm060383x
46835808 59101 0 None -6 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 5 0 5 5.1 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)c(C)c3)c2=O)cc1 nan
CHEMBL1710711 59101 0 None -6 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 5 0 5 5.1 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)c(C)c3)c2=O)cc1 nan
30979231 69168 3 None -19 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at MCHR1 by FLIPR assayAntagonist activity at MCHR1 by FLIPR assay
ChEMBL 392 3 0 2 6.4 CCn1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
CHEMBL1934102 69168 3 None -19 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at MCHR1 by FLIPR assayAntagonist activity at MCHR1 by FLIPR assay
ChEMBL 392 3 0 2 6.4 CCn1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21 10.1016/j.bmcl.2011.10.125
46846334 59189 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 5 0 5 5.0 COc1ccc(Oc2c(-c3ccccc3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1715364 59189 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 5 0 5 5.0 COc1ccc(Oc2c(-c3ccccc3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
3527724 50201 3 None -1 3 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 475 10 3 6 3.7 COC(=O)CNC(c1ccccc1)c1cc(C)ccc1NC(=O)CNC(=O)OCc1ccccc1 nan
CHEMBL1573548 50201 3 None -1 3 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 475 10 3 6 3.7 COC(=O)CNC(c1ccccc1)c1cc(C)ccc1NC(=O)CNC(=O)OCc1ccccc1 nan
54584904 60286 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 448 8 1 3 5.0 COc1ccc([C@H]2CN(CCc3ccccc3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760225 60286 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 448 8 1 3 5.0 COc1ccc([C@H]2CN(CCc3ccccc3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
11546687 81129 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)ccc2o1 10.1021/jm060683e
CHEMBL216133 81129 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)ccc2o1 10.1021/jm060683e
5129939 36091 9 None -5 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 537 4 0 4 2.1 O=C(CN1C(=O)C2C3CC(C(Br)C3Br)C2C1=O)N1CCN(Cc2ccccc2)CC1 nan
CHEMBL1446321 36091 9 None -5 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 537 4 0 4 2.1 O=C(CN1C(=O)C2C3CC(C(Br)C3Br)C2C1=O)N1CCN(Cc2ccccc2)CC1 nan
58062355 125337 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 462 7 1 4 4.8 CC1(C)CCN(Cc2ccc3c(c2)C[C@H](NC(=O)c2ccc(OC[C@@H]4CCCO4)cc2)C3)CC1 nan
CHEMBL3648381 125337 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 462 7 1 4 4.8 CC1(C)CCN(Cc2ccc3c(c2)C[C@H](NC(=O)c2ccc(OC[C@@H]4CCCO4)cc2)C3)CC1 nan
10024171 187452 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 404 6 2 3 5.0 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497646 187452 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 404 6 2 3 5.0 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
56597689 138623 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 392 6 0 6 3.0 Cc1cc(CN(C)C)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3787333 138623 0 None -2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 392 6 0 6 3.0 Cc1cc(CN(C)C)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 10.1021/acs.jmedchem.5b01654
11599973 193218 0 None 407 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 600 8 2 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.067
CHEMBL540930 193218 0 None 407 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 600 8 2 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.067
70681216 73251 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 554 6 1 6 4.8 Cc1nc(N2CCC(N3CCN(C)C3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017753 73251 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 554 6 1 6 4.8 Cc1nc(N2CCC(N3CCN(C)C3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
45484984 195573 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568458 195573 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
10083869 65228 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL183159 65228 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
46835819 58977 0 None -3 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 382 4 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3ccc4c(c3)CCCC4)c2=O)cc1 nan
CHEMBL1705448 58977 0 None -3 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 382 4 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3ccc4c(c3)CCCC4)c2=O)cc1 nan
10083869 65228 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65228 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11545677 70019 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 394 5 1 4 5.0 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194523 70019 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 394 5 1 4 5.0 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44417974 96582 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 485 9 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc2ccccc2c1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL266972 96582 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 485 9 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc2ccccc2c1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11974233 81716 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccccc2F)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL216777 81716 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccccc2F)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
1082177 25661 5 None 1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 379 8 1 6 4.1 CCn1c(CNc2ccc(Cl)cc2)nnc1SCCN1CCCCC1 nan
CHEMBL1353612 25661 5 None 1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 379 8 1 6 4.1 CCn1c(CNc2ccc(Cl)cc2)nnc1SCCN1CCCCC1 nan
90666098 108830 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 562 7 1 5 7.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(Cl)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219001 108830 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 562 7 1 5 7.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(Cl)cc4)cc3)CC2)c1 10.1039/C1MD00015B
45273659 194149 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL558326 194149 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
44394604 124517 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 299 5 2 4 3.5 CC(CNC1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL364399 124517 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 299 5 2 4 3.5 CC(CNC1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
1933024 26100 10 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 425 5 5 5 1.6 N=C(N)NS(=O)(=O)c1ccc(NC(=S)NC(=O)Cc2ccc(Cl)cc2)cc1 nan
CHEMBL1358809 26100 10 None -1 2 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 425 5 5 5 1.6 N=C(N)NS(=O)(=O)c1ccc(NC(=S)NC(=O)Cc2ccc(Cl)cc2)cc1 nan
44143495 183663 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 430 6 2 3 5.5 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL483674 183663 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 430 6 2 3 5.5 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCC1 10.1016/j.bmcl.2009.04.147
127030069 138565 0 None -3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 434 6 1 7 2.6 CC1(O)CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3786685 138565 0 None -3 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 434 6 1 7 2.6 CC1(O)CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
56597988 138610 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 426 7 0 7 2.8 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787170 138610 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 426 7 0 7 2.8 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
53317306 56396 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2cccc(F)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642472 56396 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2cccc(F)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
53325164 56408 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 420 10 0 5 4.9 CC(C)N(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)C(C)C 10.1016/j.bmc.2010.12.002
CHEMBL1642486 56408 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 420 10 0 5 4.9 CC(C)N(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)C(C)C 10.1016/j.bmc.2010.12.002
57392823 67724 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 410 6 1 3 4.9 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914630 67724 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 410 6 1 3 4.9 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
10000146 64301 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL181813 64301 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
127033673 138556 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 463 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)nc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786609 138556 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 463 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)nc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
23593472 64359 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818786 64359 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
70695915 73205 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 480 7 2 6 4.6 COCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017608 73205 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 480 7 2 6 4.6 COCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
44394611 123815 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
44394611 123815 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL363664 123815 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363664 123815 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.035
54584906 60298 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 494 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNCc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760239 60298 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 494 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNCc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
46172941 59235 0 None -3 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 6 0 5 5.2 CCC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
CHEMBL1717450 59235 0 None -3 2 Human 5.7 pIC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 6 0 5 5.2 CCC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
675719 41587 16 None - 1 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 304 7 1 4 3.0 O=C(COc1ccc([N+](=O)[O-])cc1)NCCC1=CCCCC1 nan
CHEMBL1493564 41587 16 None - 1 Human 4.7 pIC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 304 7 1 4 3.0 O=C(COc1ccc([N+](=O)[O-])cc1)NCCC1=CCCCC1 nan
58062312 125338 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 436 8 2 4 4.3 CC(C)(C)CNCc1ccc2c(c1)C[C@H](NC(=O)c1ccc(OC[C@@H]3CCCO3)cc1)C2 nan
CHEMBL3648382 125338 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 436 8 2 4 4.3 CC(C)(C)CNCc1ccc2c(c1)C[C@H](NC(=O)c1ccc(OC[C@@H]3CCCO3)cc1)C2 nan
44394799 65907 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 347 5 1 4 4.4 CCC(c1ccccc1)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
CHEMBL184609 65907 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 347 5 1 4 4.4 CCC(c1ccccc1)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
70695913 73187 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 436 4 2 5 4.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017590 73187 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 436 4 2 5 4.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
2849164 55546 27 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 4 0 5 2.3 O=[N+]([O-])c1ccc(N2CCN(Cc3ccccc3)CC2)nc1 nan
CHEMBL1518183 55546 27 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 4 0 5 2.3 O=[N+]([O-])c1ccc(N2CCN(Cc3ccccc3)CC2)nc1 nan
CHEMBL1623233 55546 27 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 298 4 0 5 2.3 O=[N+]([O-])c1ccc(N2CCN(Cc3ccccc3)CC2)nc1 nan
58062371 125340 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 474 7 0 4 4.9 CN(C(=O)c1ccc(OC[C@@H]2CCCO2)cc1)[C@@H]1Cc2ccc(CN3CC4CCC3CC4)cc2C1 nan
CHEMBL3648384 125340 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 474 7 0 4 4.9 CN(C(=O)c1ccc(OC[C@@H]2CCCO2)cc1)[C@@H]1Cc2ccc(CN3CC4CCC3CC4)cc2C1 nan
22254582 66623 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 242 3 1 3 3.4 Nc1ccc2cccc(OCC3CCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186770 66623 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 242 3 1 3 3.4 Nc1ccc2cccc(OCC3CCCC3)c2n1 10.1016/j.bmcl.2004.07.032
2963624 36254 5 None -5 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 392 7 0 7 4.7 N#Cc1ccc(CSc2nnc(Cc3cccs3)n2Cc2ccco2)cc1 nan
CHEMBL1447678 36254 5 None -5 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 392 7 0 7 4.7 N#Cc1ccc(CSc2nnc(Cc3cccs3)n2Cc2ccco2)cc1 nan
44430455 86410 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 499 4 0 6 4.6 CC(C)N1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232257 86410 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 499 4 0 6 4.6 CC(C)N1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44430475 86628 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232619 86628 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
49801837 138468 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 7 2.5 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(COC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3785663 138468 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 7 2.5 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(COC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
56597851 138518 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 422 7 0 7 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(C)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786272 138518 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 422 7 0 7 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(C)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
127030070 138618 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 464 7 1 8 2.6 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC(C)(O)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787261 138618 0 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 464 7 1 8 2.6 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC(C)(O)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
89691439 137707 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770359 137707 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
53320117 56413 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 390 7 0 5 3.9 CN1CCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642491 56413 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 390 7 0 5 3.9 CN1CCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
11654412 197230 22 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL584538 197230 22 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
70695918 73213 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 499 9 3 6 4.4 Cc1nc(NCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017616 73213 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 499 9 3 6 4.4 Cc1nc(NCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
25017033 19075 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium releaseAntagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium release
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccc(Cl)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290383 19075 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium releaseAntagonistic activity at MCH-1 receptor expressed in CHO-K1 cell assessed as inhibition of MCH-induced calcium release
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccc(Cl)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
45485018 196924 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 437 6 2 6 3.9 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(OC(F)(F)F)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL578784 196924 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 437 6 2 6 3.9 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(OC(F)(F)F)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
70691723 73204 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 466 6 3 6 4.0 Cc1nc(N2CCC(O)(CCO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017607 73204 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 466 6 3 6 4.0 Cc1nc(N2CCC(O)(CCO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
16756754 91683 21 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 478 7 1 3 7.0 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1 10.1021/jm060383x
CHEMBL242004 91683 21 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 478 7 1 3 7.0 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1 10.1021/jm060383x
54583912 60257 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 468 9 1 5 4.6 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccoc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760085 60257 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 468 9 1 5 4.6 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccoc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
44442063 93946 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 337 5 2 4 4.8 c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250927 93946 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 337 5 2 4 4.8 c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
24818378 29423 5 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 513 9 2 6 3.4 COc1ccc(NS(=O)(=O)c2cccc(C(=O)NCC(c3ccc(F)cc3)N3CCOCC3)c2)cc1 nan
CHEMBL1386141 29423 5 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 513 9 2 6 3.4 COc1ccc(NS(=O)(=O)c2cccc(C(=O)NCC(c3ccc(F)cc3)N3CCOCC3)c2)cc1 nan
1479652 51437 13 None -7 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1584538 51437 13 None -7 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
653550 36895 5 None -15 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 481 6 1 6 2.0 O=C(c1ccco1)N1CCN(S(=O)(=O)c2ccc(S(=O)(=O)NC3CCCCC3)cc2)CC1 nan
CHEMBL1452812 36895 5 None -15 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 481 6 1 6 2.0 O=C(c1ccco1)N1CCN(S(=O)(=O)c2ccc(S(=O)(=O)NC3CCCCC3)cc2)CC1 nan
646509 24588 6 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 385 4 1 6 3.3 OC1(c2ccc(F)cc2)CC2CCC(C1)N2Cc1nnnn1C1CCCCC1 nan
CHEMBL1344766 24588 6 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 385 4 1 6 3.3 OC1(c2ccc(F)cc2)CC2CCC(C1)N2Cc1nnnn1C1CCCCC1 nan
44414391 79772 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 427 5 0 6 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213641 79772 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 427 5 0 6 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44414540 79901 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 459 4 0 5 5.6 Cc1cc(Cl)ccc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
CHEMBL214221 79901 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 459 4 0 5 5.6 Cc1cc(Cl)ccc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
11994138 141103 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)OC[C@H](CN1CCCC1)O2 10.1021/jm060572f
CHEMBL385347 141103 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)OC[C@H](CN1CCCC1)O2 10.1021/jm060572f
54585863 60304 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 456 8 1 4 5.2 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760246 60304 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 456 8 1 4 5.2 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
89702226 138770 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assay
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792516 138770 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as change in MCH(4 to 19)-stimulated Ca2+ concentration by Ca2+ mobilization assay
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11596311 56407 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 392 10 0 5 4.1 CCN(CC)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642485 56407 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 392 10 0 5 4.1 CCN(CC)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
70691722 73203 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 478 6 2 6 4.6 CC(=O)CC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017606 73203 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 478 6 2 6 4.6 CC(=O)CC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
9806086 64861 0 None 91 2 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL182554 64861 0 None 91 2 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
16756403 150398 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 378 7 1 3 4.8 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm060383x
CHEMBL395789 150398 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 378 7 1 3 4.8 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm060383x
46188603 121237 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 408 4 1 6 2.9 CN[C@H]1CCN(c2ccc(N3Cc4cn(-c5ccc(Cl)cc5)nc4C3=O)cn2)C1 10.1016/j.bmcl.2015.05.008
CHEMBL3589145 121237 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 408 4 1 6 2.9 CN[C@H]1CCN(c2ccc(N3Cc4cn(-c5ccc(Cl)cc5)nc4C3=O)cn2)C1 10.1016/j.bmcl.2015.05.008
44417977 81870 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 10 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)Cc1cccc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217193 81870 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 10 5 3 3.5 N=C(N)NCCC[C@@H](NC(=O)Cc1cccc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
3825639 29600 13 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 302 3 0 4 5.0 Cc1ccccc1Oc1ncnc2oc(-c3ccccc3)cc12 nan
CHEMBL1387472 29600 13 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 302 3 0 4 5.0 Cc1ccccc1Oc1ncnc2oc(-c3ccccc3)cc12 nan
44394864 125664 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 377 4 1 6 3.7 CNc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364983 125664 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 377 4 1 6 3.7 CNc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
2948210 38164 7 None -7 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 340 3 1 5 4.1 COc1ccccc1C1CC(c2ccc(Cl)cc2)Nc2ncnn21 nan
CHEMBL1463698 38164 7 None -7 3 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 340 3 1 5 4.1 COc1ccccc1C1CC(c2ccc(Cl)cc2)Nc2ncnn21 nan
2424660 40144 6 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 456 8 2 4 3.8 COC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCC(=O)c1ccc(Br)cc1 nan
CHEMBL1482022 40144 6 None 1 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 456 8 2 4 3.8 COC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCC(=O)c1ccc(Br)cc1 nan
70695851 73090 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 481 6 1 6 4.8 Cc1nc(N2CCN(CC(C)(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016700 73090 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 481 6 1 6 4.8 Cc1nc(N2CCN(CC(C)(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
45487653 197319 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCH1R receptor expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPRAntagonist activity against human MCH1R receptor expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585664 197319 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCH1R receptor expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPRAntagonist activity against human MCH1R receptor expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
11994137 82138 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)C[C@H]1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL217844 82138 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)C[C@H]1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
23027830 195606 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 371 5 2 5 3.1 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568664 195606 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 371 5 2 5 3.1 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)n1 10.1016/j.bmcl.2009.09.003
54579974 3177 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
7756 3177 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
CHEMBL1760248 3177 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
127030071 138634 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 506 7 1 8 3.6 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CC(O)C(C)(C)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787462 138634 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 506 7 1 8 3.6 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CC(O)C(C)(C)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
70691652 73110 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016721 73110 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442065 93862 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250540 93862 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
11628328 193856 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 566 8 2 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL554332 193856 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 566 8 2 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
16755871 92049 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 497 10 2 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243138 92049 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 497 10 2 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44417941 96129 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 492 9 6 3 3.0 N=C(N)NCCC[C@@H](NC(=O)c1cc2cc(F)ccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL263171 96129 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 492 9 6 3 3.0 N=C(N)NCCC[C@@H](NC(=O)c1cc2cc(F)ccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11511219 65789 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL184084 65789 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44416828 141199 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 0 7 5.3 Cn1c(N2CCCC2)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
CHEMBL385883 141199 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 0 7 5.3 Cn1c(N2CCCC2)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
44416949 141249 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 392 2 1 5 5.0 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL386188 141249 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 392 2 1 5 5.0 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44416272 79599 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 453 7 0 8 4.7 COc1cc(-n2cnc3cc(-c4ccsc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212883 79599 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 453 7 0 8 4.7 COc1cc(-n2cnc3cc(-c4ccsc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44416212 80495 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 573 7 0 7 5.2 COc1cc(-n2cnc3cc(-c4cccc(I)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL215334 80495 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 573 7 0 7 5.2 COc1cc(-n2cnc3cc(-c4cccc(I)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
54583953 60285 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 536 12 1 5 5.8 COc1ccc([C@H]2CN(CCCCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760224 60285 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 536 12 1 5 5.8 COc1ccc([C@H]2CN(CCCCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
9824428 65910 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 438 9 3 4 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184634 65910 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 438 9 3 4 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
44416975 141286 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 541 6 0 8 6.2 COc1ccc(Cn2c(N(C)C)nc3ccc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL386397 141286 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 541 6 0 8 6.2 COc1ccc(Cn2c(N(C)C)nc3ccc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cc32)cc1 10.1016/j.bmcl.2006.07.054
44405560 72088 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 495 5 1 9 4.6 O=C(c1cscn1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL198835 72088 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 495 5 1 9 4.6 O=C(c1cscn1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
16192403 38325 2 None -2 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 430 4 1 3 4.5 Cc1ccccc1CN1C[C@@H]2C[C@@H](c3c[nH]nc3-c3ccc(F)cc3)N3CCC[C@@]23C1=O nan
CHEMBL1464847 38325 2 None -2 2 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 430 4 1 3 4.5 Cc1ccccc1CN1C[C@@H]2C[C@@H](c3c[nH]nc3-c3ccc(F)cc3)N3CCC[C@@]23C1=O nan
70685397 73202 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 450 5 2 5 5.0 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017605 73202 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 450 5 2 5 5.0 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
70695917 73210 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 488 9 2 6 5.1 Cc1nc(N(CCCO)C(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017613 73210 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 488 9 2 6 5.1 Cc1nc(N(CCCO)C(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
46892401 125349 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 392 7 1 3 4.5 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc([C@H]4CCCN4)cc3C2)cc1 nan
CHEMBL3648393 125349 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 392 7 1 3 4.5 CCCCOc1ccc(C(=O)N(C)[C@@H]2Cc3ccc([C@H]4CCCN4)cc3C2)cc1 nan
90666257 108866 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 560 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(C(C)c3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219266 108866 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 560 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(C(C)c3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
45485002 196834 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cccc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL577913 196834 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cccc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
11222404 193698 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 368 4 1 4 4.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccccn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551934 193698 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 368 4 1 4 4.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccccn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
127031356 138648 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 7 1 8 3.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCC(O)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787642 138648 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 7 1 8 3.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCC(O)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
70685398 73214 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 10 3 6 4.8 Cc1nc(NCCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017617 73214 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 10 3 6 4.8 Cc1nc(NCCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70687550 73252 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 576 6 2 7 3.6 Cc1nc(N2CCC(N3CCNS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017754 73252 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 576 6 2 7 3.6 Cc1nc(N2CCC(N3CCNS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
16756185 149177 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL394793 149177 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
20817761 76900 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 411 4 2 6 4.4 Oc1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1 10.1016/j.bmcl.2006.02.044
CHEMBL208028 76900 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 411 4 2 6 4.4 Oc1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1 10.1016/j.bmcl.2006.02.044
90666252 108861 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 553 7 1 6 6.5 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C#N)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219261 108861 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 553 7 1 6 6.5 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C#N)cc4)cc3)CC2)c1 10.1039/C1MD00015B
10434776 125848 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL365055 125848 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
11653882 140761 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL383359 140761 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
54581980 60253 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 562 10 1 5 5.9 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(OC(F)(F)F)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760081 60253 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 562 10 1 5 5.9 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(OC(F)(F)F)cc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
16756639 92785 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)c(Cl)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244791 92785 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)c(Cl)c4)c3)CC2)c1 10.1021/jm060383x
46850889 59228 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 4.7 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C(F)(F)F)c3)c2=O)cc1 nan
CHEMBL1717204 59228 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 4.7 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C(F)(F)F)c3)c2=O)cc1 nan
54586826 60292 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 471 9 1 5 3.5 COc1ccc([C@H]2CN(CCCN3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760231 60292 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 471 9 1 5 3.5 COc1ccc([C@H]2CN(CCCN3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
2310853 55905 2 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 328 2 1 2 3.2 Cc1cc(C[n+]2cc(Br)ccc2N)c2ncccc2c1 nan
CHEMBL1335094 55905 2 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 328 2 1 2 3.2 Cc1cc(C[n+]2cc(Br)ccc2N)c2ncccc2c1 nan
CHEMBL1626478 55905 2 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 328 2 1 2 3.2 Cc1cc(C[n+]2cc(Br)ccc2N)c2ncccc2c1 nan
11510887 81843 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL217105 81843 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
52918017 60308 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 469 9 1 4 4.4 COc1ccc([C@H]2CN(CCCN3CCCC3=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760251 60308 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 469 9 1 4 4.4 COc1ccc([C@H]2CN(CCCN3CCCC3=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44143496 191479 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 444 6 2 3 5.9 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL520296 191479 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO-K1 cells assessed as inhibition of MCH-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 444 6 2 3 5.9 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
56597542 138409 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 480 8 0 9 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCOCC5)c(OC)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785102 138409 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 480 8 0 9 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCOCC5)c(OC)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
49801838 138627 22 None -2 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 462 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(COC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787394 138627 22 None -2 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 462 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(COC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11502008 56263 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 390 8 0 5 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1641614 56263 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 390 8 0 5 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
70689525 73144 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 530 7 2 7 5.0 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016781 73144 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 530 7 2 7 5.0 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70693808 73257 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 479 6 3 6 3.3 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017759 73257 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 479 6 3 6 3.3 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
16756073 91842 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 10 2 3 6.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242689 91842 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 10 2 3 6.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
10324628 141681 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 527 10 3 4 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL388440 141681 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 527 10 3 4 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
16756072 166798 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 547 10 2 3 6.4 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL429464 166798 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 547 10 2 3 6.4 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm060381c
45487384 195156 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)nc1 10.1016/j.bmcl.2009.07.023
CHEMBL565833 195156 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)nc1 10.1016/j.bmcl.2009.07.023
44438755 93057 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 550 9 2 7 3.2 COc1cc(C(=O)NCCN2CCCC2)ccc1CN1CCC(NC(=O)c2cc(=O)c3ccc(F)cc3o2)CC1 10.1016/j.bmcl.2006.11.068
CHEMBL246259 93057 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 550 9 2 7 3.2 COc1cc(C(=O)NCCN2CCCC2)ccc1CN1CCC(NC(=O)c2cc(=O)c3ccc(F)cc3o2)CC1 10.1016/j.bmcl.2006.11.068
44394591 122130 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 6 2 6 3.4 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL360393 122130 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 6 2 6 3.4 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
16756401 150397 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 364 7 1 3 4.5 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccccc3)CC2)c1 10.1021/jm060383x
CHEMBL395788 150397 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 364 7 1 3 4.5 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccccc3)CC2)c1 10.1021/jm060383x
46172921 59017 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 4 0 5 5.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)(C)C)cc3)c2=O)cc1 nan
CHEMBL1706988 59017 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 384 4 0 5 5.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)(C)C)cc3)c2=O)cc1 nan
2649486 29728 7 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 437 8 1 10 2.8 COc1ccccc1NC(=O)Cc1noc(CSc2nnnn2-c2cccc(C)c2)n1 nan
CHEMBL1388448 29728 7 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 437 8 1 10 2.8 COc1ccccc1NC(=O)Cc1noc(CSc2nnnn2-c2cccc(C)c2)n1 nan
11974227 168728 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)cc(F)c2o1 10.1021/jm060683e
CHEMBL441542 168728 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)cc(F)c2o1 10.1021/jm060683e
2491454 46572 7 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 366 8 2 5 2.5 CCN(CC(=O)Nc1cccc(C#N)c1)CC(=O)Nc1cccc(OC)c1 nan
CHEMBL1540447 46572 7 None - 1 Human 4.6 pIC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 366 8 2 5 2.5 CCN(CC(=O)Nc1cccc(C#N)c1)CC(=O)Nc1cccc(OC)c1 nan
127031621 138552 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 462 7 0 7 4.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786572 138552 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 462 7 0 7 4.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
16665072 98073 0 None 56 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
CHEMBL276393 98073 0 None 56 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
10047339 70047 2 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 412 4 1 6 4.3 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194564 70047 2 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 412 4 1 6 4.3 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
10250850 72051 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4cc[nH]c4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL198727 72051 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4cc[nH]c4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44403765 135324 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL373084 135324 0 None -1 3 Human 7.6 pIC50 = 7.6 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
49865976 16026 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 470 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224230 16026 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 470 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11282448 62231 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2nn(CCN3CCCC3)cc12 10.1021/jm0490890
CHEMBL178259 62231 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2nn(CCN3CCCC3)cc12 10.1021/jm0490890
16193698 32839 3 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 400 7 1 4 3.5 COCCCNC(=O)/C=C1\Sc2ccccc2N(Cc2ccccc2F)C1=O nan
CHEMBL1416734 32839 3 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 400 7 1 4 3.5 COCCCNC(=O)/C=C1\Sc2ccccc2N(Cc2ccccc2F)C1=O nan
11994662 140970 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 568 5 0 7 7.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060814b
CHEMBL384553 140970 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 568 5 0 7 7.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060814b
11539096 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
1303 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
CHEMBL214021 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
11539096 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
1303 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
CHEMBL214021 181 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
23120575 194190 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL558826 194190 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
44430452 149214 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 457 3 1 6 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCNC1 10.1016/j.bmcl.2007.02.012
CHEMBL394822 149214 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 457 3 1 6 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCNC1 10.1016/j.bmcl.2007.02.012
56598130 138607 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 408 7 0 7 2.7 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787134 138607 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 408 7 0 7 2.7 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
21939915 64370 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818799 64370 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
9983233 75633 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 494 5 1 7 4.4 O=c1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL205492 75633 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 494 5 1 7 4.4 O=c1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
22348022 76983 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2006.02.044
CHEMBL208473 76983 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2006.02.044
44394569 65870 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 285 4 1 4 3.1 CC(CN1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184477 65870 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 285 4 1 4 3.1 CC(CN1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44405618 71656 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1cccnc1 10.1016/j.bmcl.2005.08.049
CHEMBL197497 71656 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1cccnc1 10.1016/j.bmcl.2005.08.049
46172934 58905 0 None -2 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 4.9 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(OC(F)(F)F)cc3)c2=O)cc1 nan
CHEMBL1702876 58905 0 None -2 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 396 4 0 5 4.9 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(OC(F)(F)F)cc3)c2=O)cc1 nan
46846323 59602 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 442 5 0 5 4.0 O=C(C1CCCCN1Cc1cccc(Cl)c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1731906 59602 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 442 5 0 5 4.0 O=C(C1CCCCN1Cc1cccc(Cl)c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
44438753 93014 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 570 8 2 6 3.8 O=C(NCCN1CCC(F)(F)CC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL246051 93014 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 570 8 2 6 3.8 O=C(NCCN1CCC(F)(F)CC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
58062362 125327 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 476 8 1 4 4.7 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCC(C(C)(C)O)CC3)cc2C1 nan
CHEMBL3648371 125327 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 476 8 1 4 4.7 CN(C(=O)c1ccc(OCC2CC2)cc1)[C@@H]1Cc2ccc(CN3CCC(C(C)(C)O)CC3)cc2C1 nan
70681115 73098 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 483 7 1 7 2.9 COCC(=O)N1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016709 73098 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 483 7 1 7 2.9 COCC(=O)N1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
1431538 28974 4 None -5 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 485 7 1 7 3.3 Cc1ccc(-n2c(SCC(N)=O)nnc2-c2ccc(S(=O)(=O)N3CCCCC3)cc2)c(C)c1 nan
CHEMBL1382150 28974 4 None -5 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 485 7 1 7 3.3 Cc1ccc(-n2c(SCC(N)=O)nnc2-c2ccc(S(=O)(=O)N3CCCCC3)cc2)c(C)c1 nan
3229425 51353 2 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 395 6 0 5 4.4 COc1ccccc1C(=O)N(CCC1CCCN1C)c1nc2ccccc2s1 nan
CHEMBL1583768 51353 2 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 395 6 0 5 4.4 COc1ccccc1C(=O)N(CCC1CCCN1C)c1nc2ccccc2s1 nan
90666095 108827 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 557 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
CHEMBL3218998 108827 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 557 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
90666096 108828 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 532 7 1 4 7.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3218999 108828 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 532 7 1 4 7.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
10258364 193106 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assayAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assay
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 193106 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assayAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assay
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 193106 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assayAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced calcium mobilization by FLIPR assay
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
70693733 73113 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 8 2 7 4.3 Cc1nc(N2CCC(C(=O)NC3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016724 73113 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 8 2 7 4.3 Cc1nc(N2CCC(C(=O)NC3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
46933538 16025 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 484 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224229 16025 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 484 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
10360874 64588 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL182261 64588 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
11994414 79891 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 489 4 0 5 6.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCCC1)C2 10.1021/jm060814b
CHEMBL214181 79891 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 489 4 0 5 6.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)CCC(CN1CCCCC1)C2 10.1021/jm060814b
11995342 80094 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 501 4 0 7 5.1 CN1CCN(Cc2ccc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3n2)CC1 10.1021/jm060572f
CHEMBL214808 80094 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 501 4 0 7 5.1 CN1CCN(Cc2ccc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3n2)CC1 10.1021/jm060572f
11995245 80160 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 580 5 0 6 7.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccc(F)cc4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL214991 80160 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 580 5 0 6 7.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccc(F)cc4)CC3)ccc2c1 10.1021/jm060572f
44416890 80064 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 512 5 0 7 6.8 CCOc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL214705 80064 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 512 5 0 7 6.8 CCOc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44417044 80812 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 447 3 1 6 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL215868 80812 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 447 3 1 6 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
44416377 80667 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 482 7 0 8 4.6 COc1cc(-n2cnc3nc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL215565 80667 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 482 7 0 8 4.6 COc1cc(-n2cnc3nc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
11995444 80038 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)C[C@@H]1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL214663 80038 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)C[C@@H]1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
11994017 80576 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 452 4 1 7 4.5 CN(C)CC1CNc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL215364 80576 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 452 4 1 7 4.5 CN(C)CC1CNc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
57522946 76018 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059421 76018 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
11994019 141113 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 2 8 4.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CC[C@@H](O)C1)O2 10.1021/jm060572f
CHEMBL385391 141113 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 2 8 4.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CC[C@@H](O)C1)O2 10.1021/jm060572f
57522947 76019 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059422 76019 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
11995442 81851 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 507 4 1 8 4.2 CN1CCN(CC2CNc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3O2)CC1 10.1021/jm060572f
CHEMBL217159 81851 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 507 4 1 8 4.2 CN1CCN(CC2CNc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3O2)CC1 10.1021/jm060572f
11995345 141004 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 419 3 1 6 4.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CO)ccc2c1 10.1021/jm060572f
CHEMBL384770 141004 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 419 3 1 6 4.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CO)ccc2c1 10.1021/jm060572f
11995344 80171 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 563 5 0 7 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(c4ccccc4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL215039 80171 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 563 5 0 7 6.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(c4ccccc4)CC3)ccc2c1 10.1021/jm060572f
18436119 76014 0 None 3 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059416 76014 0 None 3 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
44416875 79960 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 407 3 2 6 4.7 CNc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL214476 79960 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 407 3 2 6 4.7 CNc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44414357 79328 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 479 4 0 5 6.0 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5Cl)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL211736 79328 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 479 4 0 5 6.0 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5Cl)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
127030367 138521 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 9 0 8 3.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)CC5(C)COC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786311 138521 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 9 0 8 3.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)CC5(C)COC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
53317305 56395 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccccc2F)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642471 56395 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccccc2F)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
70693732 73100 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 529 7 1 7 3.9 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016711 73100 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 529 7 1 7 3.9 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70683287 73209 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 446 8 3 6 4.3 Cc1nc(NCCCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017612 73209 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 446 8 3 6 4.3 Cc1nc(NCCCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44394922 65795 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL184116 65795 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
44394726 65813 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 351 7 2 5 3.0 COc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL184243 65813 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 351 7 2 5 3.0 COc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
44394860 65901 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 285 5 2 4 3.1 CC(CNC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184590 65901 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 285 5 2 4 3.1 CC(CNC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
10361342 122396 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL360620 122396 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
10248906 123123 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 375 4 1 4 4.8 CC(C)(C)c1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL362009 123123 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 375 4 1 4 4.8 CC(C)(C)c1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
9828622 96193 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 536 9 1 5 5.3 O=C1c2cc(OCCC3CCN(Cc4ccc(C5=NCCN5)cc4)CC3)ccc2CCCN1Cc1ccccc1 10.1021/jm8016199
CHEMBL263702 96193 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCH1R by [35S]GTPgammaS binding assayAntagonist activity at MCH1R by [35S]GTPgammaS binding assay
ChEMBL 536 9 1 5 5.3 O=C1c2cc(OCCC3CCN(Cc4ccc(C5=NCCN5)cc4)CC3)ccc2CCCN1Cc1ccccc1 10.1021/jm8016199
45279489 123050 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618327 123050 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
49865975 16024 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 486 8 2 6 4.7 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224228 16024 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 486 8 2 6 4.7 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
135478067 23652 13 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 8 1 5 4.1 COc1ccnc(Oc2ccc(F)cc2)c1C(=O)N=CNOCc1ccc(F)cc1 nan
135485243 23652 13 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 8 1 5 4.1 COc1ccnc(Oc2ccc(F)cc2)c1C(=O)N=CNOCc1ccc(F)cc1 nan
154780186 23652 13 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 8 1 5 4.1 COc1ccnc(Oc2ccc(F)cc2)c1C(=O)N=CNOCc1ccc(F)cc1 nan
CHEMBL1336601 23652 13 None -1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 413 8 1 5 4.1 COc1ccnc(Oc2ccc(F)cc2)c1C(=O)N=CNOCc1ccc(F)cc1 nan
70687471 73106 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 410 5 1 5 4.6 Cc1nc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016717 73106 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 410 5 1 5 4.6 Cc1nc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
45273887 121236 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 452 7 0 6 4.2 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.05.008
CHEMBL3589138 121236 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
ChEMBL 452 7 0 6 4.2 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.05.008
11974030 154725 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(C(F)(F)F)cc2o1 10.1021/jm060683e
CHEMBL402868 154725 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(C(F)(F)F)cc2o1 10.1021/jm060683e
11995646 79855 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 484 5 0 8 4.5 COc1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
CHEMBL213966 79855 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 484 5 0 8 4.5 COc1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
54582957 60284 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760223 60284 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44430453 87480 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 575 7 0 6 5.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL233889 87480 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 575 7 0 6 5.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2007.02.012
70681113 73094 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016704 73094 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70687549 73248 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 541 6 1 7 4.9 Cc1nc(N2CCC(N3CCOC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017750 73248 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 541 6 1 7 4.9 Cc1nc(N2CCC(N3CCOC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70681215 73250 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 540 6 2 6 4.5 Cc1nc(N2CCC(N3CCNC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017752 73250 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 540 6 2 6 4.5 Cc1nc(N2CCC(N3CCNC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70693810 73263 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 578 8 2 7 3.9 Cc1nc(N2CCC(NS(=O)(=O)N(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017765 73263 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 578 8 2 7 3.9 Cc1nc(N2CCC(NS(=O)(=O)N(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
10075375 75634 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 520 5 1 7 4.9 O=c1nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL205493 75634 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 520 5 1 7 4.9 O=c1nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
11994275 81988 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 418 3 1 5 5.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2cc(CO)ccc2c1 10.1021/jm060814b
CHEMBL217356 81988 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 418 3 1 5 5.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2cc(CO)ccc2c1 10.1021/jm060814b
44417140 79829 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 451 6 2 7 4.7 COCCNc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL213864 79829 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 451 6 2 7 4.7 COCCNc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44416851 141298 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 468 3 0 6 6.4 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccccc1 10.1016/j.bmcl.2006.07.054
CHEMBL386460 141298 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 468 3 0 6 6.4 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccccc1 10.1016/j.bmcl.2006.07.054
44416858 165540 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 393 2 2 6 4.2 Nc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL425982 165540 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 393 2 2 6 4.2 Nc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
54581466 60234 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 470 9 1 4 5.0 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760003 60234 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 470 9 1 4 5.0 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
24997711 58893 2 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 284 2 0 4 2.9 COc1nn(-c2cccc(C)c2)c(=O)c(Cl)c1Cl nan
CHEMBL1702161 58893 2 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 284 2 0 4 2.9 COc1nn(-c2cccc(C)c2)c(=O)c(Cl)c1Cl nan
46835796 58921 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 383 5 0 5 4.9 CC(C)c1ccc(-n2ncc(Cl)c(Oc3cccc(N(C)C)c3)c2=O)cc1 nan
CHEMBL1703306 58921 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 383 5 0 5 4.9 CC(C)c1ccc(-n2ncc(Cl)c(Oc3cccc(N(C)C)c3)c2=O)cc1 nan
46846326 59041 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 458 5 0 5 4.5 O=C(C1CCCCN1Cc1ccc2ccccc2c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1708047 59041 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 458 5 0 5 4.5 O=C(C1CCCCN1Cc1ccc2ccccc2c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
46846335 59069 0 None -11 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1709509 59069 0 None -11 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
46172916 59311 0 None -4 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 428 6 0 5 5.3 CCOc1ccc(Oc2c(Br)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1720787 59311 0 None -4 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 428 6 0 5 5.3 CCOc1ccc(Oc2c(Br)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
44417986 165510 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 503 9 5 3 3.7 N=C(N)NCCC[C@@H](NC(=O)c1ccc(F)c2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL425801 165510 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 503 9 5 3 3.7 N=C(N)NCCC[C@@H](NC(=O)c1ccc(F)c2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
44394573 123152 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 570 10 3 7 7.1 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.07.034
CHEMBL362150 123152 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 570 10 3 7 7.1 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.07.034
54579972 60302 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 518 10 1 4 6.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2cc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760244 60302 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 518 10 1 4 6.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2cc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
44417968 81150 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 475 9 5 4 3.1 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2o1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL216241 81150 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 475 9 5 4 3.1 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2o1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
44416303 138125 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 504 8 1 8 4.6 COc1cc(-n2cnc3cc(-c4ccc(NC(C)=O)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL377758 138125 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 504 8 1 8 4.6 COc1cc(-n2cnc3cc(-c4ccc(NC(C)=O)cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
4881730 51605 6 None - 1 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 364 8 2 4 4.8 CCCCNc1nc2ccccc2n1CC(=O)Nc1c(C)cccc1CC nan
CHEMBL1585808 51605 6 None - 1 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 364 8 2 4 4.8 CCCCNc1nc2ccccc2n1CC(=O)Nc1c(C)cccc1CC nan
54580923 60254 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccccc3OC)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760082 60254 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccccc3OC)C2)cc1OC 10.1016/j.bmcl.2011.02.046
70695855 73114 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 503 7 2 7 3.6 Cc1nc(N2CCC(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016725 73114 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 503 7 2 7 3.6 Cc1nc(N2CCC(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11712898 178599 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472363 178599 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
70687538 73212 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 523 10 3 7 3.8 Cc1nc(NCCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017615 73212 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 523 10 3 7 3.8 Cc1nc(NCCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
16756641 142045 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL389128 142045 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
54585827 60255 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 484 9 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3cccs3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760083 60255 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 484 9 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3cccs3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
6463414 46907 8 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 384 3 0 3 3.5 O=C(c1ccc(Cl)c(S(=O)(=O)N2CCCCCC2)c1)N1CCCCC1 nan
CHEMBL1543278 46907 8 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 384 3 0 3 3.5 O=C(c1ccc(Cl)c(S(=O)(=O)N2CCCCCC2)c1)N1CCCCC1 nan
44414571 79850 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 455 4 0 7 4.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc6c(c5)OCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213949 79850 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 455 4 0 7 4.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc6c(c5)OCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
21062998 64369 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818798 64369 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
117798744 138930 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysis
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3794256 138930 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysis
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
70691650 73096 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016707 73096 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70693737 73143 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 516 7 2 7 4.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016780 73143 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 516 7 2 7 4.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
57391573 68493 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 362 3 3 4 2.1 CC1c2c([nH]c3ccc(NCS(N)(=O)=O)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922257 68493 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 362 3 3 4 2.1 CC1c2c([nH]c3ccc(NCS(N)(=O)=O)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
46846325 58874 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 460 5 0 5 4.1 O=C(C1CCCCN1Cc1c(F)cccc1Cl)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1701512 58874 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 460 5 0 5 4.1 O=C(C1CCCCN1Cc1c(F)cccc1Cl)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
46846316 59054 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 476 5 0 5 4.6 O=C(C1CCCCN1Cc1cccc(Cl)c1Cl)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1708651 59054 0 None 1 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 476 5 0 5 4.6 O=C(C1CCCCN1Cc1cccc(Cl)c1Cl)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
24794275 23549 5 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 391 6 2 3 3.3 CC(C)Cc1cc(C(=O)N2CCCC(CO)(Cc3ccc(F)cc3F)C2)[nH]n1 nan
CHEMBL1335692 23549 5 None 1 2 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 391 6 2 3 3.3 CC(C)Cc1cc(C(=O)N2CCCC(CO)(Cc3ccc(F)cc3F)C2)[nH]n1 nan
16191953 52017 6 None - 1 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 357 4 1 2 4.1 Cc1ccccc1CC1(CO)CCCN(C(=O)c2ccccc2Cl)C1 nan
CHEMBL1589399 52017 6 None - 1 Human 4.5 pIC50 = 4.5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 357 4 1 2 4.1 Cc1ccccc1CC1(CO)CCCN(C(=O)c2ccccc2Cl)C1 nan
90666259 108868 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 580 7 1 5 7.4 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3Cl)CC2)c1 10.1039/C1MD00015B
CHEMBL3219268 108868 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 580 7 1 5 7.4 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3Cl)CC2)c1 10.1039/C1MD00015B
56597407 138512 0 None -5 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 434 7 0 7 3.2 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786169 138512 0 None -5 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 434 7 0 7 3.2 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
123471111 138595 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 464 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCOCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787028 138595 0 None -3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 464 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCOCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
53318801 56392 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 406 8 0 6 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCOCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642468 56392 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 406 8 0 6 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCOCC2)cc1 10.1016/j.bmc.2010.12.002
21108114 67717 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 424 6 0 3 5.2 CN1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914623 67717 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 424 6 0 3 5.2 CN1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
70695930 73256 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 6 2 6 4.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(NS(C)(=O)=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017758 73256 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 6 2 6 4.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(NS(C)(=O)=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
70693809 73261 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 557 8 1 7 4.6 COCC(=O)N(C)C1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017763 73261 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 557 8 1 7 4.6 COCC(=O)N(C)C1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
10437982 92125 1 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 569 10 2 3 6.4 CC(C)C(=O)Nc1cc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(F)cc1F 10.1021/jm060381c
CHEMBL243355 92125 1 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 569 10 2 3 6.4 CC(C)C(=O)Nc1cc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(F)cc1F 10.1021/jm060381c
22348219 76156 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 457 6 1 7 3.9 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)F)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL206030 76156 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 457 6 1 7 3.9 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)F)ccc21 10.1016/j.bmcl.2006.02.044
21062991 64355 0 None 1 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818782 64355 0 None 1 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
70685395 73184 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 476 5 2 5 5.4 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017587 73184 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 476 5 2 5 5.4 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
44394644 65790 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 307 6 2 4 3.4 CC(CNCc1ccccc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184087 65790 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 307 6 2 4 3.4 CC(CNCc1ccccc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44405487 71516 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 375 4 2 6 3.2 N#Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197059 71516 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 375 4 2 6 3.2 N#Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
46850891 58854 0 None -8 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 358 5 0 6 3.7 COc1ccc(Oc2c(Cl)cnn(-c3cccc(OC)c3)c2=O)cc1 nan
CHEMBL1700476 58854 0 None -8 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 358 5 0 6 3.7 COc1ccc(Oc2c(Cl)cnn(-c3cccc(OC)c3)c2=O)cc1 nan
10480652 64975 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 488 9 3 5 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL182913 64975 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 488 9 3 5 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
10332650 65848 1 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 2 1 3 3.9 Nc1ccc2cccc(OC3CCCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184394 65848 1 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 256 2 1 3 3.9 Nc1ccc2cccc(OC3CCCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
44414392 79773 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 5 0 6 4.9 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213642 79773 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 445 5 0 6 4.9 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
127030368 138435 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 448 8 0 7 3.1 CN(Cc1ccc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)cc1)CC1(C)COC1 10.1021/acs.jmedchem.5b01654
CHEMBL3785343 138435 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 448 8 0 7 3.1 CN(Cc1ccc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)cc1)CC1(C)COC1 10.1021/acs.jmedchem.5b01654
44442144 154145 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 480 8 2 6 5.8 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OC(F)F)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL399721 154145 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 480 8 2 6 5.8 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OC(F)F)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
70691725 73215 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 10 3 6 5.0 Cc1nc(NCCCC(=O)NC2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017618 73215 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 513 10 3 6 5.0 Cc1nc(NCCCC(=O)NC2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70683300 73247 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 7 4.6 Cc1nc(N2CCC(N3C(=O)CCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017749 73247 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 7 4.6 Cc1nc(N2CCC(N3C(=O)CCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44414542 79910 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 469 5 0 7 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc6c(c5)CCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL214252 79910 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 469 5 0 7 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc6c(c5)CCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
54582015 60290 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 456 8 1 4 4.6 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760229 60290 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 456 8 1 4 4.6 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
70683237 73091 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 451 6 1 6 3.9 Cc1nc(N2CCN(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016701 73091 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 451 6 1 6 3.9 Cc1nc(N2CCN(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70681117 73103 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 507 6 1 6 4.4 Cc1nc(N2CCN(C(=O)C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016714 73103 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 507 6 1 6 4.4 Cc1nc(N2CCN(C(=O)C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
16756642 92834 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)cc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL245010 92834 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)cc4)cc3)CC2)c1 10.1021/jm060383x
44405464 165787 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 485 7 1 8 4.8 O=[N+]([O-])c1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL427367 165787 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 485 7 1 8 4.8 O=[N+]([O-])c1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
46846321 59411 0 None -2 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 412 6 0 6 4.9 CC(=O)OCc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1724571 59411 0 None -2 2 Human 5.5 pIC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 412 6 0 6 4.9 CC(=O)OCc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
935062 46161 11 None -1 2 Human 4.4 pIC50 = 4.4 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 343 4 1 3 3.3 CN1CCN(c2ccccc2NC(=O)Cc2ccc(Cl)cc2)CC1 nan
CHEMBL1536967 46161 11 None -1 2 Human 4.4 pIC50 = 4.4 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 343 4 1 3 3.3 CN1CCN(c2ccccc2NC(=O)Cc2ccc(Cl)cc2)CC1 nan
11995140 140934 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 522 4 0 7 5.5 O=c1c2sc(-c3ccc(C(F)(F)F)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL384371 140934 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 522 4 0 7 5.5 O=c1c2sc(-c3ccc(C(F)(F)F)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
54582476 60252 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1cccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2011.02.046
CHEMBL1760080 60252 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1cccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2011.02.046
16756753 91682 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 478 7 1 3 7.0 Cc1ccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060383x
CHEMBL242003 91682 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 478 7 1 3 7.0 Cc1ccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060383x
44394605 66668 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 271 4 1 4 2.7 CC(CN1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL187003 66668 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 271 4 1 4 2.7 CC(CN1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11993897 96923 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 614 8 0 9 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(CCCN4CCOCC4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL269695 96923 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 614 8 0 9 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCN(CCCN4CCOCC4)CC3)ccc2c1 10.1021/jm060572f
90666262 108872 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)nc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219271 108872 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)nc3)CC2)c1 10.1039/C1MD00015B
9844702 64361 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818788 64361 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
49866036 16040 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 520 8 1 4 6.9 CC(=O)Nc1cccc(C2CCN(CCCC(F)(F)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224306 16040 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 520 8 1 4 6.9 CC(=O)Nc1cccc(C2CCN(CCCC(F)(F)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
46850890 58792 0 None -3 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 7 3.9 CCOC(=O)c1cccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)c1 nan
CHEMBL1698073 58792 0 None -3 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 7 3.9 CCOC(=O)c1cccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)c1 nan
46172918 59086 0 None -5 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 1 5 4.3 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(CO)cc3)c2=O)cc1 nan
CHEMBL1710128 59086 0 None -5 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 370 5 1 5 4.3 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(CO)cc3)c2=O)cc1 nan
11995026 141363 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 493 4 0 7 5.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCOCC3)cc2c1 10.1021/jm060814b
CHEMBL386900 141363 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 493 4 0 7 5.8 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCOCC3)cc2c1 10.1021/jm060814b
44405408 72074 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 376 5 3 5 3.5 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c[nH]nc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL198789 72074 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 376 5 3 5 3.5 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c[nH]nc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44397221 66781 0 None -4 2 Mouse 6.4 pIC50 = 6.4 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 453 6 1 5 4.3 N#Cc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187503 66781 0 None -4 2 Mouse 6.4 pIC50 = 6.4 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 453 6 1 5 4.3 N#Cc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
54585376 60248 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccccc2F)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760071 60248 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccccc2F)cc1 10.1016/j.bmcl.2011.02.046
70693620 72783 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 9 2 5 4.1 N[C@H]1CN(c2ccc(CCNC(=O)c3ccc(OCC4CC4)cc3)cn2)C[C@@H]1c1cc(F)ccc1F 10.1016/j.bmcl.2012.02.010
CHEMBL2011529 72783 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 9 2 5 4.1 N[C@H]1CN(c2ccc(CCNC(=O)c3ccc(OCC4CC4)cc3)cn2)C[C@@H]1c1cc(F)ccc1F 10.1016/j.bmcl.2012.02.010
69603769 73088 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 425 5 1 6 3.4 Cc1nc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016698 73088 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 425 5 1 6 3.4 Cc1nc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70695859 73140 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 454 6 2 6 4.4 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016778 73140 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 454 6 2 6 4.4 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
90666261 108871 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 571 7 1 6 6.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
CHEMBL3219270 108871 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 571 7 1 6 6.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
70685408 73243 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 6 5.5 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017745 73243 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 553 6 1 6 5.5 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
11974231 81994 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 410 5 1 5 3.3 COc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1021/jm060683e
CHEMBL217400 81994 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 410 5 1 5 3.3 COc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1021/jm060683e
46835791 59029 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 362 6 0 5 4.8 C=Cc1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
CHEMBL1707743 59029 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 362 6 0 5 4.8 C=Cc1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
46172919 59528 0 None -14 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cc(C)cc(C)c3)c2=O)cc1 nan
CHEMBL1729021 59528 0 None -14 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3cc(C)cc(C)c3)c2=O)cc1 nan
46172935 59635 0 None -6 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.2 CCc1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
CHEMBL1733129 59635 0 None -6 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.2 CCc1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
11995137 141013 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3cccc(Cl)c3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL384825 141013 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3cccc(Cl)c3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
44416362 165210 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 371 6 0 7 2.9 COc1cc(-n2cnc3ccsc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL424723 165210 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 371 6 0 7 2.9 COc1cc(-n2cnc3ccsc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
45485063 195682 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.6 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(Cl)cc(Cl)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL569204 195682 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.6 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(Cl)cc(Cl)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
57522945 76017 0 None 2 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059419 76017 0 None 2 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
70691653 73119 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 510 7 3 6 4.3 Cc1nc(N2CCC(NC(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016730 73119 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 510 7 3 6 4.3 Cc1nc(N2CCC(NC(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70687477 73138 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 7 1 7 4.4 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016776 73138 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 7 1 7 4.4 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11561126 68504 0 None -2 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells by aequorin bioluminescence assayAntagonist activity at rat MCHR1 expressed in HEK293 cells by aequorin bioluminescence assay
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922270 68504 0 None -2 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells by aequorin bioluminescence assayAntagonist activity at rat MCHR1 expressed in HEK293 cells by aequorin bioluminescence assay
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
44417949 81864 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 539 9 5 4 4.0 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2Oc2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217171 81864 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 539 9 5 4 4.0 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2Oc2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
18436114 74528 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 451 6 1 4 6.1 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
CHEMBL2031734 74528 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 451 6 1 4 6.1 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
18435902 76007 0 None -1 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059409 76007 0 None -1 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
57523087 1132 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
7754 1132 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
CHEMBL2059513 1132 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
23027211 195564 0 None 26 4 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 421 5 2 5 4.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568400 195564 0 None 26 4 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 421 5 2 5 4.3 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
21939937 64371 0 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818800 64371 0 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
11995552 79857 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL213973 79857 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 488 4 0 7 5.1 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
11995138 81850 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 532 4 0 7 5.3 O=c1c2sc(-c3ccc(Br)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL217158 81850 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 532 4 0 7 5.3 O=c1c2sc(-c3ccc(Br)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
56597991 138633 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 481 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCN(C)CC5)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787461 138633 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 481 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCN(C)CC5)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
10159452 74480 0 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2nc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031575 74480 0 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2nc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
70689594 73185 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 472 5 2 6 4.5 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017588 73185 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 472 5 2 6 4.5 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44394891 64869 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5ccc(Cl)cc5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL182575 64869 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5ccc(Cl)cc5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
57400241 68492 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 284 1 1 2 3.4 COc1ccc2[nH]c3c(c2c1)C(C)C1CN(C)CCC1C3 10.1016/j.bmcl.2011.09.110
CHEMBL1922256 68492 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 284 1 1 2 3.4 COc1ccc2[nH]c3c(c2c1)C(C)C1CN(C)CCC1C3 10.1016/j.bmcl.2011.09.110
70687361 72784 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 7 1 5 4.7 CCCCOc1ccc2c(c1)CCN(c1ccc(N3C[C@H](c4cc(F)ccc4F)[C@@H](N)C3)nc1)C2=O 10.1016/j.bmcl.2012.02.010
CHEMBL2011532 72784 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 492 7 1 5 4.7 CCCCOc1ccc2c(c1)CCN(c1ccc(N3C[C@H](c4cc(F)ccc4F)[C@@H](N)C3)nc1)C2=O 10.1016/j.bmcl.2012.02.010
46835788 59571 0 None -3 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 7 3.9 CCOC(=O)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
CHEMBL1730555 59571 0 None -3 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 400 6 0 7 3.9 CCOC(=O)c1ccc(-n2ncc(Cl)c(Oc3ccc(OC)cc3)c2=O)cc1 nan
70685346 73135 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 493 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016772 73135 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 493 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44438745 93412 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 551 11 1 6 4.9 O=C(NC1CCN(Cc2ccc(OCCCN(C3CC3)C3CC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL247891 93412 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 551 11 1 6 4.9 O=C(NC1CCN(Cc2ccc(OCCCN(C3CC3)C3CC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
44414342 77667 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 458 4 0 5 5.1 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL209895 77667 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 458 4 0 5 5.1 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
54583954 60296 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760237 60296 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44394826 66257 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 585 9 1 5 9.0 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCc5ccc(-c6cccc(C(F)(F)F)c6)o5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL185266 66257 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 585 9 1 5 9.0 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCc5ccc(-c6cccc(C(F)(F)F)c6)o5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
11440762 81715 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 392 6 1 6 3.6 COc1ccc(OCC(=O)Nc2ccc3nc(N4CCCC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2006.11.092
CHEMBL216754 81715 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 392 6 1 6 3.6 COc1ccc(OCC(=O)Nc2ccc3nc(N4CCCC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2006.11.092
11531660 135058 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 410 4 1 5 4.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)CCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL372919 135058 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 410 4 1 5 4.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)CCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
54585375 60247 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 474 10 1 5 4.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccccc2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760070 60247 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 474 10 1 5 4.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2ccccc2)cc1 10.1016/j.bmcl.2011.02.046
46835793 58979 0 None -6 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 382 4 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3cccc4c3CCCC4)c2=O)cc1 nan
CHEMBL1705499 58979 0 None -6 2 Human 5.4 pIC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 382 4 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3cccc4c3CCCC4)c2=O)cc1 nan
11973801 141424 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(F)c1 10.1021/jm060683e
CHEMBL387309 141424 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(F)c1 10.1021/jm060683e
90666254 108863 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 492 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CC4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219263 108863 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 492 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CC4)cc3)CC2)c1 10.1039/C1MD00015B
70691724 73207 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 450 7 2 5 5.0 Cc1nc(N(CCO)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017610 73207 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 450 7 2 5 5.0 Cc1nc(N(CCO)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11995346 81064 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 530 5 0 8 3.9 CN(C)CC1CN(S(C)(=O)=O)c2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL216008 81064 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 530 5 0 8 3.9 CN(C)CC1CN(S(C)(=O)=O)c2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
11974228 79947 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 460 4 1 6 3.3 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)c(F)c2o1 10.1021/jm060683e
CHEMBL214413 79947 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 460 4 1 6 3.3 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)c(F)c2o1 10.1021/jm060683e
71816518 137743 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770706 137743 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH (4 to 19 residues)-stimulated intracellular calcium mobilization after 24 hrs by fluorometric analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
44442097 93563 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1cccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc12 10.1016/j.bmcl.2007.05.034
CHEMBL248694 93563 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1cccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc12 10.1016/j.bmcl.2007.05.034
44417862 80204 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 366 7 1 4 3.2 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215114 80204 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 366 7 1 4 3.2 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
22348140 168147 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 501 6 1 6 5.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2006.02.044
CHEMBL436953 168147 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 501 6 1 6 5.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2006.02.044
11648240 71102 0 None -1 3 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196196 71102 0 None -1 3 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
16739263 92968 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 538 8 2 6 3.3 O=C(NC1CCN(Cc2ccc(C(=O)NCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL245846 92968 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 538 8 2 6 3.3 O=C(NC1CCN(Cc2ccc(C(=O)NCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
90666264 108874 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 582 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5c(F)cc(F)cc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219273 108874 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 582 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5c(F)cc(F)cc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
127031339 138632 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1nnc(-c2ccccc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787457 138632 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1nnc(-c2ccccc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
1314 3657 18 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
9865843 3657 18 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
CHEMBL178707 3657 18 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
23593468 64358 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818785 64358 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
70683299 73245 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 503 5 1 5 5.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017747 73245 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 503 5 1 5 5.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
44414310 137940 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 439 5 0 5 5.2 CCc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL377479 137940 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 439 5 0 5 5.2 CCc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
54585864 60306 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 493 10 1 5 3.7 COc1ccc([C@H]2CN(CCCN(C)S(C)(=O)=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760249 60306 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 493 10 1 5 3.7 COc1ccc([C@H]2CN(CCCN(C)S(C)(=O)=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44430478 86811 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 555 5 0 7 4.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)C(C)(C)C)C1 10.1016/j.bmcl.2007.02.012
CHEMBL233027 86811 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 555 5 0 7 4.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)C(C)(C)C)C1 10.1016/j.bmcl.2007.02.012
127031623 138606 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 450 6 0 6 4.2 O=C(c1nnc(-c2ccc(F)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787131 138606 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 450 6 0 6 4.2 O=C(c1nnc(-c2ccc(F)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
45279402 123059 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618336 123059 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
16756187 92727 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 507 9 2 3 5.9 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCC2)CC1 10.1021/jm060381c
CHEMBL244370 92727 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 507 9 2 3 5.9 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCC2)CC1 10.1021/jm060381c
20817800 70059 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 390 5 1 5 4.2 COc1ccc2oc(O)c/c(=N\C3CCN(C/C=C/c4ccccc4)CC3)c2c1 10.1021/jm050598r
CHEMBL194576 70059 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 390 5 1 5 4.2 COc1ccc2oc(O)c/c(=N\C3CCN(C/C=C/c4ccccc4)CC3)c2c1 10.1021/jm050598r
57404374 72786 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 506 6 1 6 4.6 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)CC[C@@H]1c1cc(F)c(F)cc1F 10.1016/j.bmcl.2012.02.010
CHEMBL2011535 72786 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced responseAntagonist activity at human MCH1R expressed in CHO cells assessed as inhibition of MCH-induced response
ChEMBL 506 6 1 6 4.6 N[C@H]1CN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)CC[C@@H]1c1cc(F)c(F)cc1F 10.1016/j.bmcl.2012.02.010
44417988 81995 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 515 10 5 4 3.5 COc1ccc2cc(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)ccc2c1 10.1016/j.bmcl.2006.10.056
CHEMBL217403 81995 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 515 10 5 4 3.5 COc1ccc2cc(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)ccc2c1 10.1016/j.bmcl.2006.10.056
71227161 128652 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3670644 128652 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
70691651 73102 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 7 1 7 4.3 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016713 73102 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 543 7 1 7 4.3 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70691737 73254 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 489 6 2 5 4.7 Cc1nc(N2CCC(NC(=O)C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017756 73254 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 489 6 2 5 4.7 Cc1nc(N2CCC(NC(=O)C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11684745 15900 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 499 9 2 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223830 15900 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 499 9 2 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417943 82052 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 491 9 5 4 3.6 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2s1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217678 82052 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 491 9 5 4 3.6 N=C(N)NCCC[C@@H](NC(=O)c1cc2ccccc2s1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
23658492 178389 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 434 10 1 7 3.4 COc1cc(-n2ccnc(NCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL470633 178389 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 434 10 1 7 3.4 COc1cc(-n2ccnc(NCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
44405430 71590 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 370 5 2 4 4.3 COc1cccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c1 10.1016/j.bmcl.2005.08.049
CHEMBL197281 71590 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 370 5 2 4 4.3 COc1cccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c1 10.1016/j.bmcl.2005.08.049
10083869 65228 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65228 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
20817864 75692 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 483 5 1 8 3.8 COC(=O)c1c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n(C)c1=O 10.1016/j.bmcl.2006.02.044
CHEMBL205741 75692 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 483 5 1 8 3.8 COC(=O)c1c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n(C)c1=O 10.1016/j.bmcl.2006.02.044
45484974 195603 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.7 CCN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)ncc1C 10.1016/j.bmcl.2009.09.003
CHEMBL568649 195603 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.7 CCN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)ncc1C 10.1016/j.bmcl.2009.09.003
44394883 125830 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 271 6 2 4 2.6 CC(CNCC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL365041 125830 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 271 6 2 4 2.6 CC(CNCC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
54579971 60297 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 536 12 1 5 5.8 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760238 60297 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 536 12 1 5 5.8 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
46835797 59424 0 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 476 5 0 5 4.6 O=C(C1CCCCN1Cc1ccc(Cl)c(Cl)c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1725011 59424 0 None -1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 476 5 0 5 4.6 O=C(C1CCCCN1Cc1ccc(Cl)c(Cl)c1)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
11632909 132907 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ncoc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL370608 132907 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ncoc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
10377914 122645 1 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 260 5 1 4 3.0 COC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL361288 122645 1 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 260 5 1 4 3.0 COC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
90666256 108865 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 536 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CCOCC4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219265 108865 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 536 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CCOCC4)cc3)CC2)c1 10.1039/C1MD00015B
21062999 64272 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
CHEMBL1817681 64272 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
46172937 58786 0 None -4 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 454 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3ccc(I)cc3)c2=O)cc1 nan
CHEMBL1697929 58786 0 None -4 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 454 4 0 5 4.3 COc1ccc(Oc2c(Cl)cnn(-c3ccc(I)cc3)c2=O)cc1 nan
11975436 78668 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)c(Cl)ccc2o1 10.1021/jm060683e
CHEMBL2113245 78668 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)c(Cl)ccc2o1 10.1021/jm060683e
3202885 40426 4 None - 1 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 422 8 1 4 4.7 O=C(NC1CCCC1)C(c1ccccc1)N(Cc1ccco1)C(=O)Cc1cccs1 nan
CHEMBL1484343 40426 4 None - 1 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 422 8 1 4 4.7 O=C(NC1CCCC1)C(c1ccccc1)N(Cc1ccco1)C(=O)Cc1cccs1 nan
11995139 82397 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 8 4.4 N#Cc1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
CHEMBL218031 82397 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 8 4.4 N#Cc1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
44562500 186143 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 479 7 1 4 4.5 O=C(COc1ccc(F)c(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL488721 186143 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 479 7 1 4 4.5 O=C(COc1ccc(F)c(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
44438747 92929 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 485 8 1 7 3.5 CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL245642 92929 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 485 8 1 7 3.5 CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
54584857 60256 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 484 9 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccsc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
CHEMBL1760084 60256 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 484 9 1 5 5.1 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccsc3)C2)cc1OC 10.1016/j.bmcl.2011.02.046
46835810 58798 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 364 6 0 6 4.0 COc1ccc(Oc2c(C=O)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1698337 58798 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 364 6 0 6 4.0 COc1ccc(Oc2c(C=O)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
53318593 56401 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 458 8 0 5 4.9 O=c1cc(OCc2ccc(C(F)(F)F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642477 56401 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assayAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium release by FLIPR assay
ChEMBL 458 8 0 5 4.9 O=c1cc(OCc2ccc(C(F)(F)F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11605775 15850 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223708 15850 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44405570 71633 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 6 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5nsnc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197395 71633 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 6 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5nsnc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
11994277 81214 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 528 6 1 6 5.7 O=C(NCCN1CCCC1)c1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2c1 10.1021/jm060814b
CHEMBL216356 81214 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 528 6 1 6 5.7 O=C(NCCN1CCCC1)c1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2c1 10.1021/jm060814b
15987265 195202 0 None 61 5 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL566075 195202 0 None 61 5 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 503 6 2 5 5.3 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
44425834 150872 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells by MCH-stimulated [35S]GTP-gammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cells by MCH-stimulated [35S]GTP-gammaS binding assay
ChEMBL 562 7 0 5 6.6 COc1cccc(N2C(=O)N(CC3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL396174 150872 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells by MCH-stimulated [35S]GTP-gammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cells by MCH-stimulated [35S]GTP-gammaS binding assay
ChEMBL 562 7 0 5 6.6 COc1cccc(N2C(=O)N(CC3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44417957 141361 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 523 9 5 3 3.9 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2-c2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL386880 141361 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 523 9 5 3 3.9 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2-c2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
44416777 80139 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 511 4 0 7 6.5 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccc(N(C)C)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL214908 80139 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 511 4 0 7 6.5 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccc(N(C)C)cc1 10.1016/j.bmcl.2006.07.054
44416872 80164 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 498 4 0 7 6.4 COc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL215008 80164 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 498 4 0 7 6.4 COc1ccc(-n2c(C)nc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc32)cc1 10.1016/j.bmcl.2006.07.054
44416838 80416 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 464 6 0 7 5.5 COCCCn1c(C)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
CHEMBL215256 80416 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 464 6 0 7 5.5 COCCCn1c(C)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
44417146 140889 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 504 6 1 7 5.2 CN(CCN1CCCC1)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL384132 140889 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 504 6 1 7 5.2 CN(CCN1CCCC1)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44416955 140909 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 5 0 7 5.6 CCCn1c(N(C)C)nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1016/j.bmcl.2006.07.054
CHEMBL384233 140909 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 5 0 7 5.6 CCCn1c(N(C)C)nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1016/j.bmcl.2006.07.054
44416935 141120 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 5 0 7 5.6 CCCn1c(N(C)C)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
CHEMBL385410 141120 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 463 5 0 7 5.6 CCCn1c(N(C)C)nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc21 10.1016/j.bmcl.2006.07.054
44417066 141408 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 1 6 5.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL387217 141408 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 1 6 5.6 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(N3CCCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
44416302 79623 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 492 8 0 9 4.5 COc1cc(-n2cnc3cc(-c4ccc([N+](=O)[O-])cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212958 79623 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 492 8 0 9 4.5 COc1cc(-n2cnc3cc(-c4ccc([N+](=O)[O-])cc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44416231 168413 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(-n2cnc3cc(-c4ccccc4Cl)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL439146 168413 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(-n2cnc3cc(-c4ccccc4Cl)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
11201645 71512 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197050 71512 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11995441 141417 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 2 8 4.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CC[C@H](O)C1)O2 10.1021/jm060572f
CHEMBL387266 141417 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 2 8 4.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CC[C@H](O)C1)O2 10.1021/jm060572f
57396294 67731 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914637 67731 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57399740 67727 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914633 67727 0 None 1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
1314 3657 18 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2009.09.003
9865843 3657 18 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2009.09.003
CHEMBL178707 3657 18 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2009.09.003
11995243 82126 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 555 5 0 7 6.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(N4CCCC4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL217812 82126 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 555 5 0 7 6.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(N4CCCC4)CC3)ccc2c1 10.1021/jm060572f
11654412 197230 22 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL584538 197230 22 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPRAntagonistic activity against MCH1R expressed on CHOK1 cells assessed as intracellular calcium mobilization by FLIPR
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
11994661 81997 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 567 5 0 6 8.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCC(c4ccccc4)CC3)cc2c1 10.1021/jm060814b
CHEMBL217410 81997 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 567 5 0 6 8.4 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2sc(CN3CCC(c4ccccc4)CC3)cc2c1 10.1021/jm060814b
21940083 64372 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818801 64372 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
127031355 138625 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 448 6 1 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CCC(Oc2ccc(CN3CCC(O)C3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787345 138625 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 448 6 1 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CCC(Oc2ccc(CN3CCC(O)C3)cc2)CC1 10.1021/acs.jmedchem.5b01654
23532180 68494 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.7 CC1c2c([nH]c3cc(Cl)c(Cl)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922258 68494 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 322 0 1 1 4.7 CC1c2c([nH]c3cc(Cl)c(Cl)cc23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
57403785 68505 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 448 5 1 2 6.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922271 68505 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 448 5 1 2 6.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
44410876 75737 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 482 8 1 7 5.0 CCCCCn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL205760 75737 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 482 8 1 7 5.0 CCCCCn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
45279868 123061 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618338 123061 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assayAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-induced Ca2+ influx for 120 mins by FLIPR assay
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
46172920 58927 0 None -7 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 340 4 0 4 4.5 CCc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1703562 58927 0 None -7 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 340 4 0 4 4.5 CCc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
45382322 59360 0 None 3 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 419 3 0 6 4.0 Cc1ccc(-n2ncc(Cl)c(OC3CCN(C(=O)OC(C)(C)C)CC3)c2=O)cc1 nan
CHEMBL1722551 59360 0 None 3 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 419 3 0 6 4.0 Cc1ccc(-n2ncc(Cl)c(OC3CCN(C(=O)OC(C)(C)C)CC3)c2=O)cc1 nan
11995645 141010 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 472 4 0 7 4.6 O=c1c2sc(-c3ccc(F)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL384805 141010 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 472 4 0 7 4.6 O=c1c2sc(-c3ccc(F)cc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
11995647 141446 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 510 4 0 7 5.8 CC(C)(C)c1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
CHEMBL387420 141446 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 510 4 0 7 5.8 CC(C)(C)c1ccc(-c2cc3ncn(-c4ccc5nc(CN6CCOCC6)ccc5c4)c(=O)c3s2)cc1 10.1021/jm060572f
44562415 176381 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 436 6 1 5 3.9 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462351 176381 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 436 6 1 5 3.9 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1016/j.bmcl.2008.07.079
44394770 123309 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 3 1 6 3.2 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL362501 123309 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 363 3 1 6 3.2 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
44417971 140999 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 488 10 6 3 2.8 N=C(N)NCCC[C@@H](NC(=O)Cc1cc2ccccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL384734 140999 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 488 10 6 3 2.8 N=C(N)NCCC[C@@H](NC(=O)Cc1cc2ccccc2[nH]1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11692293 93013 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 534 8 2 6 3.5 O=C(NCCN1CCCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL246050 93013 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 534 8 2 6 3.5 O=C(NCCN1CCCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
44417841 81164 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216315 81164 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.053
44405486 139969 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 409 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL381013 139969 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 409 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44405412 71515 1 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 388 5 2 4 4.4 COc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c(F)c1 10.1016/j.bmcl.2005.08.049
CHEMBL197058 71515 1 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 388 5 2 4 4.4 COc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c(F)c1 10.1016/j.bmcl.2005.08.049
44405468 132898 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 474 6 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL370576 132898 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 474 6 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
11974130 79937 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 434 5 1 6 3.5 CCc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL214377 79937 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 434 5 1 6 3.5 CCc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
44394921 65893 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 431 9 2 4 4.3 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL184579 65893 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 431 9 2 4 4.3 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
90666097 108829 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 534 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219000 108829 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 534 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
90666265 108875 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cccnc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219274 108875 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cccnc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
44430465 92854 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 553 5 0 6 5.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCCCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL245135 92854 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 553 5 0 6 5.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCCCC2)C1 10.1016/j.bmcl.2007.02.012
20817763 140040 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 522 5 1 7 4.2 Cn1c(=O)c(C(=O)N2CCCC2)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL381335 140040 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 522 5 1 7 4.2 Cn1c(=O)c(C(=O)N2CCCC2)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44410904 171880 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL448110 171880 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44394769 66566 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 361 5 1 4 4.7 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL186548 66566 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 361 5 1 4 4.7 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
54580458 60242 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(F)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760061 60242 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 492 10 1 5 4.5 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(F)c2)cc1 10.1016/j.bmcl.2011.02.046
22254581 65878 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 448 7 1 4 8.0 CC(CC(C)(C)C)Oc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL184520 65878 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 448 7 1 4 8.0 CC(CC(C)(C)C)Oc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12 10.1016/j.bmcl.2004.07.032
44396952 66380 0 None -5 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1ccccc1-c1ccc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL185688 66380 0 None -5 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1ccccc1-c1ccc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
44397262 67153 0 None -17 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 406 4 1 4 4.1 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189496 67153 0 None -17 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 406 4 1 4 4.1 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.023
44394705 124788 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(O[C@@H]3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364540 124788 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(O[C@@H]3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
10262766 66630 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 216 3 1 3 3.0 CCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186818 66630 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 216 3 1 3 3.0 CCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70685338 73118 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(NC(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016729 73118 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(NC(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70689595 73199 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 476 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017602 73199 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 476 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11691995 15927 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 511 10 2 6 5.7 COc1cccc(Cn2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223886 15927 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 511 10 2 6 5.7 COc1cccc(Cn2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)c1 10.1016/j.bmcl.2010.07.086
44397425 66528 0 None -6 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 422 5 1 5 3.7 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186333 66528 0 None -6 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 422 5 1 5 3.7 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2005.05.023
16756638 92784 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cccc(C(F)(F)F)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244790 92784 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cccc(C(F)(F)F)c4)c3)CC2)c1 10.1021/jm060383x
46172939 59516 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 348 5 0 5 4.2 COc1ccc(Oc2c(C3CC3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1728621 59516 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 348 5 0 5 4.2 COc1ccc(Oc2c(C3CC3)cnn(-c3ccc(C)cc3)c2=O)cc1 nan
46835805 59521 0 None -9 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C)c3)c2=O)cc1 nan
CHEMBL1728794 59521 0 None -9 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 342 4 0 5 4.0 COc1ccc(Oc2c(Cl)cnn(-c3cccc(C)c3)c2=O)cc1 nan
44438750 92967 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 571 9 1 8 3.9 O=C(NC1CCN(Cc2ccc(OCCCN3C(=O)CSC3=O)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL245844 92967 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 571 9 1 8 3.9 O=C(NC1CCN(Cc2ccc(OCCCN3C(=O)CSC3=O)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
44414455 79847 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 442 5 0 7 4.1 COc1ccncc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
CHEMBL213933 79847 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 442 5 0 7 4.1 COc1ccncc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
70685347 73147 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3ccc(F)cc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016784 73147 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3ccc(F)cc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44410849 137756 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 508 6 1 5 6.3 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
CHEMBL377084 137756 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 508 6 1 5 6.3 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
44405651 71571 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
CHEMBL197232 71571 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
46172942 58818 0 None -3 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 380 3 0 4 5.0 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(C(F)(F)F)cc3)c2=O)cc1 nan
CHEMBL1698879 58818 0 None -3 2 Human 5.3 pIC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 380 3 0 4 5.0 Cc1ccc(-n2ncc(Cl)c(Oc3ccc(C(F)(F)F)cc3)c2=O)cc1 nan
70691739 73262 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 543 7 2 7 3.9 Cc1nc(N2CCC(N(C)C(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017764 73262 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 543 7 2 7 3.9 Cc1nc(N2CCC(N(C)C(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44405619 72144 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccncc1 10.1016/j.bmcl.2005.08.049
CHEMBL199025 72144 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccncc1 10.1016/j.bmcl.2005.08.049
44397127 66733 0 None -11 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 350 6 1 3 3.6 COc1cccc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187296 66733 0 None -11 2 Mouse 6.3 pIC50 = 6.3 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 350 6 1 3 3.6 COc1cccc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
49866087 16052 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 515 9 1 6 6.2 CCOC(=O)c1ccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)cc1O 10.1016/j.bmcl.2010.07.086
CHEMBL1224387 16052 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 515 9 1 6 6.2 CCOC(=O)c1ccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)cc1O 10.1016/j.bmcl.2010.07.086
70693796 73206 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 420 5 1 4 5.6 Cc1nc(N(C)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017609 73206 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 420 5 1 4 5.6 Cc1nc(N(C)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
16755870 143941 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 483 9 2 3 5.4 CC(C)C(=O)Nc1cccc(C2CCN(CCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL390679 143941 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 483 9 2 3 5.4 CC(C)C(=O)Nc1cccc(C2CCN(CCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
16756402 92400 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 398 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL243794 92400 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 398 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
46172928 59381 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 419 6 0 6 5.1 COc1ccc(Oc2c(N3CCCCC3)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1723453 59381 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 419 6 0 6 5.1 COc1ccc(Oc2c(N3CCCCC3)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
46172932 59552 0 None -4 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 374 4 0 4 5.5 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(Cl)cc3)c2=O)cc1 nan
CHEMBL1729749 59552 0 None -4 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 374 4 0 4 5.5 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(Cl)cc3)c2=O)cc1 nan
70693794 73196 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 496 5 2 5 5.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017599 73196 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 496 5 2 5 5.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2012.03.049
44414499 79902 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 441 5 0 6 5.1 Cc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL214223 79902 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 441 5 0 6 5.1 Cc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
23027181 195522 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 418 6 2 6 3.0 CN(C)c1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568209 195522 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 418 6 2 6 3.0 CN(C)c1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
44562563 173778 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)n[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL455144 173778 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)n[nH]2)cc1 10.1016/j.bmcl.2008.07.079
11452268 81147 0 None 15 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL216228 81147 0 None 15 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
23532172 68495 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 398 2 1 1 6.0 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(Cc3ccccc3)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922259 68495 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 398 2 1 1 6.0 CC1c2c([nH]c3ccc(C(F)(F)F)cc23)CC2CCN(Cc3ccccc3)CC21 10.1016/j.bmcl.2011.09.110
44394859 65899 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 257 5 2 4 2.3 CC(CNC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184589 65899 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 257 5 2 4 2.3 CC(CNC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
46846324 59083 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1ccccc1CN1CCCCC1C(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
CHEMBL1710048 59083 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1ccccc1CN1CCCCC1C(=O)N1CCN(c2ccc([N+](=O)[O-])cc2)CC1 nan
46846320 59652 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1ccc(CN2CCCCC2C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)cc1 nan
CHEMBL1733974 59652 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1ccc(CN2CCCCC2C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)cc1 nan
11974346 140956 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 422 5 1 5 3.5 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL384487 140956 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 422 5 1 5 3.5 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
11612098 69926 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 448 4 1 6 4.8 O=c1cc(NC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194292 69926 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 448 4 1 6 4.8 O=c1cc(NC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44395076 66646 0 None 3 2 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 549 10 3 5 5.7 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL186894 66646 0 None 3 2 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 549 10 3 5 5.7 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.07.077
44414518 77541 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 459 4 0 5 5.6 Cc1cc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)ccc1Cl 10.1016/j.bmcl.2006.05.075
CHEMBL209416 77541 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 459 4 0 5 5.6 Cc1cc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)ccc1Cl 10.1016/j.bmcl.2006.05.075
44414327 79756 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 479 4 0 5 5.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213540 79756 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 479 4 0 5 5.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
90666266 108876 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cnccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219275 108876 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cnccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
23120572 194379 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL560474 194379 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
70683241 73141 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 504 7 2 7 4.6 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016779 73141 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 504 7 2 7 4.6 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
70689527 73149 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 571 7 2 8 4.9 Cc1nc(N2CCC(O)(c3ccc(F)cn3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016786 73149 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 571 7 2 8 4.9 Cc1nc(N2CCC(O)(c3ccc(F)cn3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442064 154258 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 351 5 2 4 5.1 Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL400298 154258 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 351 5 2 4 5.1 Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
70683286 73193 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 458 6 2 6 4.3 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017596 73193 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 458 6 2 6 4.3 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
11975438 79807 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 380 4 1 4 3.3 O=C(NC1CCN(Cc2ccccc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL213761 79807 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 380 4 1 4 3.3 O=C(NC1CCN(Cc2ccccc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
23027527 195107 0 None 50 5 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL565551 195107 0 None 50 5 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 371 5 2 5 3.1 Cc1cnc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc1N(C)C 10.1016/j.bmcl.2009.09.003
57393332 68503 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 420 3 1 2 5.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922269 68503 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 420 3 1 2 5.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
11561126 68504 0 None 2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922270 68504 0 None 2 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
70687552 73259 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 529 7 3 7 3.6 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017761 73259 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 529 7 3 7 3.6 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11993895 79957 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 630 5 0 6 8.7 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccc(C(F)(F)F)cc4)CC3)ccc2c1 10.1021/jm060572f
CHEMBL214468 79957 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 630 5 0 6 8.7 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2nc(CN3CCC(c4ccc(C(F)(F)F)cc4)CC3)ccc2c1 10.1021/jm060572f
11305934 3776 2 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assayAntagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assay
ChEMBL 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 10.1016/j.bmcl.2012.08.025
1315 3776 2 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assayAntagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assay
ChEMBL 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 10.1016/j.bmcl.2012.08.025
CHEMBL2147477 3776 2 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assayAntagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR assay
ChEMBL 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 10.1016/j.bmcl.2012.08.025
11993896 80676 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 515 5 0 7 5.5 CCN1CCN(Cc2ccc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3n2)CC1 10.1021/jm060572f
CHEMBL215591 80676 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 515 5 0 7 5.5 CCN1CCN(Cc2ccc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3n2)CC1 10.1021/jm060572f
56589628 67792 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914852 67792 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
44416845 80118 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 0 7 5.3 Cn1c(N2CCCC2)nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1016/j.bmcl.2006.07.054
CHEMBL214824 80118 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 461 3 0 7 5.3 Cn1c(N2CCCC2)nc2ccc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1016/j.bmcl.2006.07.054
44416814 80389 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 474 3 0 6 6.9 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C1CCCCC1 10.1016/j.bmcl.2006.07.054
CHEMBL215234 80389 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 474 3 0 6 6.9 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C1CCCCC1 10.1016/j.bmcl.2006.07.054
44416815 140930 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 505 5 0 8 4.8 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2006.07.054
CHEMBL384346 140930 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 505 5 0 8 4.8 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2006.07.054
44417151 141011 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 3 0 7 4.7 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C 10.1016/j.bmcl.2006.07.054
CHEMBL384806 141011 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 3 0 7 4.7 CN(C)c1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1C 10.1016/j.bmcl.2006.07.054
44417145 141039 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 490 6 2 7 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(NCCN3CCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
CHEMBL384988 141039 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 490 6 2 7 5.2 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2[nH]c(NCCN3CCCC3)nc2c1 10.1016/j.bmcl.2006.07.054
44416315 79409 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(-n2cnc3cc(-c4cccc(Cl)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL212137 79409 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 481 7 0 7 5.3 COc1cc(-n2cnc3cc(-c4cccc(Cl)c4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
44416376 140883 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 475 7 0 6 5.2 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
CHEMBL384113 140883 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assayAntagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay
ChEMBL 475 7 0 6 5.2 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.07.008
23022536 76016 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059418 76016 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
57523086 76023 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
CHEMBL2059426 76023 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
23027402 195605 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568663 195605 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 5 2 5 3.7 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
22251624 64366 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818795 64366 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
57521366 76027 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059512 76027 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release after 45 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
44414570 77670 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 471 6 0 7 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(OC)c1 10.1016/j.bmcl.2006.05.075
CHEMBL209905 77670 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 471 6 0 7 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(OC)c1 10.1016/j.bmcl.2006.05.075
11531010 133052 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL371222 133052 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
45485043 195519 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 475 5 3 5 4.8 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N 10.1016/j.bmcl.2009.09.003
CHEMBL568183 195519 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 475 5 3 5 4.8 Cc1cnc(N[C@H]2CC[C@@H](CNC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)nc1N 10.1016/j.bmcl.2009.09.003
49865738 15925 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 537 9 2 5 7.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C(C)(C)C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223884 15925 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 537 9 2 5 7.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C(C)(C)C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
16755968 92046 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 539 13 2 3 7.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243129 92046 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 539 13 2 3 7.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44394650 65136 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 7 2 5 3.4 COc1cccc(CNCC(C)Oc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL183032 65136 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 7 2 5 3.4 COc1cccc(CNCC(C)Oc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
11974229 82057 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 460 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OC(F)(F)O3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL217707 82057 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 460 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OC(F)(F)O3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
11778029 65862 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 272 4 1 3 4.5 CNc1ccc2cccc(OC(C)CC(C)(C)C)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184446 65862 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 272 4 1 3 4.5 CNc1ccc2cccc(OC(C)CC(C)(C)C)c2n1 10.1016/j.bmcl.2004.07.032
127031908 138629 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 431 6 0 5 4.6 O=C(c1cc(-c2ccccc2)on1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787417 138629 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 431 6 0 5 4.6 O=C(c1cc(-c2ccccc2)on1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
11553648 73116 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 425 5 2 6 3.5 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016727 73116 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 425 5 2 6 3.5 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
46850886 59588 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1cccc(CN2CCCCC2C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)c1 nan
CHEMBL1731173 59588 0 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 422 5 0 5 3.6 Cc1cccc(CN2CCCCC2C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)c1 nan
70691721 73194 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 478 6 2 5 5.3 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017597 73194 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 478 6 2 5 5.3 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44417828 80254 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215138 80254 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44410823 75188 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 500 5 1 5 5.8 O=c1nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL204508 75188 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 500 5 1 5 5.8 O=c1nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
44410821 76755 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 426 4 1 7 3.4 Cn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207668 76755 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 426 4 1 7 3.4 Cn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
16755872 92050 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 11 2 3 6.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243139 92050 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 511 11 2 3 6.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44405459 132622 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 374 4 2 3 4.9 Clc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1 10.1016/j.bmcl.2005.08.049
CHEMBL370360 132622 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 374 4 2 3 4.9 Clc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1 10.1016/j.bmcl.2005.08.049
44417931 141050 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 505 10 5 5 3.1 COc1cccc2cc(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)oc12 10.1016/j.bmcl.2006.10.056
CHEMBL385037 141050 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 505 10 5 5 3.1 COc1cccc2cc(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)oc12 10.1016/j.bmcl.2006.10.056
22254632 123564 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 244 3 1 4 2.2 Nc1ccc2cccc(OCC3CCOC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL363311 123564 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 244 3 1 4 2.2 Nc1ccc2cccc(OCC3CCOC3)c2n1 10.1016/j.bmcl.2004.07.032
11995240 80673 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 389 2 0 5 5.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2ncccc2c1 10.1021/jm060572f
CHEMBL215580 80673 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 389 2 0 5 5.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2ncccc2c1 10.1021/jm060572f
70695914 73195 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 494 7 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017598 73195 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 494 7 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11603897 123796 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4[nH]ccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL363583 123796 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4[nH]ccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44394763 66702 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 349 8 2 4 4.5 CC(C)c1ccc(CNCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
CHEMBL187162 66702 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 349 8 2 4 4.5 CC(C)c1ccc(CNCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
46835800 59020 0 None -3 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 397 5 1 5 4.8 CC(=O)Nc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1707135 59020 0 None -3 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 397 5 1 5 4.8 CC(=O)Nc1ccc(Oc2c(Cl)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
46835816 59719 0 None -3 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.1 COc1ccc(Oc2c(Cl)cnn(Cc3ccc(C)cc3)c2=O)cc1 nan
CHEMBL1736481 59719 0 None -3 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 356 5 0 5 4.1 COc1ccc(Oc2c(Cl)cnn(Cc3ccc(C)cc3)c2=O)cc1 nan
49865790 15951 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 462 7 1 4 6.5 Fc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223969 15951 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 462 7 1 4 6.5 Fc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
45485038 195597 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.6 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(Cl)cc(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL568604 195597 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 435 6 2 5 4.6 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(Cl)cc(Cl)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
54584905 60295 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.3 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)NCc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760236 60295 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 522 11 1 5 5.3 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)NCc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44405612 134943 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 481 6 1 5 6.4 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4ccccc4c3)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
CHEMBL372848 134943 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 481 6 1 5 6.4 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4ccccc4c3)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
1091600 27608 14 None - 1 Human 4.2 pIC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 386 5 1 6 2.7 CC(C)C(=O)N1CCN(c2ccccc2NC(=O)c2ccc([N+](=O)[O-])o2)CC1 nan
CHEMBL1371138 27608 14 None - 1 Human 4.2 pIC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 386 5 1 6 2.7 CC(C)C(=O)N1CCN(c2ccccc2NC(=O)c2ccc([N+](=O)[O-])o2)CC1 nan
49865929 16005 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 502 8 2 6 5.3 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224154 16005 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 502 8 2 6 5.3 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
21062990 64354 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818781 64354 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
11591644 15899 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223829 15899 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
16756186 92726 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL244369 92726 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
10389978 69256 0 None 75 2 Human 7.2 pIC50 = 7.2 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL193473 69256 0 None 75 2 Human 7.2 pIC50 = 7.2 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
887424 55862 6 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 277 9 0 2 4.6 CCCN(CCC)CCOc1cc(C)ccc1C(C)C nan
CHEMBL1582334 55862 6 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 277 9 0 2 4.6 CCCN(CCC)CCOc1cc(C)ccc1C(C)C nan
CHEMBL1626085 55862 6 None 1 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 277 9 0 2 4.6 CCCN(CCC)CCOc1cc(C)ccc1C(C)C nan
90666263 108873 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cn3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219272 108873 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cn3)CC2)c1 10.1039/C1MD00015B
10025899 76697 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 433 4 1 6 4.2 Cn1c(=O)nc(NC2CCN(Cc3ccc4ncccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207308 76697 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 433 4 1 6 4.2 Cn1c(=O)nc(NC2CCN(Cc3ccc4ncccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11512135 69950 0 None -3 2 Human 7.2 pIC50 = 7.2 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194408 69950 0 None -3 2 Human 7.2 pIC50 = 7.2 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
11201867 98220 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 454 4 1 6 3.9 Cc1c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)oc2cc(Cl)ccc2c1=O 10.1021/jm060683e
CHEMBL277531 98220 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 454 4 1 6 3.9 Cc1c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)oc2cc(Cl)ccc2c1=O 10.1021/jm060683e
70691656 73146 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 552 7 2 7 5.3 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016783 73146 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 552 7 2 7 5.3 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44562564 188539 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)no2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL510667 188539 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)no2)cc1 10.1016/j.bmcl.2008.07.079
54585374 60243 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 499 10 1 6 4.3 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760062 60243 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 499 10 1 6 4.3 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2011.02.046
16756184 91693 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242053 91693 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilizationAntagonist activity at rat MCHR1 expressed in HEK293 cells assessed as effect on calcium mobilization
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccccc2)CC1 10.1021/jm060381c
46172936 58938 0 None -6 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 368 5 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C4CC4)cc3)c2=O)cc1 nan
CHEMBL1703918 58938 0 None -6 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 368 5 0 5 4.6 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C4CC4)cc3)c2=O)cc1 nan
44394958 66556 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 461 11 2 5 4.8 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL186491 66556 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 461 11 2 5 4.8 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
20817762 76957 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 450 4 1 7 3.9 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL208340 76957 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 450 4 1 7 3.9 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
46835813 59629 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 394 6 0 7 3.9 COC(=O)c1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
CHEMBL1732922 59629 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 394 6 0 7 3.9 COC(=O)c1cnn(-c2ccc(C(C)C)cc2)c(=O)c1Oc1ccc(OC)cc1 nan
46835807 59674 0 None 2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 353 5 1 4 4.6 CC(C)c1ccc(-n2ncc(Cl)c(NCc3ccccc3)c2=O)cc1 nan
CHEMBL1734822 59674 0 None 2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 353 5 1 4 4.6 CC(C)c1ccc(-n2ncc(Cl)c(NCc3ccccc3)c2=O)cc1 nan
11994018 80594 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 592 6 0 8 5.3 CN(C)CC1CN(S(=O)(=O)c2ccccc2)c2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL215374 80594 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 592 6 0 8 5.3 CN(C)CC1CN(S(=O)(=O)c2ccccc2)c2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
11995445 82020 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)OC[C@@H](CN1CCCC1)O2 10.1021/jm060572f
CHEMBL217535 82020 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 479 4 0 7 5.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)OC[C@@H](CN1CCCC1)O2 10.1021/jm060572f
9887864 178495 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 411 7 1 6 4.8 CC(C)N(C)c1nc2cc(-c3noc(COCc4ccc(Cl)cc4)n3)ccc2[nH]1 10.1021/jm8016199
CHEMBL471651 178495 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 411 7 1 6 4.8 CC(C)N(C)c1nc2cc(-c3noc(COCc4ccc(Cl)cc4)n3)ccc2[nH]1 10.1021/jm8016199
52917998 60293 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760234 60293 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
23022422 74527 0 None 213 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1c(NC(=O)c2ccc(-c3ccccc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031733 74527 0 None 213 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1c(NC(=O)c2ccc(-c3ccccc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
10274635 68502 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 435 3 1 3 3.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3=O)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922268 68502 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 435 3 1 3 3.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3=O)C[C@@H]21 10.1016/j.bmcl.2011.09.110
10360874 64588 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL182261 64588 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.035
44394698 65894 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 346 6 2 5 2.9 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL184581 65894 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 346 6 2 5 2.9 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
1305 508 10 None 2 7 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
9934033 508 10 None 2 7 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
CHEMBL182150 508 10 None 2 7 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2009.09.003
57392824 67726 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914632 67726 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11548234 70837 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195635 70837 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
45485028 195480 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 383 6 2 6 3.0 COc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(C)cc(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
CHEMBL567950 195480 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 383 6 2 6 3.0 COc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(C)cc(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
18436066 74530 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 455 5 1 3 6.7 Cc1c(NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031736 74530 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 455 5 1 3 6.7 Cc1c(NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
11995443 79977 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)CC1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
CHEMBL214532 79977 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 453 4 0 7 4.5 CN(C)CC1COc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2O1 10.1021/jm060572f
16043291 79568 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 441 5 0 6 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL212758 79568 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 441 5 0 6 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
9910346 64386 0 None -12 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818901 64386 0 None -12 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
44417022 79971 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 4 2 6 5.5 CC(C)Nc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
CHEMBL214512 79971 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 435 4 2 6 5.5 CC(C)Nc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2[nH]1 10.1016/j.bmcl.2006.07.054
44417083 80483 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 526 5 0 7 7.2 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccc(OC(C)C)cc1 10.1016/j.bmcl.2006.07.054
CHEMBL215298 80483 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assayAntagonist activity against MCH1R expressed in CHO cells assessed as inhibition of MCH-induced EC80 thrombin response by luciferase reporter gene assay
ChEMBL 526 5 0 7 7.2 Cc1nc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1-c1ccc(OC(C)C)cc1 10.1016/j.bmcl.2006.07.054
54580457 60240 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760059 60240 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
23120550 194921 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL564106 194921 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
127033945 138411 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 491 7 0 8 3.2 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCN(C)CC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785118 138411 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 491 7 0 8 3.2 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCN(C)CC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
44394725 65805 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 365 6 2 6 2.7 Nc1ccc2cccc(OCCCNC(=O)c3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184191 65805 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 365 6 2 6 2.7 Nc1ccc2cccc(OCCCNC(=O)c3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
44405482 71492 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 395 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL196973 71492 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 395 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
57395049 68486 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3cccc(Cl)c23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
CHEMBL1922250 68486 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assayAntagonist activity at human MCHR1 expressed in Jurkat cells co-expressing apoaequorin assessed as inhibition of MCH-induced calcium mobilization by aequorin bioluminescence assay
ChEMBL 288 0 1 1 4.0 CC1c2c([nH]c3cccc(Cl)c23)CC2CCN(C)CC21 10.1016/j.bmcl.2011.09.110
46172917 59209 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 355 4 1 5 4.4 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(N)cc3)c2=O)cc1 nan
CHEMBL1716369 59209 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 355 4 1 5 4.4 CC(C)c1ccc(-n2ncc(Cl)c(Oc3ccc(N)cc3)c2=O)cc1 nan
11775505 141443 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(Cl)cc2o1 10.1021/jm060683e
CHEMBL387418 141443 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(Cl)cc2o1 10.1021/jm060683e
127031354 138562 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCOCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786662 138562 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 478 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCOCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
44562600 172550 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 480 5 1 4 5.8 Cc1c(-c2ccccc2)[nH]c(=O)n1C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL452087 172550 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 480 5 1 4 5.8 Cc1c(-c2ccccc2)[nH]c(=O)n1C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
49865679 15870 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 492 8 2 6 5.5 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223768 15870 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 492 8 2 6 5.5 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11419666 122025 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0490890
CHEMBL360142 122025 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0490890
16756752 142047 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)c(Cl)c4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL389129 142047 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)c(Cl)c4)cc3)CC2)c1 10.1021/jm060383x
10137322 148864 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 426 8 1 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL394569 148864 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 426 8 1 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
44410838 76693 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 432 4 1 5 4.8 Cn1c(=O)nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207296 76693 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 432 4 1 5 4.8 Cn1c(=O)nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
16756751 92865 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2ccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)cc2)cc1 10.1021/jm060383x
CHEMBL245229 92865 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assayAntagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2ccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)cc2)cc1 10.1021/jm060383x
44397128 123570 0 None -12 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 428 6 1 4 4.4 O=C(Cc1ccc(-c2ccccc2)cc1)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
CHEMBL363336 123570 0 None -12 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 428 6 1 4 4.4 O=C(Cc1ccc(-c2ccccc2)cc1)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
46172930 59703 0 None 1 2 Human 6.1 pIC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 414 5 0 5 4.9 COc1ccc(Oc2c(Br)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1735852 59703 0 None 1 2 Human 6.1 pIC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 414 5 0 5 4.9 COc1ccc(Oc2c(Br)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
11328029 76162 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL206081 76162 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
11634061 191745 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 463 7 1 4 4.5 O=C(COc1cccc(Cl)c1)NC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL520714 191745 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 463 7 1 4 4.5 O=C(COc1cccc(Cl)c1)NC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
70693792 73186 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 422 4 2 5 4.2 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017589 73186 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 422 4 2 5 4.2 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70687536 73188 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 512 6 2 6 5.2 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017591 73188 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 512 6 2 6 5.2 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
10388797 71400 0 None -4 3 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196667 71400 0 None -4 3 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
46835804 59149 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 366 6 1 6 3.6 COc1ccc(Oc2c(CO)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1713871 59149 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 366 6 1 6 3.6 COc1ccc(Oc2c(CO)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
127033095 138528 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1nc(-c2ccccc2)no1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3786352 138528 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 432 6 0 6 4.0 O=C(c1nc(-c2ccccc2)no1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
46835802 59092 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 361 5 0 6 4.0 COc1ccc(Oc2c(C#N)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1710499 59092 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 361 5 0 6 4.0 COc1ccc(Oc2c(C#N)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
49865869 15986 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 528 8 1 5 7.3 FC(F)(F)Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224080 15986 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 528 8 1 5 7.3 FC(F)(F)Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44397026 126636 0 None -15 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1ccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL365714 126636 0 None -15 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1ccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2005.05.023
44417946 82026 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 537 9 5 3 3.8 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2Cc2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL217557 82026 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 537 9 5 3 3.8 N=C(N)NCCC[C@@H](NC(=O)C1c2ccccc2Cc2ccccc21)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
58062359 125341 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 449 7 1 5 3.9 O=C(N[C@@H]1Cc2ccc(CN3CCCCCC3)cc2C1)c1ccc(OC[C@@H]2CCCO2)cn1 nan
CHEMBL3648385 125341 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 449 7 1 5 3.9 O=C(N[C@@H]1Cc2ccc(CN3CCCCCC3)cc2C1)c1ccc(OC[C@@H]2CCCO2)cn1 nan
44438740 93490 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 499 9 1 6 3.8 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL248296 93490 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 499 9 1 6 3.8 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
46892785 125348 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 474 7 1 4 4.8 O=C1c2ccc(OC[C@@H]3CCCO3)cc2CCN1[C@@H]1Cc2ccc(CNC3CCCCC3)cc2C1 nan
CHEMBL3648392 125348 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 474 7 1 4 4.8 O=C1c2ccc(OC[C@@H]3CCCO3)cc2CCN1[C@@H]1Cc2ccc(CNC3CCCCC3)cc2C1 nan
44418005 81968 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 504 10 6 4 2.9 COc1ccc2[nH]c(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2006.10.056
CHEMBL217257 81968 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 504 10 6 4 2.9 COc1ccc2[nH]c(C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2006.10.056
11974345 79915 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccc(F)cc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL214278 79915 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccc(F)cc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
11259253 82119 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Cl)cc2o1 10.1021/jm060683e
CHEMBL217789 82119 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Cl)cc2o1 10.1021/jm060683e
90469437 120744 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysis
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578244 120744 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysisAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ mobilization measured every 2 secs by fluorometric analysis
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
44394798 123853 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 391 5 1 6 3.6 CC(Cc1ccc2c(c1)OCO2)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
CHEMBL363909 123853 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 391 5 1 6 3.6 CC(Cc1ccc2c(c1)OCO2)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
11995136 80485 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 454 4 0 7 4.5 O=c1c2sc(-c3ccccc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
CHEMBL215307 80485 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 454 4 0 7 4.5 O=c1c2sc(-c3ccccc3)cc2ncn1-c1ccc2nc(CN3CCOCC3)ccc2c1 10.1021/jm060572f
49865708 15898 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 545 9 2 7 5.1 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(S(C)(=O)=O)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223828 15898 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 545 9 2 7 5.1 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(S(C)(=O)=O)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
45485061 197066 0 None 25 4 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 489 5 2 5 5.0 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL583014 197066 0 None 25 4 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 489 5 2 5 5.0 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
44442090 93713 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL249489 93713 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 367 6 2 5 4.8 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
10067783 65853 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 370 6 3 4 4.1 Nc1ccc2cccc(OCCCNC(=O)Nc3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184417 65853 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 370 6 3 4 4.1 Nc1ccc2cccc(OCCCNC(=O)Nc3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
44414451 168362 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 429 4 0 5 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL438792 168362 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 429 4 0 5 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
18436083 74525 0 None 81 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031731 74525 0 None 81 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11994136 141394 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 1 8 4.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CCOCC1)O2 10.1021/jm060572f
CHEMBL387085 141394 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 494 4 1 8 4.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1-c1ccc2c(c1)NCC(CN1CCOCC1)O2 10.1021/jm060572f
18436055 74510 0 None 251 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 441 5 1 3 6.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1021/jm201596h
CHEMBL2031716 74510 0 None 251 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 441 5 1 3 6.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1021/jm201596h
90666260 108869 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 564 7 1 5 6.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3F)CC2)c1 10.1039/C1MD00015B
CHEMBL3219269 108869 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 564 7 1 5 6.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3F)CC2)c1 10.1039/C1MD00015B
11662906 73117 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 475 6 2 7 3.8 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016728 73117 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 475 6 2 7 3.8 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
46172923 59058 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 332 3 1 5 3.5 O=c1c(Oc2ccc(O)cc2)c(Cl)cnn1-c1ccc(F)cc1 nan
CHEMBL1708907 59058 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 332 3 1 5 3.5 O=c1c(Oc2ccc(O)cc2)c(Cl)cnn1-c1ccc(F)cc1 nan
3114950 37521 29 None -2 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 318 3 0 4 2.8 O=[N+]([O-])c1cc(S(=O)(=O)N2CCCCCC2)ccc1Cl nan
CHEMBL1458112 37521 29 None -2 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 318 3 0 4 2.8 O=[N+]([O-])c1cc(S(=O)(=O)N2CCCCCC2)ccc1Cl nan
44562403 189226 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 413 5 1 5 4.4 O=C(NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)c1csc([N+](=O)[O-])c1 10.1016/j.bmcl.2008.07.079
CHEMBL516489 189226 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 413 5 1 5 4.4 O=C(NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)c1csc([N+](=O)[O-])c1 10.1016/j.bmcl.2008.07.079
45485003 196687 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(F)cc(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
CHEMBL576665 196687 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 403 6 2 5 3.5 Cc1cc(N(C)C)nc(N[C@H]2CC[C@@H](CNC(=O)c3cc(F)cc(F)c3)CC2)n1 10.1016/j.bmcl.2009.09.003
11583835 73120 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016731 73120 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
90666253 108862 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 466 6 1 5 5.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219262 108862 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 466 6 1 5 5.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C)cc3)CC2)c1 10.1039/C1MD00015B
44394607 123821 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 333 5 3 5 3.6 CC(CNc1ccc2[nH]ncc2c1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL363701 123821 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 333 5 3 5 3.6 CC(CNc1ccc2[nH]ncc2c1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11569300 82056 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Br)cc2o1 10.1021/jm060683e
CHEMBL217706 82056 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Br)cc2o1 10.1021/jm060683e
45382327 58923 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 372 5 0 6 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1OC nan
CHEMBL1703414 58923 0 None -1 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 372 5 0 6 4.0 COc1ccc(Oc2c(Cl)cnn(-c3ccc(C)cc3)c2=O)cc1OC nan
70687478 73139 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 440 5 2 6 4.0 Cc1nc(N2CCC(C)(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016777 73139 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 440 5 2 6 4.0 Cc1nc(N2CCC(C)(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11619850 75409 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm060683e
CHEMBL204828 75409 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm060683e
23657037 94075 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 415 6 2 6 4.6 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251701 94075 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 415 6 2 6 4.6 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
70693793 73192 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 496 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017595 73192 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 496 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44592256 188776 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 435 10 0 7 3.3 COc1cc(-n2ccnc(OCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL512873 188776 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 435 10 0 7 3.3 COc1cc(-n2ccnc(OCCc3ccccc3)c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
11973916 140952 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 436 6 1 7 2.8 COc1ccc2c(=O)cc(C(=O)NCC3CCN(Cc4ccc5c(c4)OCO5)C3)oc2c1 10.1021/jm060683e
CHEMBL384458 140952 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 436 6 1 7 2.8 COc1ccc2c(=O)cc(C(=O)NCC3CCN(Cc4ccc5c(c4)OCO5)C3)oc2c1 10.1021/jm060683e
54582014 60288 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760227 60288 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 478 9 1 4 5.0 COc1ccc(CCN2C[C@H](CNC(=O)c3cccc(Cl)c3)[C@@H](c3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2011.02.046
46835792 59332 0 None -23 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 378 4 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3cccc4ccccc34)c2=O)cc1 nan
CHEMBL1721648 59332 0 None -23 2 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 378 4 0 5 4.8 COc1ccc(Oc2c(Cl)cnn(-c3cccc4ccccc34)c2=O)cc1 nan
2042108 47705 8 None 1 3 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 404 6 0 5 5.8 Clc1ccc(-n2c(SC/C=C/c3ccccc3)nnc2-c2cccnc2)cc1 nan
CHEMBL1549996 47705 8 None 1 3 Human 5.1 pIC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 404 6 0 5 5.8 Clc1ccc(-n2c(SC/C=C/c3ccccc3)nnc2-c2cccnc2)cc1 nan
58062337 125342 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 10 2 4 3.7 O=C(N[C@@H]1Cc2ccc(CNCCC3CC3)cc2C1)c1ccc(OCC2CC2)cn1 nan
CHEMBL3648386 125342 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.Calcium Mobilization Assay: Calcium mobilization assay using MCHR1.
ChEMBL 405 10 2 4 3.7 O=C(N[C@@H]1Cc2ccc(CNCCC3CC3)cc2C1)c1ccc(OCC2CC2)cn1 nan
45271839 194862 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 382 4 1 4 5.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
CHEMBL563728 194862 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 382 4 1 4 5.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
44442139 94009 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 414 6 2 5 5.2 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251290 94009 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 414 6 2 5 5.2 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
49865680 15871 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 481 8 2 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223769 15871 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 481 8 2 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
49865739 15926 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(OC(F)(F)F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223885 15926 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(OC(F)(F)F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11649549 93491 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 539 9 1 6 4.7 O=C(NC1CCN(Cc2ccc(OCCCN3CCCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL248297 93491 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cellsAntagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
ChEMBL 539 9 1 6 4.7 O=C(NC1CCN(Cc2ccc(OCCCN3CCCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
70685396 73198 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 498 5 2 5 5.7 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017601 73198 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 498 5 2 5 5.7 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11776033 66821 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 230 4 1 3 3.4 CCCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL187702 66821 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 230 4 1 3 3.4 CCCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11995241 80134 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 508 5 0 6 7.0 CN(Cc1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1)c1ccccc1 10.1021/jm060572f
CHEMBL214891 80134 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCHR1 expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 508 5 0 6 7.0 CN(Cc1ccc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2n1)c1ccccc1 10.1021/jm060572f
1314 3657 18 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
9865843 3657 18 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
CHEMBL178707 3657 18 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
11190261 62898 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cn(CCN3CCCC3)nc2c1 10.1021/jm0490890
CHEMBL179091 62898 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1-mediated [Ca2+] release in human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cn(CCN3CCCC3)nc2c1 10.1021/jm0490890
11592199 15928 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(OC(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223887 15928 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(OC(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
20817846 138154 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 407 5 1 4 4.8 Cn1c(=O)cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL377884 138154 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPRInhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
ChEMBL 407 5 1 4 4.8 Cn1c(=O)cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
10456755 70739 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195351 70739 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44395019 65890 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184560 65890 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assayAntagonistic activity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using IP3 assay
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
70681197 73200 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 464 5 2 5 5.2 Cc1nc(N2CCC(O)(C(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017603 73200 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 464 5 2 5 5.2 Cc1nc(N2CCC(O)(C(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
10344176 66834 4 None 31 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL187756 66834 4 None 31 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
4033 1860 42 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1021/jm8016199
9826520 1860 42 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1021/jm8016199
CHEMBL214957 1860 42 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assayAntagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1021/jm8016199
44397194 66632 0 None -44 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186825 66632 0 None -44 2 Mouse 6.1 pIC50 = 6.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 458 7 1 5 4.4 COc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
44394638 123269 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 6 2 6 2.7 Nc1ccc2cccc(OCCNCc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL362309 123269 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 337 6 2 6 2.7 Nc1ccc2cccc(OCCNCc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
52917999 60305 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 504 8 1 5 4.6 COc1ccc([C@H]2CN(CCC3CCS(=O)(=O)CC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760247 60305 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 504 8 1 5 4.6 COc1ccc([C@H]2CN(CCC3CCS(=O)(=O)CC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
44430458 142267 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 511 4 0 6 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL389295 142267 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assayAntagonist activity at human MCHR1 by [35S]GTP-gamma-S binding assay
ChEMBL 511 4 0 6 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC2)C1 10.1016/j.bmcl.2007.02.012
70696356 74478 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 424 5 1 2 6.5 O=C(Nc1ccc2cc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031573 74478 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 424 5 1 2 6.5 O=C(Nc1ccc2cc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
70685337 73111 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 8 2 7 4.6 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016722 73111 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 545 8 2 7 4.6 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
49866088 16053 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 482 7 1 4 5.9 O=C1Cc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2N1 10.1016/j.bmcl.2010.07.086
CHEMBL1224388 16053 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 482 7 1 4 5.9 O=C1Cc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2N1 10.1016/j.bmcl.2010.07.086
11281523 81376 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 418 5 1 5 4.2 Cn1c(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2006.11.092
CHEMBL216430 81376 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 418 5 1 5 4.2 Cn1c(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2006.11.092
11153928 165216 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 404 5 2 4 4.2 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)[nH]c2c1 10.1016/j.bmcl.2006.11.092
CHEMBL424739 165216 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cellsInhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
ChEMBL 404 5 2 4 4.2 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)[nH]c2c1 10.1016/j.bmcl.2006.11.092
23593464 64356 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64356 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
18436075 74481 0 None 30 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031576 74481 0 None 30 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced [3H]arachidonic acid release after 16 hrs by liquid scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
57401509 67730 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914636 67730 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid releaseAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-stimulated arachidonic acid release
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
23593464 64356 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64356 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
11995028 140894 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 505 6 0 7 6.1 COC[C@H]1CCCN1Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2o1 10.1021/jm060814b
CHEMBL384147 140894 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 505 6 0 7 6.1 COC[C@H]1CCCN1Cc1cc2cc(-n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)ccc2o1 10.1021/jm060814b
45485077 195517 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(C)cc(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
CHEMBL568162 195517 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 367 5 2 5 3.3 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(C)cc(N(C)C)n3)CC2)c1 10.1016/j.bmcl.2009.09.003
11547939 160724 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 506 4 0 7 5.7 CN1CCN(Cc2cc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3s2)CC1 10.1021/jm060814b
CHEMBL412135 160724 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assayAntagonist activity against human MCH1 receptor stably-expressed in CHO cells by Gal4/Elk1-Luc reporter assay
ChEMBL 506 4 0 7 5.7 CN1CCN(Cc2cc3cc(-n4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)ccc3s2)CC1 10.1021/jm060814b
44414483 79308 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 461 5 0 6 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL211619 79308 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Activity at human MCH1R by GTPgammaS assayActivity at human MCH1R by GTPgammaS assay
ChEMBL 461 5 0 6 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
45267577 194284 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL559680 194284 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
11165058 154083 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 385 6 2 5 5.0 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(F)cc12 10.1016/j.bmcl.2007.05.034
CHEMBL399367 154083 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 385 6 2 5 5.0 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(F)cc12 10.1016/j.bmcl.2007.05.034
11633862 178578 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 453 8 1 5 4.3 COc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL472195 178578 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 453 8 1 5 4.3 COc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
10083869 65228 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
10083869 65228 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL183159 65228 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65228 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44397476 67073 0 None -29 2 Mouse 7.1 pIC50 = 7.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 412 6 1 6 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
CHEMBL188937 67073 0 None -29 2 Mouse 7.1 pIC50 = 7.1 Functional
Inhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assayInhibitory concentration required for functional antagonism of MCH mediated Ca+2 release competing human IMR32 cells receptor in a FLIPRTM based assay
ChEMBL 412 6 1 6 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
44417981 165417 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1ccc2ccccc2n1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL425269 165417 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1ccc2ccccc2n1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
54582961 60301 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 519 10 1 5 6.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760243 60301 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 519 10 1 5 6.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
21939767 64352 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818777 64352 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation countingAntagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
70689519 73095 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 481 6 1 6 3.9 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016706 73095 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assayAntagonist activity at human MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH peptide mediated response measuring [3H]inositol phosphate production by IP3-SPA-YSI assay
ChEMBL 481 6 1 6 3.9 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70689596 73201 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 464 6 2 5 5.4 CCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017604 73201 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assayAntagonist activity at human recombinant MCHR1 expressed in CHO-K1 cells assessed as inhibition of MCH-induced IP3 accumulation response preincubated for 10 mins prior MCH peptide-stimulation measured after 45 mins by IP3-SPA-YSI assay
ChEMBL 464 6 2 5 5.4 CCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
44394596 65858 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 377 3 1 6 2.8 Nc1ccc2cccc(O[C@H]3CCN(C(=O)c4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL184437 65858 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate readerConcentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
ChEMBL 377 3 1 6 2.8 Nc1ccc2cccc(O[C@H]3CCN(C(=O)c4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11554989 178475 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL471514 178475 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTPgammaS accumulation
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
10070680 71750 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 418 4 1 4 5.7 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL197797 71750 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assayInhibition of melanin concentrating hormone receptor 1 mediated [Ca2+] release in IMR-32 cells in Ca+2 release cell assay
ChEMBL 418 4 1 4 5.7 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
56597990 138642 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 451 6 0 7 2.5 CN1CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2F)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3787582 138642 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assayAntagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay
ChEMBL 451 6 0 7 2.5 CN1CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2F)CC1 10.1021/acs.jmedchem.5b01654
11526824 15929 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 549 9 2 5 6.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223888 15929 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 549 9 2 5 6.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
44405557 132217 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 489 5 1 8 4.6 O=C(c1cccnc1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL369986 132217 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cellsFunctional antagonism of MCH-mediated calcium release by FLIPR using human MCHr1 from neuronal IMR32 cells
ChEMBL 489 5 1 8 4.6 O=C(c1cccnc1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
1017287 55716 8 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 369 7 2 3 4.9 CC(C)(CO)NCc1c(OCc2ccc(Cl)cc2)ccc2ccccc12 nan
CHEMBL1568072 55716 8 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 369 7 2 3 4.9 CC(C)(CO)NCc1c(OCc2ccc(Cl)cc2)ccc2ccccc12 nan
CHEMBL1624689 55716 8 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 369 7 2 3 4.9 CC(C)(CO)NCc1c(OCc2ccc(Cl)cc2)ccc2ccccc12 nan
45268470 194611 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL562136 194611 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
45268465 194876 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 446 5 1 6 4.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(S(C)(=O)=O)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563836 194876 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at human MCH1 receptor expressed in CHO cells assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 446 5 1 6 4.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(S(C)(=O)=O)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
54585861 60289 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 482 8 1 3 5.7 COc1ccc([C@H]2CN(CCc3ccc(Cl)cc3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760228 60289 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHR1 by aequorin bioluminescence assayAntagonist activity at MCHR1 by aequorin bioluminescence assay
ChEMBL 482 8 1 3 5.7 COc1ccc([C@H]2CN(CCc3ccc(Cl)cc3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
2729502 80625 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
CHEMBL215388 80625 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
46172925 59143 0 None 1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 360 4 0 5 4.1 COc1cc(F)ccc1Oc1c(Cl)cnn(-c2ccc(C)cc2)c1=O nan
CHEMBL1713683 59143 0 None 1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 360 4 0 5 4.1 COc1cc(F)ccc1Oc1c(Cl)cnn(-c2ccc(C)cc2)c1=O nan
44417972 141049 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 491 9 5 4 3.6 N=C(N)NCCC[C@@H](NC(=O)c1csc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL385036 141049 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 491 9 5 4 3.6 N=C(N)NCCC[C@@H](NC(=O)c1csc2ccccc12)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
90666267 108877 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 524 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc(C)c(C)n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219276 108877 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assayAntagonist activity at MCHR1 (unknown origin) assessed as IP3 levels by cell-based functional assay
ChEMBL 524 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc(C)c(C)n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
49865927 16003 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 511 9 2 5 6.2 O=C(Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1)C1CC1 10.1016/j.bmcl.2010.07.086
CHEMBL1224152 16003 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 511 9 2 5 6.2 O=C(Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1)C1CC1 10.1016/j.bmcl.2010.07.086
44417952 141198 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cnc2ccccc2c1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
CHEMBL385876 141198 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 486 9 5 4 2.9 N=C(N)NCCC[C@@H](NC(=O)c1cnc2ccccc2c1)C(=O)NCc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2006.10.056
11973800 81146 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2cccc(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL216225 81146 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assayAntagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2cccc(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
44442071 154065 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 380 6 2 5 4.9 CN(C)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL399244 154065 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulationAntagonist activity at human MCHR1 expressed in HEK293 cells assessed as [35S]GTP-gamma-S accumulation
ChEMBL 380 6 2 5 4.9 CN(C)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
49865871 15988 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 471 9 2 5 6.3 CCNc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224082 15988 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 471 9 2 5 6.3 CCNc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
49866086 16051 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 499 7 2 5 4.7 CC(=O)Nc1cccc(C2CCN(CCNC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224386 16051 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assayAntagonist activity at human recombinant MCHR1 expressed in CHOK1 cells assessed as reduction in [3H]inositol phosphate levels by scintillation proximity assay
ChEMBL 499 7 2 5 4.7 CC(=O)Nc1cccc(C2CCN(CCNC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11634230 69816 0 None 851 2 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL194046 69816 0 None 851 2 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositolInhibitory concentration against 10 nM MCH-induced IP3 accumulation in CHO-K1 cells expressing human MCH1R after incubation with [3H]myo-inositol
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
46835794 59211 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 350 5 0 5 4.5 COc1ccc(Oc2c(C)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
CHEMBL1716381 59211 0 None -1 2 Human 5.0 pIC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]PUBCHEM_BIOASSAY: Late-stage fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1861, AID1880, AID1952, AID2148, AID2251, AID2257, AID485339]
ChEMBL 350 5 0 5 4.5 COc1ccc(Oc2c(C)cnn(-c3ccc(C(C)C)cc3)c2=O)cc1 nan
1746683 31069 11 None - 1 Human 5.0 pIC50 = 5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 508 7 1 3 5.1 O=P(Cc1cc(Br)cc(Br)c1OCCO)(c1ccccc1)c1ccccc1 nan
CHEMBL1401638 31069 11 None - 1 Human 5.0 pIC50 = 5 Functional
PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]PUBCHEM_BIOASSAY: Fluorescence-based counterscreen for antagonists of the G-protein coupled receptor 7 (GPR7): cell-based high throughput dose response assay to identify antagonists of the melanin-concentrating hormone receptor 1 (MCHR1). (Class of assay: confirmatory) [Related pubchem assays: 1880 (Summary AID.), 2148 (Screening assay (MCHR1 antagonists).), 1952 (Screening assay (GPR7 antagonists).), 1861 (Screening assay (GPR7 antagonists).)]
ChEMBL 508 7 1 3 5.1 O=P(Cc1cc(Br)cc(Br)c1OCCO)(c1ccccc1)c1ccccc1 nan
11520239 3562 4 None - 1 Human 9.2 pKd = 9.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2009.09.003
1313 3562 4 None - 1 Human 9.2 pKd = 9.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2009.09.003
CHEMBL185271 3562 4 None - 1 Human 9.2 pKd = 9.2 Functional
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assayAntagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2009.09.003
11236807 81140 0 None -2 3 Human 8.0 pKd = 8 Functional
Antagonist activity at MCHR1 by Schild experimentAntagonist activity at MCHR1 by Schild experiment
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81140 0 None -2 3 Human 8.0 pKd = 8 Functional
Antagonist activity at MCHR1 by Schild experimentAntagonist activity at MCHR1 by Schild experiment
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
16037921 139630 0 None - 0 Human 9.0 pKi = 9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 549 9 1 3 7.9 N#Cc1cccc(-c2ccc(C(CCC(=O)Nc3ccc(F)c(F)c3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL380371 139630 0 None - 0 Human 9.0 pKi = 9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 549 9 1 3 7.9 N#Cc1cccc(-c2ccc(C(CCC(=O)Nc3ccc(F)c(F)c3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52945130 16853 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 541 7 2 5 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254563 16853 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 541 7 2 5 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
44412852 137862 0 None - 0 Human 8.9 pKi = 8.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 459 7 2 3 6.0 N#Cc1cccc(-c2ccc(C(CCC(=O)Nc3ccc(F)c(F)c3)C3CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL377321 137862 0 None - 0 Human 8.9 pKi = 8.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 459 7 2 3 6.0 N#Cc1cccc(-c2ccc(C(CCC(=O)Nc3ccc(F)c(F)c3)C3CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52943873 16838 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 529 9 2 5 5.3 CC(C)N(CCO)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254400 16838 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 529 9 2 5 5.3 CC(C)N(CCO)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
52945087 16839 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 543 9 2 5 5.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.ejmech.2010.07.011
CHEMBL1254401 16839 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 543 9 2 5 5.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.ejmech.2010.07.011
11191034 79439 0 None - 0 Human 8.8 pKi = 8.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 490 3 2 3 6.3 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCNCC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL212256 79439 0 None - 0 Human 8.8 pKi = 8.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 490 3 2 3 6.3 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCNCC4)cc2)c1 10.1016/j.bmcl.2006.04.062
52942885 16845 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 485 7 2 4 5.6 CC(C)NCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254481 16845 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 485 7 2 4 5.6 CC(C)NCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
10230947 72222 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 548 10 1 4 6.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL199274 72222 0 None - 0 Human 8.0 pKi = 8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 548 10 1 4 6.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
44413473 96810 0 None - 0 Human 8.0 pKi = 8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 4 1 4 7.3 Cn1cccc1C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL268938 96810 0 None - 0 Human 8.0 pKi = 8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 4 1 4 7.3 Cn1cccc1C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44413297 137871 0 None - 0 Human 8.0 pKi = 8.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 531 5 1 4 7.0 N#Cc1cncc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL377372 137871 0 None - 0 Human 8.0 pKi = 8.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 531 5 1 4 7.0 N#Cc1cncc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44413474 166894 0 None - 1 Human 8.0 pKi = 8.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 5 1 3 8.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(Cc3ccccc3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL429895 166894 0 None - 1 Human 8.0 pKi = 8.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 5 1 3 8.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(Cc3ccccc3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
52948758 16844 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1ccc(F)cc1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254480 16844 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1ccc(F)cc1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52945129 16852 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 7 2 4 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254562 16852 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 7 2 4 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
52950112 16879 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 496 6 1 4 5.0 N#Cc1cccc([C@]23CCC(N(CCN4CCOCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254797 16879 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 496 6 1 4 5.0 N#Cc1cccc([C@]23CCC(N(CCN4CCOCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44417918 81121 0 None - 0 Human 4.0 pKi = 4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 463 7 1 3 3.7 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CNCC(F)(F)F)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL216103 81121 0 None - 0 Human 4.0 pKi = 4 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 463 7 1 3 3.7 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CNCC(F)(F)F)ccc2C1 10.1016/j.bmcl.2006.10.052
44417928 95957 0 None - 0 Human 7.0 pKi = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 5 0 3 4.8 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cc2)C3)CC1 10.1016/j.bmcl.2006.10.053
CHEMBL261964 95957 0 None - 0 Human 7.0 pKi = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 5 0 3 4.8 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cc2)C3)CC1 10.1016/j.bmcl.2006.10.053
23626228 88881 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 511 7 2 5 4.8 NCc1ncc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL236889 88881 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 511 7 2 5 4.8 NCc1ncc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
44417919 80446 0 None - 1 Human 8.0 pKi = 8.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cc3)cn1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL215278 80446 0 None - 1 Human 8.0 pKi = 8.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cc3)cn1)C2 10.1016/j.bmcl.2006.10.053
44417905 82046 0 None - 1 Human 8.0 pKi = 8.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL217637 82046 0 None - 1 Human 8.0 pKi = 8.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
52949912 16832 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 514 9 1 3 6.4 CC(C)N(CCF)CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254328 16832 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 514 9 1 3 6.4 CC(C)N(CCF)CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
44424263 85346 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 431 6 1 3 5.6 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccco2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL229406 85346 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 431 6 1 3 5.6 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccco2)CC1 10.1016/j.ejmech.2010.07.011
44434153 144697 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@H]1CC[C@@]2(c3cnc(CN)s3)C[C@@H]12 10.1016/j.bmcl.2007.06.048
CHEMBL391275 144697 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@H]1CC[C@@]2(c3cnc(CN)s3)C[C@@H]12 10.1016/j.bmcl.2007.06.048
44417993 81339 0 None - 1 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccc3)cn1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216406 81339 0 None - 1 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccc3)cn1)C2 10.1016/j.bmcl.2006.10.053
10303281 133030 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 10 2 5 5.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL371099 133030 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 10 2 5 5.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
44417922 82127 0 None - 1 Human 7.9 pKi = 7.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cc3)nc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL217820 82127 0 None - 1 Human 7.9 pKi = 7.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cc3)nc1)C2 10.1016/j.bmcl.2006.10.053
20609028 138353 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 579 7 1 3 8.6 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL378269 138353 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 579 7 1 3 8.6 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
11592317 138982 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 582 5 1 4 6.9 CC(C)S(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL379521 138982 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 582 5 1 4 6.9 CC(C)S(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44418004 168245 0 None - 0 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 500 5 1 3 4.3 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCN(C(N)=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.053
CHEMBL437728 168245 0 None - 0 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 500 5 1 3 4.3 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCN(C(N)=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.053
11236807 81140 0 None -2 3 Human 7.9 pKi = 7.9 Functional
Activity at human MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at human MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81140 0 None -2 3 Human 7.9 pKi = 7.9 Functional
Activity at human MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at human MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11236807 81140 0 None 1 3 Rat 7.9 pKi = 7.9 Functional
Activity at rat MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at rat MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81140 0 None 1 3 Rat 7.9 pKi = 7.9 Functional
Activity at rat MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at rat MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
52947407 16813 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 10 1 3 7.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN(C)C)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254148 16813 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 10 1 3 7.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN(C)C)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
11634329 141756 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
CHEMBL388524 141756 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
11634329 141756 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmcl.2007.06.048
CHEMBL388524 141756 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmcl.2007.06.048
20608975 77395 0 None - 0 Human 7.9 pKi = 7.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 513 7 1 3 7.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209089 77395 0 None - 0 Human 7.9 pKi = 7.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 513 7 1 3 7.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44434151 89170 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cnc(CN)s3)CC12 10.1016/j.bmcl.2007.06.048
CHEMBL237531 89170 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cnc(CN)s3)CC12 10.1016/j.bmcl.2007.06.048
10166088 72050 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 548 8 1 4 6.3 CC(C)(c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CCCC1 10.1016/j.bmcl.2005.08.043
CHEMBL198724 72050 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 548 8 1 4 6.3 CC(C)(c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CCCC1 10.1016/j.bmcl.2005.08.043
44413138 138352 0 None - 1 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 6 1 4 7.1 CS(=O)(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL378261 138352 0 None - 1 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 6 1 4 7.1 CS(=O)(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
52947140 16921 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 444 6 2 4 4.0 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1255054 16921 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 444 6 2 4 4.0 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44413326 79438 0 None - 1 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 469 5 1 4 6.3 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C#N)ccc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL212254 79438 0 None - 1 Human 6.9 pKi = 6.9 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 469 5 1 4 6.3 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C#N)ccc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
52946021 16757 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 688 14 2 8 6.8 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(OCOc5ccccc5)c(OCOc5ccccc5)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253628 16757 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 688 14 2 8 6.8 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(OCOc5ccccc5)c(OCOc5ccccc5)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
11236807 81140 0 None -1 3 Mouse 7.9 pKi = 7.9 Functional
Activity at mouse MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at mouse MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81140 0 None -1 3 Mouse 7.9 pKi = 7.9 Functional
Activity at mouse MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assayActivity at mouse MCHR1 expressed in CHOK1-Gqi cells assessed as inhibition of MCH-induced calcium ion release by FLIPR assay
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11156790 77564 0 None - 0 Human 7.9 pKi = 7.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 527 8 2 4 6.8 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209510 77564 0 None - 0 Human 7.9 pKi = 7.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 527 8 2 4 6.8 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
16659197 96622 0 None - 1 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccn3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL267320 96622 0 None - 1 Human 6.9 pKi = 6.9 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccn3)cc1)C2 10.1016/j.bmcl.2006.10.053
10311798 79564 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 541 7 2 3 6.9 O=C(CNC1(c2ccc(-c3cc(F)cc(F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212750 79564 0 None - 0 Human 6.9 pKi = 6.9 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 541 7 2 3 6.9 O=C(CNC1(c2ccc(-c3cc(F)cc(F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
10128764 77890 0 None - 0 Human 5.8 pKi = 5.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3ccc(Cl)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210857 77890 0 None - 0 Human 5.8 pKi = 5.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3ccc(Cl)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44417901 79890 0 None - 0 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 471 5 1 3 4.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2006.10.053
CHEMBL214178 79890 0 None - 0 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 471 5 1 3 4.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2006.10.053
44417895 165291 0 None - 1 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 6 0 3 5.2 CN(C)C(=O)[C@@H]1CCCN1Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL424895 165291 0 None - 1 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 6 0 3 5.2 CN(C)C(=O)[C@@H]1CCCN1Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
44424260 85337 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 443 6 1 4 4.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cncnc2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL229348 85337 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 443 6 1 4 4.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cncnc2)CC1 10.1016/j.ejmech.2010.07.011
44417967 81871 0 None - 1 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 459 7 0 4 4.5 O=C(c1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
CHEMBL217196 81871 0 None - 1 Human 6.8 pKi = 6.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 459 7 0 4 4.5 O=C(c1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
10143980 72121 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 9 2 5 4.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL198945 72121 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 9 2 5 4.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
52943978 16742 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 7 1 4 5.8 COC1CCN(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253196 16742 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 7 1 4 5.8 COC1CCN(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
52947331 16785 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cc(F)cc(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253875 16785 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cc(F)cc(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52942540 16815 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 590 8 1 4 5.6 CN(C)Cc1cccc([C@]23CCC(N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254150 16815 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 590 8 1 4 5.6 CN(C)Cc1cccc([C@]23CCC(N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52943913 16851 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCC[C@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254561 16851 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCC[C@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52949472 16868 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 502 6 1 3 6.6 N#Cc1cccc([C@]23CCC(N(CCN4C=CC=CC=C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254714 16868 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 502 6 1 3 6.6 N#Cc1cccc([C@]23CCC(N(CCN4C=CC=CC=C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52945155 54676 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 509 6 1 2 6.3 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCCC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254636 54676 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 509 6 1 2 6.3 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCCC1 10.1016/j.ejmech.2010.07.011
CHEMBL1615721 54676 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 509 6 1 2 6.3 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCCC1 10.1016/j.ejmech.2010.07.011
44413475 77639 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 8 1 4 7.4 CCN(CC)CCN1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
CHEMBL209754 77639 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 8 1 4 7.4 CCN(CC)CCN1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
11497179 79343 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 512 5 1 3 7.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(Cl)c(Cl)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211820 79343 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 512 5 1 3 7.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(Cl)c(Cl)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417950 172175 0 None - 0 Human 7.8 pKi = 7.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 459 8 0 3 5.1 O=C1c2cc(CCc3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL450942 172175 0 None - 0 Human 7.8 pKi = 7.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 459 8 0 3 5.1 O=C1c2cc(CCc3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
44413470 77973 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 533 5 2 4 5.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC(N)=O)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211069 77973 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 533 5 2 4 5.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC(N)=O)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417923 82155 0 None - 0 Human 4.8 pKi = 4.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 451 6 0 4 2.9 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCOCC3)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL217875 82155 0 None - 0 Human 4.8 pKi = 4.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 451 6 0 4 2.9 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCOCC3)ccc2C1 10.1016/j.bmcl.2006.10.052
44405437 71589 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 492 7 1 3 6.7 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL197280 71589 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 492 7 1 3 6.7 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
44405417 72194 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 510 7 1 3 6.5 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL199179 72194 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 510 7 1 3 6.5 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
44405461 71497 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 8 2 5 5.1 C[C@@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL197005 71497 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 8 2 5 5.1 C[C@@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
52941493 54678 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 495 6 1 2 5.9 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254564 54678 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 495 6 1 2 5.9 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCC1 10.1016/j.ejmech.2010.07.011
CHEMBL1615759 54678 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 495 6 1 2 5.9 C[N+]1(CCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CCCC1 10.1016/j.ejmech.2010.07.011
10196608 76943 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 564 7 2 4 6.8 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL208275 76943 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 564 7 2 4 6.8 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10312244 138970 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 594 7 1 4 7.7 CN(CC(=O)Nc1ccc(Cl)c(C(F)(F)F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL379489 138970 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 594 7 1 4 7.7 CN(CC(=O)Nc1ccc(Cl)c(C(F)(F)F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
11691468 168767 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 477 7 2 5 5.0 NCc1cnc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
CHEMBL441886 168767 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 477 7 2 5 5.0 NCc1cnc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
16659239 141339 0 None - 0 Human 4.8 pKi = 4.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 492 6 0 4 2.7 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N2CCN(CCc4ccc(F)cc4)CC2=O)C3)CC1 10.1016/j.bmcl.2006.10.052
CHEMBL386717 141339 0 None - 0 Human 4.8 pKi = 4.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 492 6 0 4 2.7 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N2CCN(CCc4ccc(F)cc4)CC2=O)C3)CC1 10.1016/j.bmcl.2006.10.052
15982955 93202 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 487 9 0 6 4.9 COc1cc(N2CC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL246794 93202 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 487 9 0 6 4.9 COc1cc(N2CC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
10239929 77733 0 None - 0 Human 5.8 pKi = 5.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3c(Cl)cccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210255 77733 0 None - 0 Human 5.8 pKi = 5.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3c(Cl)cccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
11692382 168797 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@@]23CC[C@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@@H]2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL442084 168797 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@@]23CC[C@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@@H]2C3)s1 10.1016/j.bmcl.2007.06.048
44434148 89073 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237318 89073 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
52944859 16778 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 592 11 2 4 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CNS(C)(=O)=O)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1253795 16778 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 592 11 2 4 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CNS(C)(=O)=O)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
44434155 168818 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN(CCCN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@H]2CC[C@@]3(c4cnc(CN)s4)C[C@@H]23)[C@H](C)CN1 10.1016/j.bmcl.2007.06.048
CHEMBL442244 168818 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN(CCCN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@H]2CC[C@@]3(c4cnc(CN)s4)C[C@@H]23)[C@H](C)CN1 10.1016/j.bmcl.2007.06.048
44413428 78192 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 522 5 2 4 6.8 Oc1ccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)cn1 10.1016/j.bmcl.2006.04.062
CHEMBL211232 78192 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 522 5 2 4 6.8 Oc1ccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)cn1 10.1016/j.bmcl.2006.04.062
10196214 77762 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3ccccc3F)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210344 77762 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3ccccc3F)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44405439 72128 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 9 2 5 5.5 C[C@@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL198969 72128 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 9 2 5 5.5 C[C@@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
10129058 138123 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 7 1 4 7.2 CN(CC(=O)Nc1ccc(F)c(C(F)(F)F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL377738 138123 0 None - 0 Human 7.8 pKi = 7.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 7 1 4 7.2 CN(CC(=O)Nc1ccc(F)c(C(F)(F)F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
44417916 81711 0 None - 1 Human 7.8 pKi = 7.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cn3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216741 81711 0 None - 1 Human 7.8 pKi = 7.8 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 433 5 0 3 5.1 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(Cl)cn3)cc1)C2 10.1016/j.bmcl.2006.10.053
10239448 77791 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3ccc(F)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210436 77791 0 None - 0 Human 6.8 pKi = 6.8 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3ccc(F)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
52944540 16869 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 571 5 2 3 6.1 CNC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254715 16869 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 571 5 2 3 6.1 CNC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
44417913 81163 0 None - 1 Human 6.7 pKi = 6.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 417 5 0 3 4.6 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)nc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216314 81163 0 None - 1 Human 6.7 pKi = 6.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 417 5 0 3 4.6 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)nc1)C2 10.1016/j.bmcl.2006.10.053
10143421 71989 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 534 9 1 4 5.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL198483 71989 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 534 9 1 4 5.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
44434149 148110 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 568 8 3 6 4.8 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1ccc(F)c(C(F)(F)F)c1)[C@@H]1CC[C@]2(c3cnc(CN)s3)CC12 10.1016/j.bmcl.2007.06.048
CHEMBL393959 148110 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 568 8 3 6 4.8 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1ccc(F)c(C(F)(F)F)c1)[C@@H]1CC[C@]2(c3cnc(CN)s3)CC12 10.1016/j.bmcl.2007.06.048
20608974 79457 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 499 7 1 3 6.8 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C4CCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212330 79457 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 499 7 1 3 6.8 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C4CCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
17989329 80654 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 458 8 0 6 4.8 COc1cc(N2C(=O)c3ccc(Oc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL215508 80654 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 458 8 0 6 4.8 COc1cc(N2C(=O)c3ccc(Oc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
20608989 77816 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 1 4 5.2 CS(=O)(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL210532 77816 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 1 4 5.2 CS(=O)(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
44412960 79544 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 10 1 4 5.8 CCN(CC)S(=O)(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL212671 79544 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 10 1 4 5.8 CCN(CC)S(=O)(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
10174984 77740 0 None - 0 Human 8.7 pKi = 8.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 7 1 4 7.4 N#Cc1cccc(-c2ccc(C3(OCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210274 77740 0 None - 0 Human 8.7 pKi = 8.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 7 1 4 7.4 N#Cc1cccc(-c2ccc(C3(OCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52945048 16830 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1cccc(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254326 16830 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1cccc(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52948916 16833 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254329 16833 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
10209344 122725 0 None - 0 Human 8.6 pKi = 8.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 546 6 2 3 7.6 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL361392 122725 0 None - 0 Human 8.6 pKi = 8.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 546 6 2 3 7.6 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10165503 125419 0 None - 0 Human 8.6 pKi = 8.6 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 532 5 1 3 8.0 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cc(Cl)cc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL364871 125419 0 None - 0 Human 8.6 pKi = 8.6 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 532 5 1 3 8.0 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cc(Cl)cc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.062
52946184 16821 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 503 9 1 5 5.9 CC(C)N(CCN(C(=O)Nc1cccc([N+](=O)[O-])c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254240 16821 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 503 9 1 5 5.9 CC(C)N(CCN(C(=O)Nc1cccc([N+](=O)[O-])c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52942685 16843 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254479 16843 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52946082 16786 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253876 16786 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52941054 16922 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1255055 16922 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
11317465 137660 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 473 6 3 4 5.7 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL376976 137660 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 473 6 3 4 5.7 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44413472 138149 0 None - 1 Human 7.7 pKi = 7.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 586 4 1 4 8.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)c4cccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL377864 138149 0 None - 1 Human 7.7 pKi = 7.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 586 4 1 4 8.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)c4cccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417926 80696 0 None - 1 Human 7.7 pKi = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 417 5 0 3 4.6 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cn1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL215660 80696 0 None - 1 Human 7.7 pKi = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 417 5 0 3 4.6 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cn1)C2 10.1016/j.bmcl.2006.10.053
52941272 16797 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 584 10 2 4 6.5 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN4CC[C@H](O)C4)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1253963 16797 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 584 10 2 4 6.5 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN4CC[C@H](O)C4)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52947141 16924 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 7 1 4 5.2 CCS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1255057 16924 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 7 1 4 5.2 CCS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
23573799 72039 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 534 9 1 4 6.0 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL198689 72039 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 534 9 1 4 6.0 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
10196316 77815 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 533 8 2 4 6.4 O=Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210531 77815 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 533 8 2 4 6.4 O=Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52943353 16867 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 6 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCCC(O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254713 16867 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 6 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCCC(O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
70681299 73599 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.ejmech.2010.07.011
CHEMBL2021397 73599 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.ejmech.2010.07.011
10218547 77367 0 None - 0 Human 5.7 pKi = 5.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3ccc(Cl)c(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL208970 77367 0 None - 0 Human 5.7 pKi = 5.7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3ccc(Cl)c(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44434143 88880 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 496 7 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2007.06.048
CHEMBL236888 88880 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 496 7 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2007.06.048
11657090 79305 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 575 5 1 3 7.6 CCN(CC)C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL211615 79305 0 None - 0 Human 7.7 pKi = 7.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 575 5 1 3 7.6 CCN(CC)C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44417909 157159 0 None - 0 Human 7.7 pKi = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 475 7 1 5 4.0 O=C(Nc1cccc(F)c1)c1cc2n(n1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
CHEMBL408198 157159 0 None - 0 Human 7.7 pKi = 7.7 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 475 7 1 5 4.0 O=C(Nc1cccc(F)c1)c1cc2n(n1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
11628547 138728 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 5 1 3 7.5 CCN(CC)C(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
CHEMBL379060 138728 0 None - 0 Human 6.7 pKi = 6.7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 5 1 3 7.5 CCN(CC)C(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
44417969 81151 0 None - 0 Human 6.6 pKi = 6.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 445 7 0 3 4.9 O=C1c2cc(Cc3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL216242 81151 0 None - 0 Human 6.6 pKi = 6.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 445 7 0 3 4.9 O=C1c2cc(Cc3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
44405435 72127 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 9 2 5 5.5 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL198968 72127 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 9 2 5 5.5 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
10218604 138324 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 7 2 4 7.4 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL378180 138324 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 580 7 2 4 7.4 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44417953 81159 0 None - 0 Human 7.6 pKi = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 431 6 0 3 5.0 O=C1c2cc(-c3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL216280 81159 0 None - 0 Human 7.6 pKi = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 431 6 0 3 5.0 O=C1c2cc(-c3ccc(F)cc3)cn2CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2006.10.096
52943912 16850 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 7 1 4 5.7 CC(=O)C1CCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254560 16850 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 7 1 4 5.7 CC(=O)C1CCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
44417904 79952 0 None - 1 Human 7.6 pKi = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 487 7 0 3 4.6 CN(CC(=O)N(C)C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL214432 79952 0 None - 1 Human 7.6 pKi = 7.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 487 7 0 3 4.6 CN(CC(=O)N(C)C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
10174522 139138 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 505 7 2 3 6.6 O=C(CNC1(c2ccc(-c3ccccc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL379797 139138 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 505 7 2 3 6.6 O=C(CNC1(c2ccc(-c3ccccc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44417900 81111 0 None - 0 Human 5.6 pKi = 5.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccncc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216050 81111 0 None - 0 Human 5.6 pKi = 5.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccncc3)cc1)C2 10.1016/j.bmcl.2006.10.053
44417933 140966 0 None - 0 Human 5.6 pKi = 5.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(C(F)(F)F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL384546 140966 0 None - 0 Human 5.6 pKi = 5.6 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(C(F)(F)F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
20608996 77387 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 517 7 1 4 6.4 CCOC(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL209059 77387 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 517 7 1 4 6.4 CCOC(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
20608991 77385 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 445 6 2 3 5.5 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209050 77385 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 445 6 2 3 5.5 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCNCC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52946062 16779 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 592 6 1 4 5.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253796 16779 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 592 6 1 4 5.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
44412837 76907 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 537 8 1 4 5.7 CS(=O)(=O)N1CCC(C(CCC(=O)Nc2ccc(F)c(F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL208081 76907 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 537 8 1 4 5.7 CS(=O)(=O)N1CCC(C(CCC(=O)Nc2ccc(F)c(F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
11433168 138151 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 8 1 3 9.0 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)cc(Cl)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL377874 138151 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 8 1 3 9.0 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)cc(Cl)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44413309 138366 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 6 1 3 7.8 N#CCc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL378310 138366 0 None - 0 Human 7.6 pKi = 7.6 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 6 1 3 7.8 N#CCc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
52949812 16803 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 478 6 2 4 4.6 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254055 16803 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 478 6 2 4 4.6 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
10165656 71459 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 536 8 2 5 4.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL196864 71459 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 536 8 2 5 4.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
52943485 16923 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 11 1 4 7.3 CCO/N=C/c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1255056 16923 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 11 1 4 7.3 CCO/N=C/c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
10129026 77886 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.6 O=C(CNC1(c2ccc(-c3cccc(C(F)(F)F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210818 77886 0 None - 0 Human 6.6 pKi = 6.6 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.6 O=C(CNC1(c2ccc(-c3cccc(C(F)(F)F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44405399 135461 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 476 7 1 3 6.1 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL373165 135461 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 476 7 1 3 6.1 N#Cc1cccc(-c2ccc(CN(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
52943712 16805 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.5 CS(=O)(=O)N1CCCCC1CN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254057 16805 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.5 CS(=O)(=O)N1CCCCC1CN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
44592215 188234 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CCC(N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1021/jm8016199
CHEMBL506480 188234 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CCC(N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1021/jm8016199
10196098 77654 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 514 7 2 4 6.0 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4cc(F)cc(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209828 77654 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 514 7 2 4 6.0 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4cc(F)cc(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10289494 77864 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 7 2 4 6.5 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210715 77864 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 7 2 4 6.5 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10196460 79413 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 546 7 2 4 7.0 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212159 79413 0 None - 0 Human 8.5 pKi = 8.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 546 7 2 4 7.0 N#Cc1cccc(-c2ccc(C3(NCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44592169 178244 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 488 5 0 6 5.9 Cn1cc(CCN2CCCC2)c2ccc(-n3ccc4nc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1021/jm8016199
CHEMBL469343 178244 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 488 5 0 6 5.9 Cn1cc(CCN2CCCC2)c2ccc(-n3ccc4nc(-c5ccc(Cl)cc5)sc4c3=O)cc21 10.1021/jm8016199
44592214 188757 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 470 4 1 6 4.9 CN[C@@H]1CCN(c2ccc(-n3ccc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm8016199
CHEMBL512657 188757 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 470 4 1 6 4.9 CN[C@@H]1CCN(c2ccc(-n3ccc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm8016199
44417887 140940 0 None - 0 Human 8.5 pKi = 8.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Cl)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL384400 140940 0 None - 0 Human 8.5 pKi = 8.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Cl)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
52948636 16825 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 607 8 1 5 5.5 CN(C)Cc1cccc([C@]23CCC(N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254244 16825 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 607 8 1 5 5.5 CN(C)Cc1cccc([C@]23CCC(N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
11570040 77401 0 None - 1 Human 8.5 pKi = 8.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 5 1 3 7.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209109 77401 0 None - 1 Human 8.5 pKi = 8.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 5 1 3 7.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
11698592 77688 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 476 3 2 3 6.4 N#Cc1cccc(-c2ccc(C(=C3CCNCC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209993 77688 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 476 3 2 3 6.4 N#Cc1cccc(-c2ccc(C(=C3CCNCC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
11613696 134719 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 9 2 5 4.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL372551 134719 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 9 2 5 4.6 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
44413283 79312 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 5 1 3 7.7 N#Cc1ccc(F)c(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211672 79312 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 5 1 3 7.7 N#Cc1ccc(F)c(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
20609018 139613 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 529 7 1 3 7.7 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL380275 139613 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 529 7 1 3 7.7 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52948553 16787 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 10 2 3 6.6 CC(=O)NCc1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253877 16787 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 556 10 2 3 6.6 CC(=O)NCc1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52945088 16841 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 493 7 1 4 5.7 CC(=O)C1CCC(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)S1 10.1016/j.ejmech.2010.07.011
CHEMBL1254403 16841 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 493 7 1 4 5.7 CC(=O)C1CCC(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)S1 10.1016/j.ejmech.2010.07.011
44417924 140862 0 None - 0 Human 4.5 pKi = 4.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 528 7 0 5 2.1 CS(=O)(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N2CCN(CCc4ccc(F)cc4)CC2=O)C3)CC1 10.1016/j.bmcl.2006.10.052
CHEMBL384030 140862 0 None - 0 Human 4.5 pKi = 4.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 528 7 0 5 2.1 CS(=O)(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N2CCN(CCc4ccc(F)cc4)CC2=O)C3)CC1 10.1016/j.bmcl.2006.10.052
44417892 79811 0 None - 1 Human 6.5 pKi = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 500 5 0 4 4.2 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cn2)C3)CC1 10.1016/j.bmcl.2006.10.053
CHEMBL213771 79811 0 None - 1 Human 6.5 pKi = 6.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 500 5 0 4 4.2 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cn2)C3)CC1 10.1016/j.bmcl.2006.10.053
44405501 71520 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 8 2 5 5.1 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL197065 71520 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 550 8 2 5 5.1 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
44413299 77002 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 518 3 1 3 6.7 CC(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL208573 77002 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 518 3 1 3 6.7 CC(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44413312 79222 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 4 1 3 7.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)C4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211511 79222 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 4 1 3 7.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)C4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
52949479 16881 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 5 1 3 6.0 CC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254799 16881 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 5 1 3 6.0 CC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
44424266 85347 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 481 6 1 3 6.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cc3ccccc3o2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL229407 85347 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 481 6 1 3 6.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cc3ccccc3o2)CC1 10.1016/j.ejmech.2010.07.011
11664086 77345 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 561 3 1 3 6.7 CN(C)C(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
CHEMBL208931 77345 0 None - 0 Human 7.5 pKi = 7.5 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 561 3 1 3 6.7 CN(C)C(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
44417889 140861 0 None - 0 Human 7.5 pKi = 7.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 425 8 0 3 4.5 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCC3CCCCC3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL384000 140861 0 None - 0 Human 7.5 pKi = 7.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 425 8 0 3 4.5 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCC3CCCCC3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
10312086 79426 0 None - 0 Human 5.5 pKi = 5.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.6 O=C(CNC1(c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212210 79426 0 None - 0 Human 5.5 pKi = 5.5 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.6 O=C(CNC1(c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
52946137 16802 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 6 2 4 4.7 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Br)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254054 16802 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 522 6 2 4 4.7 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Br)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52940981 16892 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 527 9 1 4 6.2 COC(=O)c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254885 16892 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 527 9 1 4 6.2 COC(=O)c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44417960 81370 0 None - 1 Human 5.5 pKi = 5.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 472 5 1 4 3.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)nc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2006.10.053
CHEMBL216429 81370 0 None - 1 Human 5.5 pKi = 5.5 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 472 5 1 4 3.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)nc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2006.10.053
10186370 71450 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 520 8 1 4 5.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL196819 71450 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 520 8 1 4 5.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CCCC3)cc2)c1 10.1016/j.bmcl.2005.08.043
11642443 77259 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 3 1 3 6.8 CN(C)C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL208827 77259 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 3 1 3 6.8 CN(C)C(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
52947314 16776 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 474 7 2 5 4.0 COc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253793 16776 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 474 7 2 5 4.0 COc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.ejmech.2010.07.011
11318709 139126 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 541 7 2 4 7.4 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL379789 139126 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 541 7 2 4 7.4 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44434156 144983 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN(CCCN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@H]2CC[C@]3(c4cnc(CN)s4)C[C@H]23)[C@H](C)CN1 10.1016/j.bmcl.2007.06.048
CHEMBL391496 144983 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN(CCCN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@H]2CC[C@]3(c4cnc(CN)s4)C[C@H]23)[C@H](C)CN1 10.1016/j.bmcl.2007.06.048
10152879 78432 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 7 1 4 6.8 CN(CC(=O)Nc1ccc(F)c(Cl)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL211285 78432 0 None - 0 Human 8.4 pKi = 8.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 7 1 4 6.8 CN(CC(=O)Nc1ccc(F)c(Cl)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
52945863 16907 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 10 1 4 6.9 CO/N=C/c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254972 16907 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 10 1 4 6.9 CO/N=C/c1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52947542 16846 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 489 8 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCNCCF)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254482 16846 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 489 8 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCNCCF)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52947539 16837 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1cc(F)cc(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254399 16837 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1cc(F)cc(F)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
11635274 138146 0 None - 1 Human 8.3 pKi = 8.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 5 1 3 7.4 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(CC3CC3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL377843 138146 0 None - 1 Human 8.3 pKi = 8.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 5 1 3 7.4 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(CC3CC3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
52942539 16812 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254147 16812 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
20608977 138709 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 513 7 1 3 7.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4cc(F)cc(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL378972 138709 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 513 7 1 3 7.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4cc(F)cc(F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
11628136 77407 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 5 2 4 6.1 N#Cc1cccc(-c2ccc(C3(c4nc5cc(F)c(C(F)(F)F)cc5[nH]4)CC34CCN(CC(=O)O)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209123 77407 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 5 2 4 6.1 N#Cc1cccc(-c2ccc(C3(c4nc5cc(F)c(C(F)(F)F)cc5[nH]4)CC34CCN(CC(=O)O)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
20608976 77761 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 545 7 1 3 8.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210343 77761 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 545 7 1 3 8.2 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44434144 166744 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 525 7 2 5 5.2 NCc1cnc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)CC2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL429393 166744 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 525 7 2 5 5.2 NCc1cnc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)CC2C3)s1 10.1016/j.bmcl.2007.06.048
11527169 77011 0 None - 1 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 587 3 1 3 7.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(C(=O)N3CCCC3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL208635 77011 0 None - 1 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 587 3 1 3 7.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(C(=O)N3CCCC3)CC4)cc2)c1 10.1016/j.bmcl.2006.04.062
44434146 88998 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237099 88998 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
20608992 77930 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 8 1 3 6.7 CCN(CC)C(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL211005 77930 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 544 8 1 3 6.7 CCN(CC)C(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
44413471 79190 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 5 1 5 7.8 N#Cc1cccc(-c2ccc(C(=C3CCN(Cc4nccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211492 79190 0 None - 0 Human 7.4 pKi = 7.4 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 5 1 5 7.8 N#Cc1cccc(-c2ccc(C(=C3CCN(Cc4nccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44412682 78029 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 562 8 1 3 8.5 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)c(F)ccc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211166 78029 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 562 8 1 3 8.5 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)c(F)ccc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52944920 16804 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 570 12 1 3 7.8 CCN(CC)Cc1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254056 16804 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 570 12 1 3 7.8 CCN(CC)Cc1cccc([C@]23CCC(N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44413345 140950 0 None - 0 Human 6.3 pKi = 6.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 5 1 3 7.6 N#Cc1ccccc1-c1ccc(C(=C2CCN(CC3CC3)CC2)c2nc3cc(C(F)(F)F)c(F)cc3[nH]2)cc1 10.1016/j.bmcl.2006.04.062
CHEMBL384449 140950 0 None - 0 Human 6.3 pKi = 6.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 5 1 3 7.6 N#Cc1ccccc1-c1ccc(C(=C2CCN(CC3CC3)CC2)c2nc3cc(C(F)(F)F)c(F)cc3[nH]2)cc1 10.1016/j.bmcl.2006.04.062
44417927 80659 0 None - 0 Human 7.3 pKi = 7.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 429 8 0 4 3.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCC3CCCS3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL215526 80659 0 None - 0 Human 7.3 pKi = 7.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 429 8 0 4 3.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCC3CCCS3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
52943689 16795 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 6 2 4 4.4 Cc1ccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)cc1F 10.1016/j.ejmech.2010.07.011
CHEMBL1253961 16795 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 476 6 2 4 4.4 Cc1ccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)cc1F 10.1016/j.ejmech.2010.07.011
52944577 16893 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 515 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CO)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254886 16893 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 515 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CO)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
44405421 71642 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 490 8 1 3 6.5 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL197429 71642 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 490 8 1 3 6.5 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
44405418 135248 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 506 8 1 3 7.1 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL373036 135248 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 506 8 1 3 7.1 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
44412686 78600 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 607 8 2 5 7.8 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(C(=O)OCc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211311 78600 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 607 8 2 5 7.8 N#Cc1cccc(-c2ccc(C(NCc3nc4cc(Cl)c(F)cc4[nH]3)C3CCN(C(=O)OCc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10196742 161160 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 581 7 1 4 7.8 N#Cc1cccc(-c2ccc(C3(OCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL413578 161160 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 581 7 1 4 7.8 N#Cc1cccc(-c2ccc(C3(OCC(=O)Nc4ccc(Cl)c(C(F)(F)F)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44417963 165447 0 None - 1 Human 6.3 pKi = 6.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4cccc(C(F)(F)F)c4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL425445 165447 0 None - 1 Human 6.3 pKi = 6.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4cccc(C(F)(F)F)c4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
52942547 16824 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.ejmech.2010.07.011
CHEMBL1254243 16824 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.ejmech.2010.07.011
52943420 16908 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 6 1 4 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254973 16908 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 542 6 1 4 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
52948635 16822 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 536 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1cccc(Br)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254241 16822 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 536 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1cccc(Br)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52946259 16831 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 492 8 1 3 6.7 CC(C)N(CCN(C(=O)Nc1cccc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254327 16831 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 492 8 1 3 6.7 CC(C)N(CCN(C(=O)Nc1cccc(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
44412624 77967 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 579 8 1 4 7.6 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C(=O)OCc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211058 77967 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 579 8 1 4 7.6 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(C(=O)OCc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
10129036 79399 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3cc(Cl)ccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212093 79399 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3cc(Cl)ccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
11562056 79366 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 480 5 1 3 6.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL211956 79366 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 480 5 1 3 6.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417893 80156 0 None - 0 Human 4.3 pKi = 4.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 432 6 0 4 3.3 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(Cn3ccnc3)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL214983 80156 0 None - 0 Human 4.3 pKi = 4.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 432 6 0 4 3.3 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(Cn3ccnc3)ccc2C1 10.1016/j.bmcl.2006.10.052
10152726 138187 0 None - 0 Human 6.3 pKi = 6.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 7 2 4 6.5 N#Cc1ccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)cc1 10.1016/j.bmcl.2006.04.061
CHEMBL378009 138187 0 None - 0 Human 6.3 pKi = 6.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 530 7 2 4 6.5 N#Cc1ccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)cc1 10.1016/j.bmcl.2006.04.061
44417912 81849 0 None - 0 Human 5.3 pKi = 5.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 489 7 0 5 4.0 CN(C(=O)c1cc2n(n1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O)c1ccc(F)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL217140 81849 0 None - 0 Human 5.3 pKi = 5.3 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 489 7 0 5 4.0 CN(C(=O)c1cc2n(n1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O)c1ccc(F)cc1 10.1016/j.bmcl.2006.10.096
11433168 138151 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 8 1 3 9.0 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)cc(Cl)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL377874 138151 0 None - 0 Human 7.3 pKi = 7.3 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 578 8 1 3 9.0 N#Cc1cccc(-c2ccc(C(CCc3nc4c(Cl)cc(Cl)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52947267 16758 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 597 10 1 4 6.7 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN4CCN(C)CC4)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1253629 16758 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 597 10 1 4 6.7 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(CN4CCN(C)CC4)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52948531 16777 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)cc4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253794 16777 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)cc4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
44424270 85356 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 473 6 1 5 5.4 N#Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
CHEMBL229463 85356 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 473 6 1 5 5.4 N#Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.ejmech.2010.07.011
52943690 16796 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 489 7 2 6 3.9 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc([N+](=O)[O-])c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1253962 16796 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 489 7 2 6 3.9 N#Cc1cccc([C@]23CCC(N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc([N+](=O)[O-])c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
24963343 72787 0 None - 1 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human MCH1R expressed in forskolin-stimulated CHO cells assessed as inhibition of MCH-induced cAMP accumulation after 90 minsAntagonist activity at human MCH1R expressed in forskolin-stimulated CHO cells assessed as inhibition of MCH-induced cAMP accumulation after 90 mins
ChEMBL 362 5 1 6 2.3 N[C@@H]1CCN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C1 10.1016/j.bmcl.2012.02.010
CHEMBL2011537 72787 0 None - 1 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human MCH1R expressed in forskolin-stimulated CHO cells assessed as inhibition of MCH-induced cAMP accumulation after 90 minsAntagonist activity at human MCH1R expressed in forskolin-stimulated CHO cells assessed as inhibition of MCH-induced cAMP accumulation after 90 mins
ChEMBL 362 5 1 6 2.3 N[C@@H]1CCN(c2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2)C1 10.1016/j.bmcl.2012.02.010
10239505 77562 0 None - 0 Human 8.2 pKi = 8.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 528 7 1 4 6.3 CN(CC(=O)Nc1cc(F)cc(F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL209504 77562 0 None - 0 Human 8.2 pKi = 8.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 528 7 1 4 6.3 CN(CC(=O)Nc1cc(F)cc(F)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
44434154 89476 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@H]1CC[C@]2(c3cnc(CN)s3)C[C@H]12 10.1016/j.bmcl.2007.06.048
CHEMBL237959 89476 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 551 8 3 7 4.3 C[C@H]1CN[C@H](C)CN1CCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@H]1CC[C@]2(c3cnc(CN)s3)C[C@H]12 10.1016/j.bmcl.2007.06.048
11512221 89379 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237748 89379 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 541 8 3 6 4.2 NCc1ncc([C@]23CC[C@H](N(CCCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)s1 10.1016/j.bmcl.2007.06.048
52947610 16858 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCC[C@@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254634 16858 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CCC(N(CCN4CCC[C@@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
10280331 140772 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 536 8 2 5 4.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL383390 140772 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 536 8 2 5 4.6 N#Cc1cccc(-c2ccc(CN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CN3CC[C@@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
20608969 77803 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 487 6 1 3 5.8 CC(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL210481 77803 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 487 6 1 3 5.8 CC(=O)N1CCC(CCC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2006.04.061
44417920 80427 0 None - 0 Human 4.2 pKi = 4.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 477 6 0 3 4.8 C[C@H]1CCC[C@@H](C)N1Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL215266 80427 0 None - 0 Human 4.2 pKi = 4.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 477 6 0 3 4.8 C[C@H]1CCC[C@@H](C)N1Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
44417987 81986 0 None - 0 Human 6.2 pKi = 6.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 474 7 1 4 4.6 O=C(Nc1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
CHEMBL217351 81986 0 None - 0 Human 6.2 pKi = 6.2 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 474 7 1 4 4.6 O=C(Nc1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2006.10.096
20609011 138173 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3cccc(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL377976 138173 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3cccc(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44413480 79516 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 5 1 4 6.0 CN(C)S(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL212573 79516 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 583 5 1 4 6.0 CN(C)S(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
11635715 77075 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 596 5 1 4 6.8 CC(C)S(=O)(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
CHEMBL208688 77075 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 596 5 1 4 6.8 CC(C)S(=O)(=O)N1CCC2(CC1)CC2(c1ccc(-c2cccc(C#N)c2)cc1)c1nc2cc(F)c(C(F)(F)F)cc2[nH]1 10.1016/j.bmcl.2006.04.062
10239639 77784 0 None - 0 Human 6.2 pKi = 6.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3ccccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL210408 77784 0 None - 0 Human 6.2 pKi = 6.2 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 539 7 2 3 7.3 O=C(CNC1(c2ccc(-c3ccccc3Cl)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
52947054 16894 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1254887 16894 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
10281308 72006 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 10 2 5 5.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL198562 72006 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 564 10 2 5 5.0 N#Cc1cccc(-c2ccc(CCN(CC(=O)Nc3cc(Cl)cc(Cl)c3)C(=O)CCN3CC[C@H](O)C3)cc2)c1 10.1016/j.bmcl.2005.08.043
44413382 77399 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 520 5 2 4 6.1 N#Cc1cccc(-c2ccc(C(=C3CCN(CCO)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209103 77399 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 520 5 2 4 6.1 N#Cc1cccc(-c2ccc(C(=C3CCN(CCO)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
11270012 81722 0 None - 1 Human 8.1 pKi = 8.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 416 5 0 2 5.2 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216821 81722 0 None - 1 Human 8.1 pKi = 8.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 416 5 0 2 5.2 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2006.10.053
52949955 16836 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 483 8 1 4 5.9 CC(C)N(CCN(C(=O)Nc1cccc(C#N)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254398 16836 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 483 8 1 4 5.9 CC(C)N(CCN(C(=O)Nc1cccc(C#N)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
52945806 16880 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 547 8 1 2 7.2 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)C1CC[C@]2(c3cccc(Br)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
CHEMBL1254798 16880 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 547 8 1 2 7.2 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)C1CC[C@]2(c3cccc(Br)c3)CC2C1)C(C)C 10.1016/j.ejmech.2010.07.011
44405436 71588 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 524 8 1 3 6.9 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
CHEMBL197279 71588 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 524 8 1 3 6.9 N#Cc1cccc(-c2ccc(CN(CCCN3CCCC3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2005.08.043
11656916 138350 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 554 4 1 4 6.1 CS(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
CHEMBL378242 138350 0 None - 0 Human 7.2 pKi = 7.2 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 554 4 1 4 6.1 CS(=O)(=O)N1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2006.04.062
44417954 96798 0 None - 0 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 482 5 0 4 4.0 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccccn4)cc2)C3)CC1 10.1016/j.bmcl.2006.10.053
CHEMBL268848 96798 0 None - 0 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 482 5 0 4 4.0 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccccn4)cc2)C3)CC1 10.1016/j.bmcl.2006.10.053
44434152 89171 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 552 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC5CC4CN5)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237532 89171 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 552 8 3 6 4.2 NCc1ncc([C@]23CC[C@@H](N(CCCN4CC5CC4CN5)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
44417898 82149 0 None - 1 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 506 5 0 4 4.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.053
CHEMBL217860 82149 0 None - 1 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 506 5 0 4 4.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.053
44405444 134662 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 578 10 2 5 5.9 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
CHEMBL372116 134662 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 578 10 2 5 5.9 C[C@H](c1ccc(-c2cccc(C#N)c2)cc1)N(CC(=O)Nc1cc(Cl)cc(Cl)c1)C(=O)CCCN1CC[C@H](O)C1 10.1016/j.bmcl.2005.08.043
10129135 77677 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 8 2 4 7.5 O=C(CNC1(c2ccc(-c3cccc(OC(F)(F)F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL209935 77677 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 589 8 2 4 7.5 O=C(CNC1(c2ccc(-c3cccc(OC(F)(F)F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
16106513 178294 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 464 7 1 6 4.5 COc1cc(-c2cnc3[nH]c(-c4ccc(Cl)cc4)cn3c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
CHEMBL469789 178294 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1RAntagonist activity at MCH1R
ChEMBL 464 7 1 6 4.5 COc1cc(-c2cnc3[nH]c(-c4ccc(Cl)cc4)cn3c2=O)ccc1OCCN1CCCC1 10.1021/jm8016199
10218194 77995 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 535 8 2 4 6.6 COc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211139 77995 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 535 8 2 4 6.6 COc1cccc(-c2ccc(C3(NCC(=O)Nc4ccc(F)c(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
44413271 137852 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 6 2 3 6.8 NC(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL377270 137852 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 548 6 2 3 6.8 NC(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
16659061 82150 0 None - 0 Human 7.1 pKi = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 463 9 1 5 3.8 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL217861 82150 0 None - 0 Human 7.1 pKi = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 463 9 1 5 3.8 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
10239930 79214 0 None - 0 Human 6.1 pKi = 6.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3cc(Cl)cc(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211504 79214 0 None - 0 Human 6.1 pKi = 6.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 573 7 2 3 7.9 O=C(CNC1(c2ccc(-c3cc(Cl)cc(Cl)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
52949693 16759 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 606 7 1 4 6.1 CS(=O)(=O)N1CCC(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253630 16759 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 606 7 1 4 6.1 CS(=O)(=O)N1CCC(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
20608981 79440 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 499 8 1 3 6.7 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL212265 79440 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 499 8 1 3 6.7 N#Cc1cccc(-c2ccc(C3(CCC(=O)Nc4ccc(F)c(F)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52947408 16814 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 512 9 2 4 5.4 CC(C)N(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
CHEMBL1254149 16814 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 512 9 2 4 5.4 CC(C)N(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.ejmech.2010.07.011
52941518 16859 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 564 6 1 4 6.6 N#Cc1cccc([C@]23CCC(N(CC4CCN(C5CCOCC5)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254635 16859 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 564 6 1 4 6.6 N#Cc1cccc([C@]23CCC(N(CC4CCN(C5CCOCC5)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.ejmech.2010.07.011
52943587 16760 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 649 8 2 6 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)C2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253631 16760 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 649 8 2 6 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)C2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
10188732 134863 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 591 10 2 5 4.8 CC(=O)N[C@@H]1CCN(CC(=O)N(CCc2ccc(-c3cccc(C#N)c3)cc2)CC(=O)Nc2cc(Cl)cc(Cl)c2)C1 10.1016/j.bmcl.2005.08.043
CHEMBL372803 134863 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity against human MCH1 receptorAntagonist activity against human MCH1 receptor
ChEMBL 591 10 2 5 4.8 CC(=O)N[C@@H]1CCN(CC(=O)N(CCc2ccc(-c3cccc(C#N)c3)cc2)CC(=O)Nc2cc(Cl)cc(Cl)c2)C1 10.1016/j.bmcl.2005.08.043
44417934 82039 0 None - 1 Human 7.1 pKi = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 435 7 1 5 3.0 CN(C)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
CHEMBL217605 82039 0 None - 1 Human 7.1 pKi = 7.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 435 7 1 5 3.0 CN(C)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2006.10.096
52949956 16840 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 465 6 1 3 6.2 CC1CCC(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)S1 10.1016/j.ejmech.2010.07.011
CHEMBL1254402 16840 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 465 6 1 3 6.2 CC1CCC(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)S1 10.1016/j.ejmech.2010.07.011
11497180 165201 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 512 5 1 3 7.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(Cl)cc(Cl)c4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL424697 165201 0 None - 0 Human 7.1 pKi = 7.1 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 512 5 1 3 7.7 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(Cl)cc(Cl)c4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
44417929 81512 0 None - 0 Human 5.1 pKi = 5.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 517 6 0 3 4.8 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCC(C(F)(F)F)CC3)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL216486 81512 0 None - 0 Human 5.1 pKi = 5.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 517 6 0 3 4.8 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCC(C(F)(F)F)CC3)ccc2C1 10.1016/j.bmcl.2006.10.052
44417985 81138 0 None - 0 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3cccnc3)cc1)C2 10.1016/j.bmcl.2006.10.053
CHEMBL216187 81138 0 None - 0 Human 6.1 pKi = 6.1 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3cccnc3)cc1)C2 10.1016/j.bmcl.2006.10.053
11752339 69041 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmcl.2007.06.048
CHEMBL193260 69041 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmcl.2007.06.048
10196576 138714 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 560 7 1 4 7.3 CN(CC(=O)Nc1cc(Cl)cc(Cl)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
CHEMBL378994 138714 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 560 7 1 4 7.3 CN(CC(=O)Nc1cc(Cl)cc(Cl)c1)C1(c2ccc(-c3cccc(C#N)c3)cc2)CCN(C2CCCC2)CC1 10.1016/j.bmcl.2006.04.061
52948951 16823 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@H](C)CO 10.1016/j.ejmech.2010.07.011
CHEMBL1254242 16823 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)C1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@H](C)CO 10.1016/j.ejmech.2010.07.011
52949768 16788 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 6 1 4 4.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cccc(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
CHEMBL1253878 16788 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 524 6 1 4 4.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cccc(F)c2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.ejmech.2010.07.011
44412683 78745 0 None - 0 Human 7.0 pKi = 7.0 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 596 8 1 3 8.9 N#Cc1cccc(-c2ccc(C(CCc3nc4cc(C(F)(F)F)c(F)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
CHEMBL211335 78745 0 None - 0 Human 7.0 pKi = 7.0 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 596 8 1 3 8.9 N#Cc1cccc(-c2ccc(C(CCc3nc4cc(C(F)(F)F)c(F)cc4[nH]3)C3CCN(Cc4ccccc4)CC3)cc2)c1 10.1016/j.bmcl.2006.04.061
52944948 16811 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 469 6 2 5 3.8 N#Cc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.ejmech.2010.07.011
CHEMBL1254146 16811 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at MCH1 receptorAntagonist activity at MCH1 receptor
ChEMBL 469 6 2 5 3.8 N#Cc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)C2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.ejmech.2010.07.011
44417891 79927 0 None - 0 Human 7.0 pKi = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(C(F)(F)F)c3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL214323 79927 0 None - 0 Human 7.0 pKi = 7.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(C(F)(F)F)c3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
44417908 81737 0 None - 0 Human 4.0 pKi = 4.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 6 0 5 2.3 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.052
CHEMBL216959 81737 0 None - 0 Human 4.0 pKi = 4.0 Functional
Functional antagonism of MCH-R1 expressed in HEK293 cellsFunctional antagonism of MCH-R1 expressed in HEK293 cells
ChEMBL 499 6 0 5 2.3 O=C1CN(CCc2ccc(F)cc2)CCN1[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2006.10.052
44413259 139147 0 None - 1 Human 7.0 pKi = 7.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 507 5 1 4 6.5 Fc1cc2[nH]c(C(=C3CCN(CC4CC4)CC3)c3ccc(-c4cncnc4)cc3)nc2cc1C(F)(F)F 10.1016/j.bmcl.2006.04.062
CHEMBL379802 139147 0 None - 1 Human 7.0 pKi = 7.0 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 507 5 1 4 6.5 Fc1cc2[nH]c(C(=C3CCN(CC4CC4)CC3)c3ccc(-c4cncnc4)cc3)nc2cc1C(F)(F)F 10.1016/j.bmcl.2006.04.062
44434145 88996 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 527 7 3 6 3.8 NCc1ncc([C@]23CC[C@@H](N(CCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
CHEMBL237098 88996 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at MCHR1Antagonist activity at MCHR1
ChEMBL 527 7 3 6 3.8 NCc1ncc([C@]23CC[C@@H](N(CCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C2C3)s1 10.1016/j.bmcl.2007.06.048
10152629 140989 0 None - 0 Human 7.0 pKi = 7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3cccc(F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
CHEMBL384676 140989 0 None - 0 Human 7.0 pKi = 7 Functional
Binding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity at human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 523 7 2 3 6.7 O=C(CNC1(c2ccc(-c3cccc(F)c3)cc2)CCN(C2CCCC2)CC1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2006.04.061
44413398 77578 0 None - 0 Human 7.0 pKi = 7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 5 2 5 6.7 N#Cc1cnc(O)c(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
CHEMBL209590 77578 0 None - 0 Human 7.0 pKi = 7 Functional
Binding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assayBinding affinity to human MCHR1 assessed as inhibition of MCH-mediated calcium ion influx by FLIPR assay
ChEMBL 547 5 2 5 6.7 N#Cc1cnc(O)c(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2006.04.062
11520239 3562 4 None - 1 Human 9.2 pA2 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
1313 3562 4 None - 1 Human 9.2 pA2 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
CHEMBL185271 3562 4 None - 1 Human 9.2 pA2 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
54579974 3177 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 21414780
7756 3177 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 21414780
CHEMBL1760248 3177 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 21414780
7735 531 8 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 17532215
9927967 531 8 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 17532215
CHEMBL400679 531 8 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 17532215
1305 508 10 None 2 7 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
9934033 508 10 None 2 7 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
CHEMBL182150 508 10 None 2 7 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
1314 3657 18 None -1 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 11909603
9865843 3657 18 None -1 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 11909603
CHEMBL178707 3657 18 None -1 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 11909603
24890862 1085 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 494 6 0 7 3.9 CCO/N=C(\c1ccc(c(c1)F)F)/c1ccc(cn1)CN1CCC2(CC1)OCc1c2cc(=O)n(c1)C 19683441
7755 1085 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 494 6 0 7 3.9 CCO/N=C(\c1ccc(c(c1)F)F)/c1ccc(cn1)CN1CCC2(CC1)OCc1c2cc(=O)n(c1)C 19683441
57523087 1132 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 22490048
7754 1132 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 22490048
CHEMBL2059513 1132 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 22490048
57521365 2567 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 22490048
57521365 2567 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 24670150
8587 2567 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 22490048
8587 2567 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 24670150
CHEMBL2059420 2567 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 22490048
CHEMBL2059420 2567 0 None 1 2 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 24670150
56835134 114 0 None - 1 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 22137790
7753 114 0 None - 1 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 22137790
CHEMBL1934835 114 0 None - 1 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 22137790
4033 1860 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 16870432
9826520 1860 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 16870432
CHEMBL214957 1860 42 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 16870432
1292 1039 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1290 256 0 None 15 2 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12009900
1307 524 0 None -1 2 Human 7.3 pIC50 None 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12009900
11305934 3776 2 None -1 2 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 19041642
1315 3776 2 None -1 2 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 19041642
CHEMBL2147477 3776 2 None -1 2 Human 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 470 12 3 3 2.9 Fc1cccc(c1)CCN1[C@@H](CCCN=C(N)N)CN(C1=S)[C@H](CNCc1ccccc1)C 19041642
1300 3027 0 None - 1 Human 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19619599
11539096 181 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 17064075
1303 181 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 17064075
CHEMBL214021 181 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 17064075
1297 3042 0 None 1 2 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
1297 3042 0 None 1 2 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11159839
1297 3042 0 None 1 2 Human 9.1 pIC50 None 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11404457
11994411 987 0 None - 1 Human 9.4 pIC50 None 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 17125263
1306 987 0 None - 1 Human 9.4 pIC50 None 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 17125263
CHEMBL214523 987 0 None - 1 Human 9.4 pIC50 None 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 4 0 5 6.9 Clc1ccc(cc1)c1cc2c(s1)c(=O)n(cn2)c1ccc2c(c1)ccc(c2)CN1CCCCC1 17125263


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
44219756 178105 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 531 9 0 6 4.0 O=C(C(c1ccc(F)c(F)c1)n1cccn1)N(CCF)CCCN1CCC2(CC1)OCc1cc(F)ncc12 10.1016/j.bmcl.2009.07.132
CHEMBL468099 178105 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 531 9 0 6 4.0 O=C(C(c1ccc(F)c(F)c1)n1cccn1)N(CCF)CCCN1CCC2(CC1)OCc1cc(F)ncc12 10.1016/j.bmcl.2009.07.132
44219756 178105 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 531 9 0 6 4.0 O=C(C(c1ccc(F)c(F)c1)n1cccn1)N(CCF)CCCN1CCC2(CC1)OCc1cc(F)ncc12 10.1016/j.bmcl.2009.04.016
CHEMBL468099 178105 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 531 9 0 6 4.0 O=C(C(c1ccc(F)c(F)c1)n1cccn1)N(CCF)CCCN1CCC2(CC1)OCc1cc(F)ncc12 10.1016/j.bmcl.2009.04.016
44442095 93853 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250516 93853 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11648912 79926 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 494 8 3 4 5.5 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)ccc1F 10.1016/j.bmcl.2006.07.040
CHEMBL214322 79926 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 494 8 3 4 5.5 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)ccc1F 10.1016/j.bmcl.2006.07.040
45487671 195593 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 481 6 0 5 5.3 CCO/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL568571 195593 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 481 6 0 5 5.3 CCO/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
44574008 188626 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 513 8 0 6 4.0 CCN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
CHEMBL511542 188626 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 513 8 0 6 4.0 CCN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
9915039 60483 0 None - 1 Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 532 7 2 3 7.1 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL176219 60483 0 None - 1 Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 532 7 2 3 7.1 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2019.126741
45487668 195312 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 467 5 0 5 4.9 CO/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL566880 195312 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 467 5 0 5 4.9 CO/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
45271549 193890 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 644 8 0 6 5.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(C(=O)OC(C)(C)C)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL555055 193890 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 644 8 0 6 5.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(C(=O)OC(C)(C)C)CC1=O 10.1016/j.bmcl.2009.03.102
24762415 197060 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 453 4 1 5 4.7 O/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL582978 197060 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 453 4 1 5 4.7 O/N=C(/c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
44417966 160959 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 5 2 3 6.0 CCC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL412831 160959 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 5 2 3 6.0 CCC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
16049789 168442 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 3 2 3 5.8 CC(C)(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL439358 168442 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 3 2 3 5.8 CC(C)(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10118862 60463 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 7 2 3 7.1 CCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL176159 60463 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 7 2 3 7.1 CCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
45487674 197037 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 482 6 0 6 4.7 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL582792 197037 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 482 6 0 6 4.7 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cn1 10.1016/j.bmcl.2009.07.132
10258364 193106 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.07.132
CHEMBL538424 193106 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.07.132
CHEMBL538425 193106 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.07.132
18436066 74530 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 455 5 1 3 6.7 Cc1c(NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031736 74530 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 455 5 1 3 6.7 Cc1c(NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
10258364 193106 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 193106 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 193106 0 None 1 2 Human 9.4 pIC50 = 9.4 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
10360874 64588 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL182261 64588 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
10230490 62834 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 536 8 2 4 6.3 COCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL178997 62834 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 536 8 2 4 6.3 COCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
10345845 177888 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 499 7 0 6 3.7 CN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
CHEMBL466425 177888 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 499 7 0 6 3.7 CN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
22018957 82016 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 468 5 2 4 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC4(CCNC4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217502 82016 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 468 5 2 4 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC4(CCNC4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
11561126 68504 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922270 68504 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
11561126 68504 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL1922270 68504 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 434 4 1 2 6.0 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
18436114 74528 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 451 6 1 4 6.1 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
CHEMBL2031734 74528 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 451 6 1 4 6.1 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
9932896 74163 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2029372 74163 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
9932896 74163 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2029372 74163 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
10004545 74588 4 None 1862 3 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74588 4 None 1862 3 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
46933538 16025 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 484 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224229 16025 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 484 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417832 141208 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385957 141208 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10258364 193106 0 None 1 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 193106 0 None 1 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 193106 0 None 1 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
10459635 195010 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 529 8 0 4 4.5 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL564788 195010 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 529 8 0 4 4.5 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
18436055 74510 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 441 5 1 3 6.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1021/jm201596h
CHEMBL2031716 74510 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 441 5 1 3 6.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1021/jm201596h
70696356 74478 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 424 5 1 2 6.5 O=C(Nc1ccc2cc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031573 74478 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 424 5 1 2 6.5 O=C(Nc1ccc2cc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
44417948 141205 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 425 4 2 3 6.1 Nc1cc(C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL385941 141205 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 425 4 2 3 6.1 Nc1cc(C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
22348140 168147 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 501 6 1 6 5.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2006.02.044
CHEMBL436953 168147 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 501 6 1 6 5.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2006.02.044
45273335 194147 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 544 8 1 5 3.3 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCNCC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL558305 194147 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 544 8 1 5 3.3 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCNCC1=O 10.1016/j.bmcl.2009.03.102
10114686 60231 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1cc(F)cc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL175993 60231 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1cc(F)cc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
10067783 65853 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 370 6 3 4 4.1 Nc1ccc2cccc(OCCCNC(=O)Nc3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184417 65853 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 370 6 3 4 4.1 Nc1ccc2cccc(OCCCNC(=O)Nc3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
10000146 64301 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL181813 64301 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11201645 71512 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197050 71512 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
57393332 68503 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 420 3 1 2 5.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922269 68503 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 420 3 1 2 5.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
44410849 137756 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 508 6 1 5 6.3 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
CHEMBL377084 137756 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 508 6 1 5 6.3 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
90666096 108828 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 532 7 1 4 7.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3218999 108828 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 532 7 1 4 7.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
44407944 165438 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL425407 165438 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70688018 74479 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 428 5 1 3 5.6 O=C(Nc1ccc2c(c1)OCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031574 74479 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 428 5 1 3 5.6 O=C(Nc1ccc2c(c1)OCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11705240 132279 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370120 132279 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
18436094 74521 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031727 74521 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
21108114 67717 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 424 6 0 3 5.2 CN1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914623 67717 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 424 6 0 3 5.2 CN1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
10226765 122607 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL361215 122607 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
44394650 65136 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 7 2 5 3.4 COc1cccc(CNCC(C)Oc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL183032 65136 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 7 2 5 3.4 COc1cccc(CNCC(C)Oc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
44394800 121829 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 373 6 2 6 4.0 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OC(F)(F)O4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL359995 121829 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 373 6 2 6 4.0 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OC(F)(F)O4)c2n1 10.1016/j.bmcl.2004.07.034
44394609 123354 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 545 10 2 5 7.6 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)c1cccc(Cl)c1 10.1016/j.bmcl.2004.07.034
CHEMBL362768 123354 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 545 10 2 5 7.6 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)c1cccc(Cl)c1 10.1016/j.bmcl.2004.07.034
10248906 123123 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 375 4 1 4 4.8 CC(C)(C)c1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL362009 123123 0 None - 0 Human 9.0 pIC50 = 9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 375 4 1 4 4.8 CC(C)(C)c1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
16721015 79996 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL214585 79996 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
11583193 141265 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 448 4 1 6 3.4 O=C(NC1CCN(Cc2ccc3ccc(=O)oc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL386281 141265 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 448 4 1 6 3.4 O=C(NC1CCN(Cc2ccc3ccc(=O)oc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
22018944 81782 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3C4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217078 81782 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3C4)ccc2c1 10.1016/j.bmcl.2006.08.006
22018964 141126 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 498 7 2 4 5.2 CC(C)C(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385452 141126 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 498 7 2 4 5.2 CC(C)C(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
56835134 114 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 10.1016/j.bmcl.2011.10.111
7753 114 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 10.1016/j.bmcl.2011.10.111
CHEMBL1934835 114 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(c1)C1CCN(CC1)CCCn1nc(c2ccc(c(c2)F)F)c2c(c1=O)cccc2 10.1016/j.bmcl.2011.10.111
25058425 60434 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761103 60434 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25114286 60450 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 504 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4F)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761119 60450 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 504 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4F)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
57890345 121877 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 7 1 2 5.7 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1F 10.1016/j.bmcl.2015.05.077
CHEMBL3600810 121877 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 7 1 2 5.7 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1F 10.1016/j.bmcl.2015.05.077
60130264 121878 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 7 1 2 5.7 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)c(F)c1 10.1016/j.bmcl.2015.05.077
CHEMBL3600811 121878 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 7 1 2 5.7 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)c(F)c1 10.1016/j.bmcl.2015.05.077
10413283 186875 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 490 7 0 3 5.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
CHEMBL494016 186875 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 490 7 0 3 5.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
18436117 74529 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 435 5 1 3 6.4 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
CHEMBL2031735 74529 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 435 5 1 3 6.4 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3C)cc2)cc1 10.1021/jm201596h
44557554 194727 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 10 2 4 5.8 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL562847 194727 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 10 2 4 5.8 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
9932896 74163 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2029372 74163 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
10481477 194002 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 511 8 0 4 4.4 CCN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL556697 194002 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 511 8 0 4 4.4 CCN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
44417875 80367 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 407 6 2 3 6.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(-c4ccccc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215204 80367 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 407 6 2 3 6.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(-c4ccccc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22348022 76983 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2006.02.044
CHEMBL208473 76983 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2006.02.044
57521365 2567 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
8587 2567 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
CHEMBL2059420 2567 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
10231341 63001 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 560 6 2 3 8.0 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCCC4)CC3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL179437 63001 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 560 6 2 3 8.0 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCCC4)CC3)cc2)c1 10.1016/j.bmcl.2019.126741
10113523 129281 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1cccc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL367532 129281 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1cccc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
44394769 66566 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 361 5 1 4 4.7 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL186548 66566 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 361 5 1 4 4.7 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
10150552 81167 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 385 4 2 3 5.1 CCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216324 81167 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 385 4 2 3 5.1 CCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417959 81369 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 7 2 3 6.2 CCCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216428 81369 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 7 2 3 6.2 CCCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10127348 141273 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 4 2 3 6.5 Nc1cc(C2CCCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL386320 141273 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 4 2 3 6.5 Nc1cc(C2CCCCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
57392823 67724 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 410 6 1 3 4.9 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914630 67724 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 410 6 1 3 4.9 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
22348155 76217 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
CHEMBL206314 76217 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 502 6 1 7 4.9 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2006.02.044
44555375 195117 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 453 4 1 5 4.7 O/N=C(\c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL565614 195117 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 453 4 1 5 4.7 O/N=C(\c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
18436038 76006 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059408 76006 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
44417845 141342 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141342 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11627530 75542 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204952 75542 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
45487660 197338 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 439 4 0 4 5.3 CN(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL585856 197338 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 439 4 0 4 5.3 CN(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
10345845 177888 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 499 7 0 6 3.7 CN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
CHEMBL466425 177888 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 499 7 0 6 3.7 CN(CCCN1CCC2(CC1)OCc1cc(F)ncc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
18436085 74524 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1cc2cc(CN3CCCC3)cnc2cc1NC(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031730 74524 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1cc2cc(CN3CCCC3)cnc2cc1NC(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
57522703 76008 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059410 76008 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
44417846 81673 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 359 6 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(CC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216580 81673 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 359 6 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(CC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
21939937 64371 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818800 64371 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
11775399 63015 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0512286
CHEMBL179501 63015 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0512286
45487647 195236 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 438 4 0 4 4.8 O=C(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL566257 195236 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 438 4 0 4 4.8 O=C(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
18436083 74525 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031731 74525 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 443 5 1 3 6.0 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1F)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
18436082 74526 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 459 5 1 3 6.5 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1Cl)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031732 74526 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 459 5 1 3 6.5 O=C(Nc1cc2ncc(CN3CCCC3)cc2cc1Cl)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
11676220 56399 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccc(Cl)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642475 56399 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccc(Cl)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11775399 63015 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmc.2010.12.002
CHEMBL179501 63015 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmc.2010.12.002
11713027 80747 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 498 8 3 4 5.4 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.040
CHEMBL215819 80747 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 498 8 3 4 5.4 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.040
11775399 63015 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL179501 63015 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1021/jm0490890
11775399 63015 0 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese miceInhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL179501 63015 0 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese miceInhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
44417998 81969 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 6 2 3 5.9 CCCc1cc(NC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217262 81969 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 6 2 3 5.9 CCCc1cc(NC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10150954 141003 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 6 2 3 5.8 CCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384765 141003 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 6 2 3 5.8 CCCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11548234 70837 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195635 70837 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
10027853 71503 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197026 71503 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
57523087 1132 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
7754 1132 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
CHEMBL2059513 1132 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
57523086 76023 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
CHEMBL2059426 76023 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
11496313 71953 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL198361 71953 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
21939898 64380 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 422 5 1 2 6.3 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818810 64380 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 422 5 1 2 6.3 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
18435902 76007 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059409 76007 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
11613073 75562 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205111 75562 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44573931 186859 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 479 7 0 4 5.6 CN(CCCC1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
CHEMBL493962 186859 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 479 7 0 4 5.6 CN(CCCC1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cccn1 10.1016/j.bmcl.2009.04.016
23022536 76016 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059418 76016 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
9932896 74163 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2029372 74163 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 439 5 1 3 6.2 Cc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
22251624 64366 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818795 64366 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
23022422 74527 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1c(NC(=O)c2ccc(-c3ccccc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031733 74527 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1c(NC(=O)c2ccc(-c3ccccc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
18435902 76007 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059409 76007 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 415 7 1 4 5.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
10183297 92867 0 None 109 3 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of rat MCH1R receptorInhibition of rat MCH1R receptor
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1016/j.bmcl.2009.07.132
CHEMBL245231 92867 0 None 109 3 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of rat MCH1R receptorInhibition of rat MCH1R receptor
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1016/j.bmcl.2009.07.132
44402563 71313 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 443 9 3 5 5.7 CC(C)CNCCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
CHEMBL196388 71313 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 443 9 3 5 5.7 CC(C)CNCCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
10005009 165812 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL427540 165812 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
21940083 64372 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818801 64372 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
9910346 64386 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818901 64386 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
10345121 186860 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1ccnn1 10.1016/j.bmcl.2009.04.016
CHEMBL493967 186860 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1ccnn1 10.1016/j.bmcl.2009.04.016
9910346 64386 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL1818901 64386 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
57522468 76026 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCNC(C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059511 76026 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCNC(C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
57521365 2567 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
8587 2567 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
CHEMBL2059420 2567 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 O=C(c1ccc(cc1)OCC1CC1)Nc1ccc2c(c1C)ncc(c2)[C@H](N1CCCC1)C 10.1021/jm300167z
71730392 130757 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 391 9 1 6 3.1 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccccc3)cc2=O)c(C)c1 nan
CHEMBL3686821 130757 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 391 9 1 6 3.1 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccccc3)cc2=O)c(C)c1 nan
71730393 130758 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 419 8 1 7 2.2 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686822 130758 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 419 8 1 7 2.2 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
71730531 130765 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686829 130765 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44394763 66702 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 349 8 2 4 4.5 CC(C)c1ccc(CNCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
CHEMBL187162 66702 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 349 8 2 4 4.5 CC(C)c1ccc(CNCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
44394683 66857 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 313 6 2 5 3.4 CC(CNCc1ccsc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL187847 66857 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 313 6 2 5 3.4 CC(CNCc1ccsc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394591 122130 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 6 2 6 3.4 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL360393 122130 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 6 2 6 3.4 Nc1ccc2cccc(OCCCNc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
44394676 123101 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 297 6 2 5 3.0 CC(CNCc1ccoc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL361878 123101 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 297 6 2 5 3.0 CC(CNCc1ccoc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394866 123817 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 397 9 2 4 4.9 CCCNc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363683 123817 0 None - 0 Human 8.0 pIC50 = 8 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 397 9 2 4 4.9 CCCNc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.034
11647458 81572 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 421 4 1 6 3.5 O=C(NC1CCN(Cc2ccc3ncoc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216524 81572 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 421 4 1 6 3.5 O=C(NC1CCN(Cc2ccc3ncoc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
44417925 81038 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 532 7 2 4 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NC(=O)c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215981 81038 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 532 7 2 4 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NC(=O)c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
22018919 141016 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 7 1 3 5.7 CCCN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL384848 141016 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 7 1 3 5.7 CCCN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
25115854 60432 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761101 60432 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70691736 73239 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 541 6 1 7 4.8 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017741 73239 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 541 6 1 7 4.8 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
57845728 121911 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 428 4 1 2 6.0 O=C(C#Cc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600971 121911 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 428 4 1 2 6.0 O=C(C#Cc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
122184694 121961 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 473 10 2 6 4.3 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCC(NC(C)=O)CC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601035 121961 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 473 10 2 6 4.3 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCC(NC(C)=O)CC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
122184706 121974 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 460 10 1 6 4.4 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601047 121974 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 460 10 1 6 4.4 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
89798657 122006 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 377 8 0 6 2.8 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601303 122006 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 377 8 0 6 2.8 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
59835853 121834 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 431 5 0 4 4.4 CN1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600392 121834 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 431 5 0 4 4.4 CN1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
60130301 121880 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 452 7 1 2 6.2 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600813 121880 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 452 7 1 2 6.2 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2015.05.077
59835871 121944 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cn3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601014 121944 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cn3)nc2)cc1 10.1016/j.bmcl.2015.05.077
9866552 80075 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 receptor expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-MCH from human MCHR1 receptor expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 415 6 2 3 5.8 CN(C)CC1CCc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc2C1 10.1016/j.bmcl.2012.08.025
CHEMBL2147476 80075 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 receptor expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-MCH from human MCHR1 receptor expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 415 6 2 3 5.8 CN(C)CC1CCc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc2C1 10.1016/j.bmcl.2012.08.025
11646818 165660 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 391 5 1 6 4.0 COc1ccc2nccc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
CHEMBL426666 165660 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 391 5 1 6 4.0 COc1ccc2nccc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
20817846 138154 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 407 5 1 4 4.8 Cn1c(=O)cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL377884 138154 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 407 5 1 4 4.8 Cn1c(=O)cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44407967 74128 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202854 74128 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
45271134 193446 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 547 5 1 4 6.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCn2cccc2C1c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL550068 193446 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 547 5 1 4 6.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCn2cccc2C1c1ccccc1 10.1016/j.bmcl.2009.05.066
11166395 93827 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 433 6 2 7 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cccc5nsnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250327 93827 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 433 6 2 7 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cccc5nsnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
90666095 108827 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 557 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
CHEMBL3218998 108827 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 557 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Cc4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
70693734 73115 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 528 8 1 7 5.1 Cc1nc(N2CCC(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016726 73115 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 528 8 1 7 5.1 Cc1nc(N2CCC(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
49865927 16003 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 511 9 2 5 6.2 O=C(Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1)C1CC1 10.1016/j.bmcl.2010.07.086
CHEMBL1224152 16003 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 511 9 2 5 6.2 O=C(Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1)C1CC1 10.1016/j.bmcl.2010.07.086
16072132 80002 0 None - 1 Human 8.0 pIC50 = 8 Binding
Inhibition of MCHR1Inhibition of MCHR1
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL214629 80002 0 None - 1 Human 8.0 pIC50 = 8 Binding
Inhibition of MCHR1Inhibition of MCHR1
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
10344176 66834 4 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm040762v
CHEMBL187756 66834 4 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm040762v
44397202 66873 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 398 6 1 6 2.8 COc1cc(OC)cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187916 66873 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 398 6 1 6 2.8 COc1cc(OC)cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
44390730 63971 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 414 5 2 6 3.7 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C#N)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181099 63971 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 414 5 2 6 3.7 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C#N)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44403548 70034 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 465 8 3 5 4.3 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(Cl)ccc3NCc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.06.089
CHEMBL194531 70034 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 465 8 3 5 4.3 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(Cl)ccc3NCc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.06.089
44403523 70061 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 474 9 2 7 3.7 CC(C)OCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL194583 70061 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 474 9 2 7 3.7 CC(C)OCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403498 70719 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 437 8 2 6 3.6 COc1ccc(NCC2CC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL195255 70719 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 437 8 2 6 3.6 COc1ccc(NCC2CC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403506 70775 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 464 8 2 5 4.8 COc1ccc(CNc2ncc(Cl)cc2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.06.089
CHEMBL195511 70775 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 464 8 2 5 4.8 COc1ccc(CNc2ncc(Cl)cc2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.06.089
10025637 65238 0 None - 0 Human 8.0 pIC50 = 8 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL183215 65238 0 None - 0 Human 8.0 pIC50 = 8 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
44413474 166894 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 580 5 1 3 8.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(Cc3ccccc3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL429895 166894 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 580 5 1 3 8.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(Cc3ccccc3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
12020151 193508 0 None - 1 Human 7.0 pIC50 = 7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
CHEMBL550545 193508 0 None - 1 Human 7.0 pIC50 = 7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
44405431 71592 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 368 4 2 3 4.9 Cc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1C 10.1016/j.bmcl.2005.08.049
CHEMBL197283 71592 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 368 4 2 3 4.9 Cc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1C 10.1016/j.bmcl.2005.08.049
44394644 65790 0 None - 0 Human 7.0 pIC50 = 7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 307 6 2 4 3.4 CC(CNCc1ccccc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184087 65790 0 None - 0 Human 7.0 pIC50 = 7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 307 6 2 4 3.4 CC(CNCc1ccccc1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394890 130917 0 None - 0 Human 7.0 pIC50 = 7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 299 6 2 4 3.4 CC(CNCC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL369116 130917 0 None - 0 Human 7.0 pIC50 = 7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 299 6 2 4 3.4 CC(CNCC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11562129 70718 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195250 70718 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
60169181 87321 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 491 9 0 7 4.9 COc1ccc(Sc2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337728 87321 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 491 9 0 7 4.9 COc1ccc(Sc2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
54582961 60301 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 519 10 1 5 6.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760243 60301 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 519 10 1 5 6.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCc2nc3ccc(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2011.02.046
89691143 138772 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792529 138772 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
21108099 67800 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 440 6 0 3 4.9 CC(=O)N1CCc2ccc(OCCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914860 67800 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 440 6 0 3 4.9 CC(=O)N1CCc2ccc(OCCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
18436118 74517 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 414 4 1 3 5.2 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccccc2)CC1 10.1021/jm201596h
CHEMBL2031723 74517 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 414 4 1 3 5.2 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccccc2)CC1 10.1021/jm201596h
23022589 74523 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 453 6 1 3 6.5 CCc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031729 74523 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 453 6 1 3 6.5 CCc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
11633862 178578 1 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 453 8 1 5 4.3 COc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL472195 178578 1 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 453 8 1 5 4.3 COc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
10050565 75338 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204801 75338 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44403527 126641 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 477 8 2 8 3.2 COc1ccc(NCc2cncn2C)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL365734 126641 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 477 8 2 8 3.2 COc1ccc(NCc2cncn2C)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403538 135575 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 470 8 3 6 4.0 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ncccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL373235 135575 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 470 8 3 6 4.0 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ncccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
44418001 141160 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 331 5 2 3 4.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385639 141160 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 331 5 2 3 4.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417822 80146 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 4 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214936 80146 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 4 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
71717085 87340 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 454 7 0 6 4.3 COc1cc(N2Cc3ccc(-c4ccc(C#N)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337747 87340 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 454 7 0 6 4.3 COc1cc(N2Cc3ccc(-c4ccc(C#N)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
71717701 87354 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 429 7 0 5 4.4 COc1cc(N2Cc3ccc(-c4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337761 87354 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 429 7 0 5 4.4 COc1cc(N2Cc3ccc(-c4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
25115619 60428 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 438 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761097 60428 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 438 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
21939900 64353 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3cccc(-c4ccccc4)c3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818780 64353 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3cccc(-c4ccccc4)c3)ccc2C1 10.1016/j.bmc.2011.07.038
90666251 108860 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 596 7 1 5 7.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C(F)(F)F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219260 108860 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 596 7 1 5 7.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C(F)(F)F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
70693737 73143 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 516 7 2 7 4.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016780 73143 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 516 7 2 7 4.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
45269335 194779 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 388 4 1 6 3.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563156 194779 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 388 4 1 6 3.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
44562522 192939 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 493 7 2 4 5.7 O=C(COc1ccc(F)c(F)c1)N[C@H]1CC[C@@H](Nc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL529450 192939 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 493 7 2 4 5.7 O=C(COc1ccc(F)c(F)c1)N[C@H]1CC[C@@H](Nc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
71716478 87341 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 7 0 5 4.7 COc1cc(N2Cc3ccc(-c4ccccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337748 87341 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 7 0 5 4.7 COc1cc(N2Cc3ccc(-c4ccccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44397303 66492 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 7 1 6 2.8 COc1cc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc(OC)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186160 66492 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 7 1 6 2.8 COc1cc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc(OC)c1 10.1016/j.bmcl.2005.05.023
155528494 170773 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 518 7 1 2 7.0 Cc1ccc(CN2CCC(Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c(C)c1 10.1016/j.bmcl.2019.126741
CHEMBL4461504 170773 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 518 7 1 2 7.0 Cc1ccc(CN2CCC(Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c(C)c1 10.1016/j.bmcl.2019.126741
11776033 66821 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.4 CCCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL187702 66821 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.4 CCCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70693810 73263 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 578 8 2 7 3.9 Cc1nc(N2CCC(NS(=O)(=O)N(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017765 73263 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 578 8 2 7 3.9 Cc1nc(N2CCC(NS(=O)(=O)N(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44407966 75527 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 455 8 1 6 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(Oc4ccccc4)nc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204912 75527 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 455 8 1 6 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(Oc4ccccc4)nc3)cc12 10.1016/j.bmcl.2005.10.066
11605260 70277 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.1 Cc1cc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2nc1N(C)CCN(C)C 10.1021/jm050103y
CHEMBL195022 70277 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.1 Cc1cc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2nc1N(C)CCN(C)C 10.1021/jm050103y
44402535 165498 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1016/j.bmcl.2005.03.114
CHEMBL425744 165498 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1016/j.bmcl.2005.03.114
44442058 93908 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 355 7 2 5 3.8 COc1ccc2nc(NCCCNC(=O)c3ccsc3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250728 93908 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 355 7 2 5 3.8 COc1ccc2nc(NCCCNC(=O)c3ccsc3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
49866089 16054 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 481 7 1 4 6.6 Cc1nc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2[nH]1 10.1016/j.bmcl.2010.07.086
CHEMBL1224389 16054 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 481 7 1 4 6.6 Cc1nc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2[nH]1 10.1016/j.bmcl.2010.07.086
44403499 70758 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 479 8 2 6 4.8 COc1ccc(NCC2CCCCC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL195435 70758 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 479 8 2 6 4.8 COc1ccc(NCC2CCCCC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
70693792 73186 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 422 4 2 5 4.2 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017589 73186 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 422 4 2 5 4.2 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
10399674 65774 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 246 5 1 4 2.6 CCOCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL184001 65774 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 246 5 1 4 2.6 CCOCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11569340 71291 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 486 8 0 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(N(C)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196360 71291 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 486 8 0 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(N(C)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11677806 185417 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 505 7 0 4 5.7 CN(C(=O)COc1cccc(Cl)c1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL487040 185417 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 505 7 0 4 5.7 CN(C(=O)COc1cccc(Cl)c1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
70685396 73198 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 498 5 2 5 5.7 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017601 73198 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 498 5 2 5 5.7 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
71226697 128645 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670637 128645 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
71730920 130692 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 416 8 0 5 4.2 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686755 130692 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 416 8 0 5 4.2 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759545 130709 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 430 8 0 5 4.6 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686772 130709 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 430 8 0 5 4.6 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730390 130754 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 9 1 7 3.0 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686818 130754 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 9 1 7 3.0 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
91759570 130756 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 433 8 1 7 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686820 130756 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 433 8 1 7 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44417897 140881 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 3 2 6 3.2 O=C(NC1CCN(C2CCc3cc4oc(=O)[nH]c4cc32)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL384111 140881 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 3 2 6 3.2 O=C(NC1CCN(C2CCc3cc4oc(=O)[nH]c4cc32)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.061
70689612 73242 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 539 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017744 73242 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 539 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
71816518 137743 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770706 137743 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
21062999 64272 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
CHEMBL1817681 64272 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
122184562 121883 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 487 8 1 3 4.9 CC(=O)NC1CCN(Cc2ccc(CCN(C)C(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600816 121883 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 487 8 1 3 4.9 CC(=O)NC1CCN(Cc2ccc(CCN(C)C(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
9978378 121940 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 400 5 0 2 5.8 Clc1ccc(-c2ccc(C#Cc3ccc(CCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601010 121940 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 400 5 0 2 5.8 Clc1ccc(-c2ccc(C#Cc3ccc(CCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
89702226 138770 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792516 138770 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
57391028 67728 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914634 67728 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57401510 67733 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 481 7 1 3 5.3 CCNC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914639 67733 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 481 7 1 3 5.3 CCNC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
56589628 67792 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914852 67792 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
11328029 76162 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL206081 76162 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
45271908 193851 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 423 5 1 3 6.2 CCCc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL554287 193851 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 423 5 1 3 6.2 CCCc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
23120582 194602 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 451 5 2 4 5.6 O=C(Nc1ccc2nc(C3CC3)c(CO)n2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL562074 194602 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 451 5 2 4 5.6 O=C(Nc1ccc2nc(C3CC3)c(CO)n2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
45273802 193155 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 564 8 2 5 6.0 Cc1cc(C)n(CC(NC(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)c2ccccc2)n1 10.1016/j.bmcl.2009.05.066
CHEMBL539475 193155 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 564 8 2 5 6.0 Cc1cc(C)n(CC(NC(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)c2ccccc2)n1 10.1016/j.bmcl.2009.05.066
45487385 195157 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cn1 10.1016/j.bmcl.2009.07.023
CHEMBL565834 195157 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cn1 10.1016/j.bmcl.2009.07.023
45487356 196145 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 440 12 0 4 5.0 CCCN(CCF)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL572300 196145 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 440 12 0 4 5.0 CCCN(CCF)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
90666094 108826 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 546 7 1 5 6.7 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3218997 108826 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 546 7 1 5 6.7 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
90666262 108872 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)nc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219271 108872 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)nc3)CC2)c1 10.1039/C1MD00015B
11605775 15850 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223708 15850 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
127031338 138529 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from MCHR1 (unknown origin) expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from MCHR1 (unknown origin) expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccc(Cl)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
CHEMBL3786375 138529 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from MCHR1 (unknown origin) expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from MCHR1 (unknown origin) expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 466 6 0 6 4.7 O=C(c1nnc(-c2ccc(Cl)cc2)o1)N1CCC(Oc2ccc(CN3CCCC3)cc2)CC1 10.1021/acs.jmedchem.5b01654
49801837 138468 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 432 6 0 7 2.5 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(COC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3785663 138468 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 432 6 0 7 2.5 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(COC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
123471111 138595 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 464 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCOCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787028 138595 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 464 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCOCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
49801838 138627 22 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 462 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(COC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787394 138627 22 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 462 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(COC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11563017 80635 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215418 80635 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44405481 71491 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 364 4 2 5 3.7 Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL196972 71491 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 364 4 2 5 3.7 Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
89690237 137683 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ncc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770135 137683 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ncc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
54580457 60240 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760059 60240 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
117816753 138794 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3792764 138794 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
89691057 138928 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 433 7 0 5 5.7 CCCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794238 138928 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 433 7 0 5 5.7 CCCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
18436095 74522 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 455 6 1 4 5.9 COc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
CHEMBL2031728 74522 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 455 6 1 4 5.9 COc1c(NC(=O)c2ccc(-c3ccc(F)cc3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm201596h
11592199 15928 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(OC(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223887 15928 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(OC(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
49865868 15985 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 460 7 2 5 6.1 Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224079 15985 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 460 7 2 5 6.1 Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44397009 66411 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 372 4 1 4 3.5 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.05.023
CHEMBL185843 66411 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 372 4 1 4 3.5 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.05.023
44397310 66960 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 354 5 1 2 4.2 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.05.023
CHEMBL188401 66960 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 354 5 1 2 4.2 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.05.023
44403471 140799 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 372 4 1 4 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.06.089
CHEMBL383567 140799 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 372 4 1 4 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.06.089
23567394 60534 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2019.126741
CHEMBL176230 60534 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2019.126741
10420382 165741 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 202 3 1 3 2.6 CCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL427153 165741 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 202 3 1 3 2.6 CCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44417866 80122 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3cccc(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214843 80122 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3cccc(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417827 80675 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 347 5 3 4 4.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215586 80675 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 347 5 3 4 4.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417996 165539 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 455 8 1 3 6.7 CCCc1cc(N(CC)CC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL425979 165539 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 455 8 1 3 6.7 CCCc1cc(N(CC)CC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
59135474 91083 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403867 91083 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
16192241 48457 4 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 384 6 1 3 4.1 COc1ccc(CN2CCCC(CNC(=O)c3ccc(F)cc3)C2)c(C)c1C 10.1016/j.bmcl.2019.126741
CHEMBL1558309 48457 4 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 384 6 1 3 4.1 COc1ccc(CN2CCCC(CNC(=O)c3ccc(F)cc3)C2)c(C)c1C 10.1016/j.bmcl.2019.126741
44394966 122433 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 460 10 2 4 5.5 CCN(CC)CCN(C)C(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL360811 122433 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 460 10 2 4 5.5 CCN(CC)CCN(C)C(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
11605260 70277 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 1 5 5.1 Cc1cc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2nc1N(C)CCN(C)C 10.1021/jm050103y
CHEMBL195022 70277 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 1 5 5.1 Cc1cc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2nc1N(C)CCN(C)C 10.1021/jm050103y
45272006 193558 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 506 6 3 4 5.4 O=C(Nc1ccc(Cl)cc1CO)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL550943 193558 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 506 6 3 4 5.4 O=C(Nc1ccc(Cl)cc1CO)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
44562501 185406 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 489 7 1 4 4.8 O=C(COc1cccc(Cl)c1)N[C@H]1[C@@H]2CN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)C[C@@H]21 10.1016/j.bmcl.2008.07.079
CHEMBL487022 185406 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 489 7 1 4 4.8 O=C(COc1cccc(Cl)c1)N[C@H]1[C@@H]2CN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)C[C@@H]21 10.1016/j.bmcl.2008.07.079
70695930 73256 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 6 2 6 4.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(NS(C)(=O)=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017758 73256 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 6 2 6 4.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(NS(C)(=O)=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
45268637 194493 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 502 8 2 5 4.7 CC(C)C(Cn1ccnc1)NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL561344 194493 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 502 8 2 5 4.7 CC(C)C(Cn1ccnc1)NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
49865929 16005 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 502 8 2 6 5.3 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224154 16005 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 502 8 2 6 5.3 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44562562 173776 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2ncc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL455143 173776 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2ncc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
11518159 134725 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL372570 134725 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
3410248 70738 5 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 430 7 1 4 5.3 CCCCc1ccc(C(=O)Nc2ccc3nc(N4CCN(CC)CC4)cc(C)c3c2)cc1 10.1021/jm050103y
CHEMBL195350 70738 5 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 430 7 1 4 5.3 CCCCc1ccc(C(=O)Nc2ccc3nc(N4CCN(CC)CC4)cc(C)c3c2)cc1 10.1021/jm050103y
11973916 140952 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 6 1 7 2.8 COc1ccc2c(=O)cc(C(=O)NCC3CCN(Cc4ccc5c(c4)OCO5)C3)oc2c1 10.1021/jm060683e
CHEMBL384458 140952 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 6 1 7 2.8 COc1ccc2c(=O)cc(C(=O)NCC3CCN(Cc4ccc5c(c4)OCO5)C3)oc2c1 10.1021/jm060683e
22254632 123564 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 3 1 4 2.2 Nc1ccc2cccc(OCC3CCOC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL363311 123564 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 3 1 4 2.2 Nc1ccc2cccc(OCC3CCOC3)c2n1 10.1016/j.bmcl.2004.07.032
91759549 130718 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 449 8 0 6 4.1 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686781 130718 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 449 8 0 6 4.1 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
70683286 73193 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 458 6 2 6 4.3 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017596 73193 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 458 6 2 6 4.3 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
70689520 73104 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 521 6 1 6 4.8 Cc1nc(N2CCN(C(=O)C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016715 73104 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 521 6 1 6 4.8 Cc1nc(N2CCN(C(=O)C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70683241 73141 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 504 7 2 7 4.6 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016779 73141 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 504 7 2 7 4.6 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
46899582 16756 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 600 13 4 7 3.4 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253627 16756 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 600 13 4 7 3.4 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
45267849 194448 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 470 8 1 4 5.4 CC(CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.bmcl.2019.126741
CHEMBL561092 194448 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 470 8 1 4 5.4 CC(CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.bmcl.2019.126741
44442059 93909 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 5.1 COc1ccc2nc(N[C@H]3CC[C@H](N(C)Cc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250729 93909 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 5.1 COc1ccc2nc(N[C@H]3CC[C@H](N(C)Cc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
91759566 130748 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 509 8 0 6 4.8 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686812 130748 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 509 8 0 6 4.8 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730391 130755 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 433 8 1 7 2.6 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686819 130755 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 433 8 1 7 2.6 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44417921 80698 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215662 80698 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
10310161 96621 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 429 7 1 3 5.8 CCCc1cc(N(C)C)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL267319 96621 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 429 7 1 3 5.8 CCCc1cc(N(C)C)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
22018896 141150 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 428 5 2 4 4.4 NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385612 141150 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 428 5 2 4 4.4 NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
57392549 69286 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)c(Cl)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934837 69286 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)c(Cl)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
89689924 137791 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 449 5 0 5 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Br)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771307 137791 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 449 5 0 5 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Br)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
52917999 60305 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 504 8 1 5 4.6 COc1ccc([C@H]2CN(CCC3CCS(=O)(=O)CC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760247 60305 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 504 8 1 5 4.6 COc1ccc([C@H]2CN(CCC3CCS(=O)(=O)CC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
59835799 121949 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601019 121949 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.077
23593474 64357 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818784 64357 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
21062998 64369 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818798 64369 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
21939915 64370 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818799 64370 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
21940008 64379 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818809 64379 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
57399741 67732 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 468 6 0 4 5.4 COC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914638 67732 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 468 6 0 4 5.4 COC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11419337 165597 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
CHEMBL426292 165597 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
44410876 75737 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 482 8 1 7 5.0 CCCCCn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL205760 75737 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 482 8 1 7 5.0 CCCCCn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44410944 76684 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 456 4 1 5 5.3 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207257 76684 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 456 4 1 5 5.3 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
10025899 76697 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 433 4 1 6 4.2 Cn1c(=O)nc(NC2CCN(Cc3ccc4ncccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207308 76697 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 433 4 1 6 4.2 Cn1c(=O)nc(NC2CCN(Cc3ccc4ncccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11973800 81146 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2cccc(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL216225 81146 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2cccc(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
44143492 192843 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 376 5 2 3 4.2 CN(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL526647 192843 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 376 5 2 3 4.2 CN(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
57522948 76020 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 458 7 1 5 4.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCN(C)CC3)cnc12 10.1021/jm300167z
CHEMBL2059423 76020 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 458 7 1 5 4.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCN(C)CC3)cnc12 10.1021/jm300167z
53322554 56397 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccccc2Cl)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642473 56397 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2ccccc2Cl)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
53320117 56413 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 390 7 0 5 3.9 CN1CCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642491 56413 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 390 7 0 5 3.9 CN1CCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
90666266 108876 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cnccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219275 108876 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cnccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
23022509 76013 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 433 8 1 4 5.3 Cc1c(NC(=O)CCCC(=O)c2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059415 76013 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 433 8 1 4 5.3 Cc1c(NC(=O)CCCC(=O)c2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
18436119 76014 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059416 76014 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
57521366 76027 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059512 76027 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
44407629 168078 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL436320 168078 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
45487653 197319 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibition of mouse MCH1R receptorInhibition of mouse MCH1R receptor
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585664 197319 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibition of mouse MCH1R receptorInhibition of mouse MCH1R receptor
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
11419337 165597 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL426292 165597 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
10041636 122666 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL361305 122666 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
44417838 81171 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216342 81171 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccccc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
60168913 87334 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 477 8 0 5 5.0 COc1cc(N2Cc3ccc(Cc4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337741 87334 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 477 8 0 5 5.0 COc1cc(N2Cc3ccc(Cc4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
57397816 69260 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 464 7 1 5 4.8 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)ccc3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934811 69260 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 464 7 1 5 4.8 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)ccc3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
89690573 137771 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 359 5 0 5 3.9 CCc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3771000 137771 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 359 5 0 5 3.9 CCc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
89690573 137771 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 359 5 0 5 3.9 CCc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3771000 137771 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 359 5 0 5 3.9 CCc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
89691019 138850 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793343 138850 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45267724 194444 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 477 5 2 4 3.4 CC(=O)NC1CCN(C(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL561083 194444 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 477 5 2 4 3.4 CC(=O)NC1CCN(C(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C1 10.1016/j.bmcl.2009.05.066
11561155 190304 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 435 7 1 4 4.6 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccccn3)cc2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL518515 190304 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 435 7 1 4 4.6 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccccn3)cc2)CC1 10.1016/j.bmcl.2008.07.079
46902024 16905 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1O[C@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254968 16905 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1O[C@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44397560 67373 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 382 5 1 5 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)ccc1C 10.1016/j.bmcl.2005.05.023
CHEMBL190775 67373 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 382 5 1 5 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)ccc1C 10.1016/j.bmcl.2005.05.023
57396293 67720 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4cccc(C)c4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914626 67720 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4cccc(C)c4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44390748 64006 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 537 5 1 6 5.1 CN(C)c1nc(NC2CCN(C(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181251 64006 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 537 5 1 6 5.1 CN(C)c1nc(NC2CCN(C(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44417994 81340 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 444 6 2 5 3.7 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(CN3CCNCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
CHEMBL216407 81340 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 444 6 2 5 3.7 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(CN3CCNCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
70691721 73194 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 478 6 2 5 5.3 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017597 73194 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 478 6 2 5 5.3 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44403501 69292 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 458 7 2 5 5.0 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCc1ccco1 10.1016/j.bmcl.2005.06.089
CHEMBL193489 69292 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 458 7 2 5 5.0 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCc1ccco1 10.1016/j.bmcl.2005.06.089
44393379 64952 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 445 5 1 5 4.4 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL182886 64952 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 445 5 1 5 4.4 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
45270302 193739 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 436 4 2 4 3.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC[C@H](O)C1 10.1016/j.bmcl.2009.05.066
CHEMBL552224 193739 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 436 4 2 4 3.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC[C@H](O)C1 10.1016/j.bmcl.2009.05.066
44573964 178068 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 483 7 0 4 4.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1 10.1016/j.bmcl.2009.04.016
CHEMBL467668 178068 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 483 7 0 4 4.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1 10.1016/j.bmcl.2009.04.016
44407951 75009 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 459 8 2 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CNc3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203804 75009 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 459 8 2 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CNc3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2005.10.066
44562523 186169 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 478 6 1 5 5.0 O=C(COc1cccc(Cl)c1)N1CCC(Nc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL488887 186169 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 478 6 1 5 5.0 O=C(COc1cccc(Cl)c1)N1CCC(Nc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
44417902 80645 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 449 5 1 6 4.0 CCc1nc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL215457 80645 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 449 5 1 6 4.0 CCc1nc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc2o1 10.1016/j.bmcl.2006.11.065
155527803 170694 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 596 6 1 5 6.9 CC(C)S(=O)(=O)CN1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL4460423 170694 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 596 6 1 5 6.9 CC(C)S(=O)(=O)CN1CCC(=C(c2ccc(-c3cccc(C#N)c3)cc2)c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)CC1 10.1016/j.bmcl.2019.126741
71226697 128645 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670637 128645 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
71730130 130736 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 539 9 1 7 4.0 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686800 130736 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 539 9 1 7 4.0 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730132 130738 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 9 1 7 3.7 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686802 130738 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 9 1 7 3.7 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730395 130762 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 3.2 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686826 130762 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 3.2 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
71730529 130763 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 3.4 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686827 130763 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 3.4 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
71730530 130764 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686828 130764 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44417894 80157 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 1 3 4.9 CN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214984 80157 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 1 3 4.9 CN(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417973 140931 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 5 1 4 4.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CO4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL384362 140931 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 5 1 4 4.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CO4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417823 165208 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 401 6 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL424721 165208 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 401 6 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417956 96190 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from rat MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from rat MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL263686 96190 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from rat MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from rat MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
11648240 71102 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196196 71102 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
122184701 121969 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 437 8 1 5 4.8 OC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601042 121969 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 437 8 1 5 4.8 OC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
122184702 121970 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 433 10 1 6 4.5 OCC1CCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601043 121970 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 433 10 1 6 4.5 OCC1CCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
52917998 60293 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760234 60293 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
89798658 121998 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 376 8 0 5 3.4 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601295 121998 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 376 8 0 5 3.4 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
56680348 64375 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 5 1 2 6.1 CC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818805 64375 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 5 1 2 6.1 CC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
89691096 138934 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794306 138934 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11973799 82036 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 410 5 1 5 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL217593 82036 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 410 5 1 5 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
44407860 75055 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204082 75055 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
45271095 193549 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 514 5 1 3 6.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1c1ccc(F)cc1 10.1016/j.bmcl.2009.05.066
CHEMBL550876 193549 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 514 5 1 3 6.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1c1ccc(F)cc1 10.1016/j.bmcl.2009.05.066
23022499 74482 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 407 5 1 3 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccccc2)cc1 10.1021/jm201596h
CHEMBL2031577 74482 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 407 5 1 3 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccccc2)cc1 10.1021/jm201596h
44442120 93802 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 443 6 2 4 6.4 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc(Cl)c(Cl)c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250123 93802 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 443 6 2 4 6.4 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc(Cl)c(Cl)c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11505089 193129 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 8 1 4 6.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL538936 193129 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 8 1 4 6.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
49866035 16039 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 498 8 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224305 16039 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 498 8 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
57522950 76022 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 9 3 5 4.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCCO)cnc12 10.1021/jm300167z
CHEMBL2059425 76022 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 9 3 5 4.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCCO)cnc12 10.1021/jm300167z
24952418 91072 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 398 4 1 4 5.0 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403856 91072 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 398 4 1 4 5.0 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
56598130 138607 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 408 7 0 7 2.7 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787134 138607 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 408 7 0 7 2.7 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
44407875 74697 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203558 74697 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44413326 79438 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 469 5 1 4 6.3 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C#N)ccc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL212254 79438 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 469 5 1 4 6.3 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C#N)ccc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
44394946 64929 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 519 8 2 4 6.0 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2004.07.077
CHEMBL182847 64929 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 519 8 2 4 6.0 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2004.07.077
44417867 140969 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 349 5 2 3 4.6 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384550 140969 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 349 5 2 3 4.6 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
71718318 87348 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 455 8 0 5 5.0 C=Cc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337755 87348 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 455 8 0 5 5.0 C=Cc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
89690622 137795 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771336 137795 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
117798780 138848 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4nc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793312 138848 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4nc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117798680 138834 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)n4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793142 138834 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)n4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117798688 138925 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 407 6 0 5 5.1 CCCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
CHEMBL3794208 138925 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 407 6 0 5 5.1 CCCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
45268527 194778 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 411 4 2 4 4.8 O=C(Nc1ccc2nc(CO)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL563147 194778 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 411 4 2 4 4.8 O=C(Nc1ccc2nc(CO)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
155569743 85618 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
CHEMBL2308118 85618 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
23593471 64360 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 460 6 1 2 6.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(-c5ccccc5)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818787 64360 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 460 6 1 2 6.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(-c5ccccc5)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
44394861 65866 1 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 426 10 3 5 3.6 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(C)=O)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184454 65866 1 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 426 10 3 5 3.6 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(C)=O)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44413138 138352 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 583 6 1 4 7.1 CS(=O)(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL378261 138352 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 583 6 1 4 7.1 CS(=O)(=O)c1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(F)c(C(F)(F)F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
10377914 122645 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 260 5 1 4 3.0 COC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL361288 122645 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 260 5 1 4 3.0 COC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11974126 141409 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 490 5 1 7 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(OC(F)(F)F)ccc2o1 10.1021/jm060683e
CHEMBL387219 141409 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 490 5 1 7 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(OC(F)(F)F)ccc2o1 10.1021/jm060683e
91759553 130721 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 409 9 1 6 3.3 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(F)cn3)cc2=O)c(C)c1 nan
CHEMBL3686784 130721 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 409 9 1 6 3.3 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(F)cn3)cc2=O)c(C)c1 nan
11386451 71513 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 498 8 3 6 4.7 NC(=O)C1CCN(CCn2ncc3cc(NC(=O)Nc4ccc(Oc5ccccc5)cc4)ccc32)CC1 10.1016/j.bmcl.2005.03.114
CHEMBL197054 71513 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 498 8 3 6 4.7 NC(=O)C1CCN(CCn2ncc3cc(NC(=O)Nc4ccc(Oc5ccccc5)cc4)ccc32)CC1 10.1016/j.bmcl.2005.03.114
44143500 192340 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 458 7 2 3 6.3 CCN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL522242 192340 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 458 7 2 3 6.3 CCN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
57402226 69046 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C(F)(F)F)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1933085 69046 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C(F)(F)F)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
10332650 65848 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.9 Nc1ccc2cccc(OC3CCCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184394 65848 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.9 Nc1ccc2cccc(OC3CCCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
22254571 66620 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 268 3 1 3 3.6 Nc1ccc2cccc(OCC3CC4CCC3C4)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186750 66620 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 268 3 1 3 3.6 Nc1ccc2cccc(OCC3CC4CCC3C4)c2n1 10.1016/j.bmcl.2004.07.032
45270297 193673 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 436 4 2 4 3.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC[C@@H](O)C1 10.1016/j.bmcl.2009.05.066
CHEMBL551826 193673 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 436 4 2 4 3.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC[C@@H](O)C1 10.1016/j.bmcl.2009.05.066
90666255 108864 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 494 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C(C)C)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219264 108864 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 494 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C(C)C)cc3)CC2)c1 10.1039/C1MD00015B
44442098 93601 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)c(C)cc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248881 93601 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)c(C)cc2c1 10.1016/j.bmcl.2007.05.034
86695567 130696 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 539 9 1 7 4.1 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686759 130696 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 539 9 1 7 4.1 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
86695568 130697 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686760 130697 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
91759567 130751 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 510 8 0 7 4.2 Cc1cc(CN2CCCC2C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)nc1=O nan
CHEMBL3686815 130751 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 510 8 0 7 4.2 Cc1cc(CN2CCCC2C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)nc1=O nan
57392546 69265 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccc(F)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934816 69265 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccc(F)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57397817 69266 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccc(Cl)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934817 69266 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccc(Cl)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
52918016 60307 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 555 11 1 5 5.1 COc1ccc([C@H]2CN(CCCN(C)S(=O)(=O)c3ccccc3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760250 60307 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 555 11 1 5 5.1 COc1ccc([C@H]2CN(CCCN(C)S(=O)(=O)c3ccccc3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
1314 3657 18 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
9865843 3657 18 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
CHEMBL178707 3657 18 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
56666754 64368 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 7 1 2 6.9 CCN(CC)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818797 64368 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 7 1 2 6.9 CCN(CC)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
89702566 138785 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792707 138785 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44407870 75546 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204968 75546 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
90666265 108875 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cccnc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219274 108875 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5cccnc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
127030368 138435 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 448 8 0 7 3.1 CN(Cc1ccc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)cc1)CC1(C)COC1 10.1021/acs.jmedchem.5b01654
CHEMBL3785343 138435 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 448 8 0 7 3.1 CN(Cc1ccc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)cc1)CC1(C)COC1 10.1021/acs.jmedchem.5b01654
56597851 138518 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 422 7 0 7 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(C)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786272 138518 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 422 7 0 7 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(C)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11641948 79916 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214280 79916 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
16659197 96622 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccn3)cc1)C2 10.1016/j.bmcl.2019.126741
CHEMBL267320 96622 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 399 5 0 3 4.4 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccccn3)cc1)C2 10.1016/j.bmcl.2019.126741
44395019 65890 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184560 65890 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44395076 66646 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 549 10 3 5 5.7 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL186894 66646 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 549 10 3 5 5.7 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.07.077
89691440 137626 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3cnc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769460 137626 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3cnc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
21062991 64355 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818782 64355 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
56673714 64374 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 502 5 1 3 7.5 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)C(=O)OC(C)(C)C 10.1016/j.bmc.2011.07.038
CHEMBL1818804 64374 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 502 5 1 3 7.5 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)C(=O)OC(C)(C)C 10.1016/j.bmc.2011.07.038
117798675 138817 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 393 5 0 5 4.7 CCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
CHEMBL3793016 138817 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 393 5 0 5 4.7 CCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
89690973 138821 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4Cl)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793051 138821 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4Cl)cc3=O)cc21 10.1016/j.bmc.2016.04.011
89691284 138879 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 6 0 5 4.4 Cn1c(CC2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793827 138879 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 6 0 5 4.4 Cn1c(CC2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45273638 194059 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 354 4 1 4 4.5 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccccn2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL557317 194059 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 354 4 1 4 4.5 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccccn2)cc1 10.1016/j.bmcl.2009.06.101
49865789 15949 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 506 9 2 6 5.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C#N)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223967 15949 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 506 9 2 6 5.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C#N)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
11678370 136029 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373886 136029 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
11284878 63997 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(N[C@H]2CC[C@@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181217 63997 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(N[C@H]2CC[C@@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44401626 70995 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 558 7 2 6 5.2 O=S(=O)(NCC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL195810 70995 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 558 7 2 6 5.2 O=S(=O)(NCC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
44403539 165716 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 517 10 2 8 4.1 CC(C)OCCNc1ncc(-c2ccncc2)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL427006 165716 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 517 10 2 8 4.1 CC(C)OCCNc1ncc(-c2ccncc2)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
45271246 193527 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 406 7 1 4 4.0 O=C(NCC1CC1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL550683 193527 0 None - 1 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 406 7 1 4 4.0 O=C(NCC1CC1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2019.126741
57397818 69280 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 526 8 1 6 6.0 CSc1ccc(-c2nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c3ccccc23)cc1 10.1016/j.bmcl.2011.10.111
CHEMBL1934830 69280 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 526 8 1 6 6.0 CSc1ccc(-c2nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c3ccccc23)cc1 10.1016/j.bmcl.2011.10.111
70681114 73097 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 1 6 4.3 Cc1nc(N2CCN(C(=O)CC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016708 73097 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 1 6 4.3 Cc1nc(N2CCN(C(=O)CC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
45271647 193502 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 504 8 0 4 4.6 CN(CCC(=O)N1CCCC1)C(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL550513 193502 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 504 8 0 4 4.6 CN(CCC(=O)N1CCCC1)C(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
45273406 194717 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 525 6 2 4 6.0 O=C(NCc1c(O)cc(Cl)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL562788 194717 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 525 6 2 4 6.0 O=C(NCc1c(O)cc(Cl)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
9804849 67102 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL189118 67102 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70687550 73252 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 576 6 2 7 3.6 Cc1nc(N2CCC(N3CCNS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017754 73252 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 576 6 2 7 3.6 Cc1nc(N2CCC(N3CCNS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
45271549 193890 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 644 8 0 6 5.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(C(=O)OC(C)(C)C)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL555055 193890 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 644 8 0 6 5.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(C(=O)OC(C)(C)C)CC1=O 10.1016/j.bmcl.2009.03.102
49866034 16038 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 498 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(C(=O)CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224304 16038 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 498 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(C(=O)CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11190261 62898 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cn(CCN3CCCC3)nc2c1 10.1021/jm0490890
CHEMBL179091 62898 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cn(CCN3CCCC3)nc2c1 10.1021/jm0490890
44394983 65933 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 446 9 3 4 4.7 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL184720 65933 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 446 9 3 4 4.7 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
11974129 80687 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 422 4 2 7 2.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(O)cc2o1 10.1021/jm060683e
CHEMBL215631 80687 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 422 4 2 7 2.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(O)cc2o1 10.1021/jm060683e
44394825 65821 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 415 8 1 4 5.9 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCC5CC5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL184277 65821 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 415 8 1 4 5.9 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCC5CC5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
60150483 73190 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 462 5 2 5 5.0 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017593 73190 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 462 5 2 5 5.0 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
10408758 121893 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 401 8 0 5 4.3 CCN(CC)CCOc1ccc(C#Cc2ncc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600826 121893 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 401 8 0 5 4.3 CCN(CC)CCOc1ccc(C#Cc2ncc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
71226268 128649 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.2 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CC2(CCOC2)C1 nan
CHEMBL3670641 128649 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.2 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CC2(CCOC2)C1 nan
71225855 128651 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.3 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CC2(CCCO2)C1 nan
CHEMBL3670643 128651 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.3 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CC2(CCCO2)C1 nan
91759571 130759 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686823 130759 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 1 7 3.0 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
10025637 65238 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL183215 65238 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 429 5 1 4 5.2 Cc1cc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
57399486 69267 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 544 8 1 6 6.0 COc1ccc2c(-c3ccc(Cl)cc3)nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c2c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934818 69267 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 544 8 1 6 6.0 COc1ccc2c(-c3ccc(Cl)cc3)nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c2c1 10.1016/j.bmcl.2011.10.111
122184698 121965 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 437 8 1 5 4.8 O[C@@H]1CCCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)C1 10.1016/j.bmcl.2015.05.074
CHEMBL3601039 121965 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 437 8 1 5 4.8 O[C@@H]1CCCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)C1 10.1016/j.bmcl.2015.05.074
122184704 121972 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 462 9 1 5 4.4 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(F)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601045 121972 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 462 9 1 5 4.4 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(F)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
89702233 137661 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 445 5 0 6 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769762 137661 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 445 5 0 6 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
122184565 121886 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600819 121886 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
44438748 148953 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 527 10 1 7 4.5 CC(C)CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL394639 148953 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 527 10 1 7 4.5 CC(C)CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
22348066 165266 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 4 2 7 4.3 N#Cc1c(O)nc2ccc(Cl)cc2c1NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2006.02.044
CHEMBL424865 165266 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 436 4 2 7 4.3 N#Cc1c(O)nc2ccc(Cl)cc2c1NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2006.02.044
10024175 187444 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 5 2 5 4.3 CC(C)N(C)c1nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497619 187444 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 5 2 5 4.3 CC(C)N(C)c1nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
7735 531 8 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 10.1016/j.bmcl.2007.05.034
9927967 531 8 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 10.1016/j.bmcl.2007.05.034
CHEMBL400679 531 8 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 341 8 2 5 4.2 COc1ccc2c(c1)c(C)cc(n2)NCCCNCc1cscc1 10.1016/j.bmcl.2007.05.034
11419776 93803 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 459 7 2 5 6.0 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cccc(OC(F)(F)F)c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250124 93803 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 459 7 2 5 6.0 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cccc(OC(F)(F)F)c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
90666264 108874 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 582 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5c(F)cc(F)cc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219273 108874 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 582 7 1 5 7.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5c(F)cc(F)cc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
70691652 73110 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016721 73110 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70685338 73118 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(NC(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016729 73118 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 7 2 6 4.4 Cc1nc(N2CCC(NC(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
49865928 16004 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 513 9 2 5 6.4 CC(C)C(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224153 16004 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 513 9 2 5 6.4 CC(C)C(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
71227161 128652 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3670644 128652 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
56597988 138610 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 426 7 0 7 2.8 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787170 138610 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 426 7 0 7 2.8 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)C)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11641948 79916 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214280 79916 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
44408027 74702 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 490 11 2 6 5.2 CCN(CC)CCNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2005.10.066
CHEMBL203586 74702 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 490 11 2 6 5.2 CCN(CC)CCNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2005.10.066
44390710 64243 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 457 5 2 5 4.9 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C(F)(F)F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181632 64243 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 457 5 2 5 4.9 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(C(F)(F)F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
71227171 128659 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 526 8 0 8 4.0 COc1cc(CN2CCCC23COC3)ccc1OC1CN(C(=O)c2nnc(-c3ccc(C(F)F)cc3)o2)C1 nan
CHEMBL3670650 128659 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 526 8 0 8 4.0 COc1cc(CN2CCCC23COC3)ccc1OC1CN(C(=O)c2nnc(-c3ccc(C(F)F)cc3)o2)C1 nan
44417967 81871 0 None 35 2 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 459 7 0 4 4.5 O=C(c1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2019.126741
CHEMBL217196 81871 0 None 35 2 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 459 7 0 4 4.5 O=C(c1ccc(F)cc1)c1cc2n(c1)CCN(CCc1ccc(CN3CCCCC3)cc1)C2=O 10.1016/j.bmcl.2019.126741
44417895 165291 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 513 6 0 3 5.2 CN(C)C(=O)[C@@H]1CCCN1Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2019.126741
CHEMBL424895 165291 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 513 6 0 3 5.2 CN(C)C(=O)[C@@H]1CCCN1Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2019.126741
10434776 125848 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL365055 125848 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44405430 71590 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 370 5 2 4 4.3 COc1cccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c1 10.1016/j.bmcl.2005.08.049
CHEMBL197281 71590 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 370 5 2 4 4.3 COc1cccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c1 10.1016/j.bmcl.2005.08.049
70691722 73203 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 478 6 2 6 4.6 CC(=O)CC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017606 73203 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 478 6 2 6 4.6 CC(=O)CC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
89690292 137647 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 372 5 0 6 3.6 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769682 137647 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 372 5 0 6 3.6 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
127025096 137686 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 419 5 0 5 5.2 Cc1cn(-c2ccc3nc(C4CC4)c(C)n3c2)c(=O)cc1OCc1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01704
CHEMBL3770175 137686 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 419 5 0 5 5.2 Cc1cn(-c2ccc3nc(C4CC4)c(C)n3c2)c(=O)cc1OCc1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01704
89691440 137626 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3cnc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769460 137626 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3cnc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
127029759 138822 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 404 5 0 4 5.4 Cn1c(C2CC2)cc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.013
CHEMBL3793053 138822 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 404 5 0 4 5.4 Cn1c(C2CC2)cc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.013
53325163 56393 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 438 10 0 6 3.9 O=c1cc(OCCOc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642469 56393 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 438 10 0 6 3.9 O=c1cc(OCCOc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
45270803 193399 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 11 1 5 5.4 COCC(O)CN(Cc1ccc(F)cc1)C(=O)CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL549636 193399 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 11 1 5 5.4 COCC(O)CN(Cc1ccc(F)cc1)C(=O)CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1 10.1016/j.bmcl.2009.05.067
90666257 108866 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 560 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(C(C)c3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219266 108866 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 560 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(C(C)c3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
70695853 73107 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 426 5 2 6 3.6 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016718 73107 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 426 5 2 6 3.6 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11553648 73116 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 425 5 2 6 3.5 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016727 73116 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 425 5 2 6 3.5 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
70685347 73147 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3ccc(F)cc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016784 73147 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3ccc(F)cc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11526824 15929 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 549 9 2 5 6.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223888 15929 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 549 9 2 5 6.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(C(F)(F)F)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
44562461 188303 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 414 7 1 6 3.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccon3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL507549 188303 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 414 7 1 6 3.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccon3)c2)CC1 10.1016/j.bmcl.2008.07.079
44390499 129122 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 579 8 2 6 6.0 CN(C)c1nc(NCC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL367355 129122 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 579 8 2 6 6.0 CN(C)c1nc(NCC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11284878 70083 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL194602 70083 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
11656044 140593 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 486 9 1 5 5.3 CCc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL382755 140593 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 486 9 1 5 5.3 CCc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
122184673 121921 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 411 8 1 5 5.0 N#Cc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600981 121921 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 411 8 1 5 5.0 N#Cc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
45267746 194752 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 486 7 3 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL563005 194752 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 486 7 3 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2009.05.066
44438739 93489 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 511 8 1 6 3.9 O=C(NC1CCN(Cc2ccc(OCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL248295 93489 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 511 8 1 6 3.9 O=C(NC1CCN(Cc2ccc(OCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
16742745 121957 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 376 9 1 5 4.3 COc1ccc(-c2ccc(CCCNc3ccc(CN(C)C)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601031 121957 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 376 9 1 5 4.3 COc1ccc(-c2ccc(CCCNc3ccc(CN(C)C)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
44397716 167740 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 398 6 1 6 2.8 COc1ccc(OC)c(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL434156 167740 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 398 6 1 6 2.8 COc1ccc(OC)c(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
11662564 132990 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 459 8 1 5 5.0 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370820 132990 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 459 8 1 5 5.0 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44395012 65947 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 402 9 3 4 3.6 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184797 65947 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 402 9 3 4 3.6 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
11974345 79915 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccc(F)cc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL214278 79915 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccc(F)cc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
22266820 203326 21 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 174 1 1 3 1.8 COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL77072 203326 21 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 174 1 1 3 1.8 COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
71226964 128646 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670638 128646 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 nan
71730663 122020 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 470 8 0 7 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3601376 122020 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 470 8 0 7 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
91759548 130717 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 458 8 1 6 3.4 Cc1cc(CN2CC3CC(C2)C3O)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686780 130717 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 458 8 1 6 3.4 Cc1cc(CN2CC3CC(C2)C3O)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71732079 130735 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686799 130735 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
91759579 130774 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 466 8 0 7 4.0 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686837 130774 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 466 8 0 7 4.0 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
9804849 67102 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL189118 67102 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11496739 69964 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194459 69964 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
44403742 71360 5 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 430 6 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL196573 71360 5 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 430 6 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
10388797 71400 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196667 71400 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
25114068 60447 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 477 7 1 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C#N)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761116 60447 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 477 7 1 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C#N)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70685407 73238 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 491 5 1 6 4.5 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017740 73238 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 491 5 1 6 4.5 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
9980157 121912 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 430 6 1 2 6.6 O=C(/C=C/c1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600972 121912 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 430 6 1 2 6.6 O=C(/C=C/c1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
71730663 122020 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 470 8 0 7 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601376 122020 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 470 8 0 7 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
89691096 138934 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794306 138934 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11653882 140761 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
CHEMBL383359 140761 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
20817763 140040 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 522 5 1 7 4.2 Cn1c(=O)c(C(=O)N2CCCC2)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL381335 140040 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 522 5 1 7 4.2 Cn1c(=O)c(C(=O)N2CCCC2)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
9804849 67102 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL189118 67102 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
53318595 56415 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 405 10 0 5 4.2 CCN(CC)CCN(C)c1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642493 56415 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 405 10 0 5 4.2 CCN(CC)CCN(C)c1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
44442134 93745 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 433 6 2 7 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc5nsnc5c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL249716 93745 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 433 6 2 7 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc5nsnc5c4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
56597542 138409 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 480 8 0 9 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCOCC5)c(OC)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785102 138409 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 480 8 0 9 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCOCC5)c(OC)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11627530 75542 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204952 75542 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407836 74901 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203699 74901 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11562138 70159 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL194697 70159 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
60168915 87335 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 4.6 COc1cc(N2Cc3ccc(Cc4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337742 87335 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 4.6 COc1cc(N2Cc3ccc(Cc4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89690973 138821 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4Cl)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793051 138821 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4Cl)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45270157 193389 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 437 4 1 5 5.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4cnc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL549583 193389 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 437 4 1 5 5.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4cnc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
9895868 12775 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL1188966 12775 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL537846 12775 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
10231050 63988 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 551 6 2 6 5.5 CN(C)c1nc(NC2CCC(NC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181184 63988 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 551 6 2 6 5.5 CN(C)c1nc(NC2CCC(NC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
9895868 69224 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=8)Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=8)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193438 69224 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=8)Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=8)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
44403492 70270 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 448 8 2 5 4.3 COc1ccc(CN2CCC(NC(=O)c3cc(Cl)cnc3NCC(C)C)CC2)cc1F 10.1016/j.bmcl.2005.06.089
CHEMBL195006 70270 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 448 8 2 5 4.3 COc1ccc(CN2CCC(NC(=O)c3cc(Cl)cnc3NCC(C)C)CC2)cc1F 10.1016/j.bmcl.2005.06.089
44403490 71297 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 451 7 2 5 3.1 COc1ccc(NS(C)(=O)=O)c(C(=O)NC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL196362 71297 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 451 7 2 5 3.1 COc1ccc(NS(C)(=O)=O)c(C(=O)NC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2005.06.089
18436043 76010 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 465 8 1 5 5.0 CCCCS(=O)(=O)c1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059412 76010 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 465 8 1 5 5.0 CCCCS(=O)(=O)c1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
44397605 67154 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 384 5 1 6 3.2 COc1cccc(OC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189508 67154 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 384 5 1 6 3.2 COc1cccc(OC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
44408093 140354 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 533 10 1 6 6.4 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3nc(-c4ccccc4)c(-c4ccccc4)o3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL382126 140354 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 533 10 1 6 6.4 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3nc(-c4ccccc4)c(-c4ccccc4)o3)cc12 10.1016/j.bmcl.2005.10.066
49865870 15987 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 8 1 5 6.3 CC(=O)N(C)c1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224081 15987 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 8 1 5 6.3 CC(=O)N(C)c1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44394854 66565 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 3 1 3 2.9 CC1CC1COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186547 66565 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 3 1 3 2.9 CC1CC1COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11189610 165213 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 430 5 1 5 4.6 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL424728 165213 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 430 5 1 5 4.6 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
44438741 93378 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 496 9 1 6 4.5 COC(C)(C)CCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL247688 93378 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 496 9 1 6 4.5 COC(C)(C)CCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
44417937 141014 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 451 4 2 6 2.7 O=C1COc2cc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)ccc2N1 10.1016/j.bmcl.2006.11.065
CHEMBL384844 141014 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 451 4 2 6 2.7 O=C1COc2cc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)ccc2N1 10.1016/j.bmcl.2006.11.065
44388409 165675 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human MCH-R1-stimulated [Ca2+] influxInhibitory concentration against human MCH-R1-stimulated [Ca2+] influx
ChEMBL 371 5 2 3 4.4 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL426777 165675 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human MCH-R1-stimulated [Ca2+] influxInhibitory concentration against human MCH-R1-stimulated [Ca2+] influx
ChEMBL 371 5 2 3 4.4 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
46902025 16920 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1O[C@@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1255050 16920 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1O[C@@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
70681198 73211 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 509 9 3 7 3.5 Cc1nc(NCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017614 73211 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 509 9 3 7 3.5 Cc1nc(NCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44562524 186170 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 8 1 5 4.1 Cc1cccc(OCC(=O)NCC2CN(Cc3ccn(-c4ccc(C(C)(C)C)cn4)c3)C2)c1 10.1016/j.bmcl.2008.07.079
CHEMBL488890 186170 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 8 1 5 4.1 Cc1cccc(OCC(=O)NCC2CN(Cc3ccn(-c4ccc(C(C)(C)C)cn4)c3)C2)c1 10.1016/j.bmcl.2008.07.079
11973802 81701 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL216680 81701 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
71731806 121999 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 390 8 0 5 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3601296 121999 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 390 8 0 5 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71732078 122003 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 469 8 0 6 3.8 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3601300 122003 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 469 8 0 6 3.8 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71731045 130740 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 8 0 6 4.4 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686804 130740 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 8 0 6 4.4 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730788 130788 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 470 9 1 7 3.3 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686851 130788 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 470 9 1 7 3.3 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
44417886 141154 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 6 1 3 6.5 CCCc1cc(N2CCCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385619 141154 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 6 1 3 6.5 CCCc1cc(N2CCCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
122184670 121913 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 8 0 2 7.1 CN(CCCc1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600973 121913 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 8 0 2 7.1 CN(CCCc1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
89702233 137661 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 445 5 0 6 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769762 137661 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 445 5 0 6 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
71731806 121999 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 390 8 0 5 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601296 121999 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 390 8 0 5 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O 10.1016/j.bmcl.2015.05.065
71732078 122003 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 469 8 0 6 3.8 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601300 122003 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 469 8 0 6 3.8 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
21062990 64354 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818781 64354 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
9844702 64361 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818788 64361 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
59835874 121951 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2cnc(C#Cc3ccc(OCCN4CCCC4)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601020 121951 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2cnc(C#Cc3ccc(OCCN4CCCC4)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
89691044 138936 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(Cl)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794345 138936 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(Cl)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
89690957 138782 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792697 138782 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
57399741 67732 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 468 6 0 4 5.4 COC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914638 67732 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 468 6 0 4 5.4 COC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11692293 93013 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 534 8 2 6 3.5 O=C(NCCN1CCCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL246050 93013 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 534 8 2 6 3.5 O=C(NCCN1CCCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
23120580 194357 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 439 4 2 4 5.5 CC(C)(O)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL560334 194357 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 439 4 2 4 5.5 CC(C)(O)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
44407667 74042 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
CHEMBL202563 74042 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
45267735 194633 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 548 8 2 5 5.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cc1cnccn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL562285 194633 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 548 8 2 5 5.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cc1cnccn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
45271673 193694 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 1 4 7.1 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccncc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL551924 193694 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 1 4 7.1 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccncc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.05.067
44250210 194263 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 521 8 2 4 5.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1cnc[nH]1 10.1016/j.bmcl.2009.05.067
CHEMBL559535 194263 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 521 8 2 4 5.7 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1cnc[nH]1 10.1016/j.bmcl.2009.05.067
70685337 73111 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 8 2 7 4.6 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016722 73111 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 8 2 7 4.6 Cc1nc(N2CCC(C(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
57401248 69262 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 518 7 1 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4c(c3=O)CCCC4)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934813 69262 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 518 7 1 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4c(c3=O)CCCC4)CC2)c1 10.1016/j.bmcl.2011.10.111
89702355 137659 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 388 5 0 6 3.6 Cc1c(CC#N)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769758 137659 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 388 5 0 6 3.6 Cc1c(CC#N)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
117798692 138803 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3792893 138803 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
18436109 76011 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 9 1 4 6.2 CCCCCC(=O)c1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059413 76011 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 9 1 4 6.2 CCCCCC(=O)c1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
44417017 79955 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 497 9 2 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)[C@@H]2C[C@H]2c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214442 79955 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 497 9 2 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)[C@@H]2C[C@H]2c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11620005 81030 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215958 81030 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
44397309 67173 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189602 67173 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
44390707 129133 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccccc3F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL367359 129133 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccccc3F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11973802 81701 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.065
CHEMBL216680 81701 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.065
44417825 141106 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 6 1 3 5.4 CCCc1cc(N)c2cc(N(C)C(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385361 141106 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 6 1 3 5.4 CCCc1cc(N)c2cc(N(C)C(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
70681197 73200 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 464 5 2 5 5.2 Cc1nc(N2CCC(O)(C(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017603 73200 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 464 5 2 5 5.2 Cc1nc(N2CCC(O)(C(C)C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44417991 82007 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 431 5 1 5 4.1 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCOCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
CHEMBL217459 82007 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 431 5 1 5 4.1 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCOCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
90666252 108861 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 553 7 1 6 6.5 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C#N)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219261 108861 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 553 7 1 6 6.5 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(C#N)cc4)cc3)CC2)c1 10.1039/C1MD00015B
45271663 194886 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 6 0 5 3.9 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCOC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.067
CHEMBL563884 194886 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 6 0 5 3.9 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCOC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.067
155516078 169472 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3cccc4c3OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4442916 169472 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3cccc4c3OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
10262766 66630 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 216 3 1 3 3.0 CCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186818 66630 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 216 3 1 3 3.0 CCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11568782 71540 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 8 1 5 4.8 CN(C)CCN(C)c1ccc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL197145 71540 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 8 1 5 4.8 CN(C)CCN(C)c1ccc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
46899578 16784 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253872 16784 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
11974030 154725 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(C(F)(F)F)cc2o1 10.1021/jm060683e
CHEMBL402868 154725 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(C(F)(F)F)cc2o1 10.1021/jm060683e
11211551 166699 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 6 4.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C)nc4C)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL429301 166699 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 6 4.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C)nc4C)C3)nc2c1 10.1016/j.bmcl.2007.05.034
57399487 69279 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 510 8 1 6 5.3 COc1ccc(-c2nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c3ccccc23)cc1 10.1016/j.bmcl.2011.10.111
CHEMBL1934829 69279 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 510 8 1 6 5.3 COc1ccc(-c2nn(CCCN3CCC(c4cccc(NC(C)=O)c4)CC3)c(=O)c3ccccc23)cc1 10.1016/j.bmcl.2011.10.111
71226697 128645 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670637 128645 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC6(CCOC6)C5)cc4)C3)o2)cc1 nan
71225842 128650 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 474 6 0 7 3.6 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CCC2(CCOC2)C1 nan
CHEMBL3670642 128650 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 474 6 0 7 3.6 Cc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CCC2(CCOC2)C1 nan
71730131 130737 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686801 130737 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730264 130747 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 483 9 1 6 4.3 Cc1cc(CNC(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686811 130747 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 483 9 1 6 4.3 Cc1cc(CNC(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730265 130749 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 497 9 0 6 4.6 Cc1cc(CN(C)C(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686813 130749 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 497 9 0 6 4.6 Cc1cc(CN(C)C(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
91759569 130753 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 0 7 3.4 Cc1cc(CN2CCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)nc1=O nan
CHEMBL3686817 130753 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 0 7 3.4 Cc1cc(CN2CCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)nc1=O nan
71730534 130776 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 426 9 1 7 3.2 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
CHEMBL3686839 130776 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 426 9 1 7 3.2 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
91759586 130785 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686848 130785 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71730789 130789 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686852 130789 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71714121 122021 3 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat MCH-R1Binding affinity to rat MCH-R1
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601377 122021 3 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat MCH-R1Binding affinity to rat MCH-R1
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
10173787 82012 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 7 2 3 6.8 CCCc1cc(NC2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217480 82012 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 7 2 3 6.8 CCCc1cc(NC2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417903 141224 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 455 6 1 3 6.6 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCCC1 10.1016/j.bmcl.2006.08.006
CHEMBL386046 141224 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 455 6 1 3 6.6 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCCC1 10.1016/j.bmcl.2006.08.006
89691044 138936 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(Cl)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794345 138936 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(Cl)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
18436126 74514 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 422 5 1 4 5.5 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cn2)cc1 10.1021/jm201596h
CHEMBL2031720 74514 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 422 5 1 4 5.5 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cn2)cc1 10.1021/jm201596h
53318592 56394 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 376 6 0 5 3.5 CN1CCC(Oc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc2)C1 10.1016/j.bmc.2010.12.002
CHEMBL1642470 56394 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 376 6 0 5 3.5 CN1CCC(Oc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc2)C1 10.1016/j.bmc.2010.12.002
53326457 56412 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 404 7 0 5 4.3 CN1CCCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642490 56412 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 404 7 0 5 4.3 CN1CCCCC1COc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
10050565 75338 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204801 75338 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44408117 139016 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379693 139016 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44408108 139271 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 462 9 2 6 4.4 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379886 139271 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 462 9 2 6 4.4 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44417979 81720 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 433 4 2 3 6.2 Nc1cc(-c2ccccc2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL216817 81720 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 433 4 2 3 6.2 Nc1cc(-c2ccccc2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
44417940 81268 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 7 2 3 5.8 CCCc1cc(N)c2cc(NCCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216372 81268 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 7 2 3 5.8 CCCc1cc(N)c2cc(NCCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11539632 70202 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 70202 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
71718910 87329 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccc(C)c(C)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337736 87329 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccc(C)c(C)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89702355 137659 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 388 5 0 6 3.6 Cc1c(CC#N)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769758 137659 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 388 5 0 6 3.6 Cc1c(CC#N)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
53324269 56411 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 392 8 0 5 4.1 CN(C)CC(C)(C)Oc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642489 56411 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 392 8 0 5 4.1 CN(C)CC(C)(C)Oc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
70687471 73106 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 410 5 1 5 4.6 Cc1nc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016717 73106 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 410 5 1 5 4.6 Cc1nc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11691995 15927 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 511 10 2 6 5.7 COc1cccc(Cn2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223886 15927 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 511 10 2 6 5.7 COc1cccc(Cn2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)c1 10.1016/j.bmcl.2010.07.086
45270416 194968 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 470 8 1 4 5.8 CCC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.bmcl.2019.126741
CHEMBL564409 194968 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 470 8 1 4 5.8 CCC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.bmcl.2019.126741
44403733 72084 3 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 420 4 1 4 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)/C=C/c3cccc(Cl)c3)cc12 10.1021/jm050103y
CHEMBL198823 72084 3 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 420 4 1 4 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)/C=C/c3cccc(Cl)c3)cc12 10.1021/jm050103y
70693795 73197 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 497 6 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(N4CCCC4)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017600 73197 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 497 6 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(N4CCCC4)cc3)cc12 10.1016/j.bmcl.2012.03.049
45178545 172636 6 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 408 5 0 4 4.1 COc1cc(OC)cc(C(=O)N2CCC3(CCCN(Cc4cccc(C)c4)C3)C2)c1 10.1016/j.bmcl.2019.126741
CHEMBL4522986 172636 6 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 408 5 0 4 4.1 COc1cc(OC)cc(C(=O)N2CCC3(CCCN(Cc4cccc(C)c4)C3)C2)c1 10.1016/j.bmcl.2019.126741
44394987 65882 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 444 11 3 6 3.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cc(OC)cc(OC)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184534 65882 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 444 11 3 6 3.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cc(OC)cc(OC)c2)cc1OC 10.1016/j.bmcl.2004.07.077
90666259 108868 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 580 7 1 5 7.4 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3Cl)CC2)c1 10.1039/C1MD00015B
CHEMBL3219268 108868 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 580 7 1 5 7.4 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3Cl)CC2)c1 10.1039/C1MD00015B
44402420 140828 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1016/j.bmcl.2005.03.114
CHEMBL383798 140828 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1016/j.bmcl.2005.03.114
122184703 121971 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 421 8 1 5 4.3 OC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(F)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601044 121971 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 421 8 1 5 4.3 OC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(F)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
137655884 158200 0 None - 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 419 5 0 4 3.9 O=C1COc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm5013243
CHEMBL4093980 158200 0 None - 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 419 5 0 4 3.9 O=C1COc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm5013243
11974035 82197 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Br)ccc2o1 10.1021/jm060683e
CHEMBL217925 82197 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Br)ccc2o1 10.1021/jm060683e
137655884 158200 0 None - 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 419 5 0 4 3.9 O=C1COc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm5013243
CHEMBL4093980 158200 0 None - 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 419 5 0 4 3.9 O=C1COc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm5013243
71226964 128646 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 nan
CHEMBL3670638 128646 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 nan
71225843 128647 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.3 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCC4(CCOC4)C3)cc2)C1 nan
CHEMBL3670639 128647 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.3 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCC4(CCOC4)C3)cc2)C1 nan
71731803 130691 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686754 130691 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730919 130705 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 376 8 1 5 3.3 CNCc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)c(C)c1 nan
CHEMBL3686768 130705 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 376 8 1 5 3.3 CNCc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)c(C)c1 nan
71730266 130750 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 483 9 0 6 4.2 CCN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686814 130750 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 483 9 0 6 4.2 CCN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
91759568 130752 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 498 10 0 7 4.0 CCN(CC)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)nc2=O)c(C)c1 nan
CHEMBL3686816 130752 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 498 10 0 7 4.0 CCN(CC)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)nc2=O)c(C)c1 nan
71731048 130782 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 452 8 0 7 3.7 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686845 130782 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 452 8 0 7 3.7 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
71730662 130783 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 498 8 1 8 2.3 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686846 130783 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 498 8 1 8 2.3 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL4115910 211194 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL None None None None nan
44417939 81956 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 451 4 2 6 2.7 O=C1COc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc2N1 10.1016/j.bmcl.2006.11.065
CHEMBL217233 81956 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 451 4 2 6 2.7 O=C1COc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc2N1 10.1016/j.bmcl.2006.11.065
9804849 67102 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL189118 67102 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
25114723 60454 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 548 8 1 4 7.9 O=C(Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1)c1ccccc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761124 60454 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 548 8 1 4 7.9 O=C(Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1)c1ccccc1 10.1016/j.bmcl.2011.02.099
89690396 137711 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770396 137711 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
23593468 64358 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818785 64358 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
89702226 138770 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792516 138770 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)s4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
57401507 67721 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(C)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914627 67721 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(C)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57392835 67794 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 444 6 0 4 5.1 CC(=O)N1CCc2sc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914854 67794 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 444 6 0 4 5.1 CC(=O)N1CCc2sc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
44143493 187453 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 390 6 2 3 4.6 CCN(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497647 187453 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 390 6 2 3 4.6 CCN(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
45273801 194022 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 536 8 2 5 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1cccn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL556927 194022 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 536 8 2 5 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1cccn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
44573823 192621 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 491 6 0 3 6.1 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)N(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
CHEMBL523697 192621 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 491 6 0 3 6.1 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)N(c1ccccc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.04.016
70687477 73138 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 7 1 7 4.4 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016776 73138 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 7 1 7 4.4 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
57522949 76021 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 445 7 2 5 4.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CC[C@H](O)C3)cnc12 10.1021/jm300167z
CHEMBL2059424 76021 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 445 7 2 5 4.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CC[C@H](O)C3)cnc12 10.1021/jm300167z
9804849 67102 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL189118 67102 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11612098 69926 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 448 4 1 6 4.8 O=c1cc(NC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194292 69926 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 448 4 1 6 4.8 O=c1cc(NC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
11518384 165343 0 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 467 7 0 5 5.4 O=C1N(c2ccc(Oc3ccccc3)cc2)CCN1c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL425013 165343 0 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 467 7 0 5 5.4 O=C1N(c2ccc(Oc3ccccc3)cc2)CCN1c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
44417858 79956 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 346 5 3 4 4.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(N)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214450 79956 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 346 5 3 4 4.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(N)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
71719523 87327 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cccc(C)c4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337734 87327 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cccc(C)c4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
21940052 64365 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 385 5 0 3 5.2 CN(C)CC1CCc2cc(OC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818794 64365 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 385 5 0 3 5.2 CN(C)CC1CCc2cc(OC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
17848895 67684 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 466 5 0 3 4.7 CC(=O)N1CCc2ccc(C(=O)CCC(=O)N3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914463 67684 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 466 5 0 3 4.7 CC(=O)N1CCc2ccc(C(=O)CCC(=O)N3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44403535 71068 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 522 10 2 8 4.8 CC(C)OCCNc1ncc(-c2cccs2)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196004 71068 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 522 10 2 8 4.8 CC(C)OCCNc1ncc(-c2cccs2)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44395007 123543 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 468 8 1 6 5.4 CCN1CCCC1CNC(=O)c1ccc(-c2noc(-c3ccc(Oc4ccccc4)cc3)n2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL363264 123543 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 468 8 1 6 5.4 CCN1CCCC1CNC(=O)c1ccc(-c2noc(-c3ccc(Oc4ccccc4)cc3)n2)cc1 10.1016/j.bmcl.2004.07.077
44401591 68540 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 8 3 7 5.1 Nc1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL192266 68540 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 8 3 7 5.1 Nc1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
10377822 126290 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 5 1 3 4.0 CCC(CC)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL365459 126290 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 5 1 3 4.0 CCC(CC)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11837128 71771 5 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 360 5 1 4 4.4 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2ccccc2o1 10.1021/jm050598r
CHEMBL197849 71771 5 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 360 5 1 4 4.4 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2ccccc2o1 10.1021/jm050598r
60168916 87336 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 499 8 0 5 5.6 COc1cc(N2Cc3ccc(Cc4ccc(C(C)(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337743 87336 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 499 8 0 5 5.6 COc1cc(N2Cc3ccc(Cc4ccc(C(C)(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44407836 74901 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203699 74901 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44394999 66312 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 447 10 2 5 4.4 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL185348 66312 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 447 10 2 5 4.4 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
11440885 82045 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccccc3Cl)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL217626 82045 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccccc3Cl)cc12 10.1016/j.bmcl.2006.11.092
44403533 71097 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 469 8 3 5 4.6 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL196168 71097 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 469 8 3 5 4.6 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
44397329 66767 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 404 6 1 6 2.4 COc1cccc(S(=O)(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187447 66767 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 404 6 1 6 2.4 COc1cccc(S(=O)(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
45267709 194287 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 5 2 4 4.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.066
CHEMBL559691 194287 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 5 2 4 4.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.066
44394958 66556 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 461 11 2 5 4.8 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL186491 66556 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 461 11 2 5 4.8 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44403486 71151 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 432 6 2 4 4.7 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
CHEMBL196273 71151 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 432 6 2 4 4.7 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
11453830 63061 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2nn(CCN3CCCC3)cc2c1 10.1021/jm0490890
CHEMBL179606 63061 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2nn(CCN3CCCC3)cc2c1 10.1021/jm0490890
10466406 66001 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 3 1 3 3.2 CC(C)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL185095 66001 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 3 1 3 3.2 CC(C)C(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44394891 64869 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5ccc(Cl)cc5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL182575 64869 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5ccc(Cl)cc5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
44394726 65813 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 351 7 2 5 3.0 COc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL184243 65813 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 351 7 2 5 3.0 COc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
22018856 80180 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 6 1 3 6.2 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCC1 10.1016/j.bmcl.2006.08.006
CHEMBL215082 80180 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 6 1 3 6.2 CN(c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1)C1CCCC1 10.1016/j.bmcl.2006.08.006
22018999 80692 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 6 1 3 5.7 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL215648 80692 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 6 1 3 5.7 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417947 140967 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 411 4 2 3 5.8 Nc1cc(C2CCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
CHEMBL384547 140967 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 411 4 2 3 5.8 Nc1cc(C2CCC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.08.008
22018945 141179 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.7 CC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385748 141179 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.7 CC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44417845 141342 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386727 141342 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.4 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
25115618 60429 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 452 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761098 60429 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 452 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
9866745 121867 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 7 1 2 5.6 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600801 121867 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 7 1 2 5.6 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
11743571 121869 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 7 1 2 6.0 O=C(NCCc1ccc(CN2CCCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600803 121869 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 7 1 2 6.0 O=C(NCCc1ccc(CN2CCCCC2)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
122184557 121870 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 408 9 3 3 4.1 O=C(NCCc1ccc(CNCCO)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600804 121870 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 408 9 3 3 4.1 O=C(NCCc1ccc(CNCCO)cc1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
60130278 121873 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 496 7 1 2 6.3 O=C(NCCc1ccc(CN2CCCC2)cc1Br)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600807 121873 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 496 7 1 2 6.3 O=C(NCCc1ccc(CN2CCCC2)cc1Br)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
11592099 93056 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 554 8 2 6 3.8 O=C(NCCN1CCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(Cl)c1 10.1016/j.bmcl.2006.11.068
CHEMBL246258 93056 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 554 8 2 6 3.8 O=C(NCCN1CCCC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(Cl)c1 10.1016/j.bmcl.2006.11.068
11562138 70159 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1021/jm0512286
CHEMBL194697 70159 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1021/jm0512286
10070016 71104 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 408 4 1 7 3.4 COc1ccc2oc(O)c/c(=N\C3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
CHEMBL196208 71104 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 408 4 1 7 3.4 COc1ccc2oc(O)c/c(=N\C3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1021/jm0512286
9983233 75633 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 494 5 1 7 4.4 O=c1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL205492 75633 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 494 5 1 7 4.4 O=c1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
11683903 82003 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 454 5 1 7 3.1 COc1cc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2cc1F 10.1021/jm060683e
CHEMBL217442 82003 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 454 5 1 7 3.1 COc1cc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2cc1F 10.1021/jm060683e
11201867 98220 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 454 4 1 6 3.9 Cc1c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)oc2cc(Cl)ccc2c1=O 10.1021/jm060683e
CHEMBL277531 98220 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 454 4 1 6 3.9 Cc1c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)oc2cc(Cl)ccc2c1=O 10.1021/jm060683e
11583049 141404 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)cc2o1 10.1021/jm060683e
CHEMBL387178 141404 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)cc2o1 10.1021/jm060683e
23120572 194379 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL560474 194379 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
44407629 168078 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL436320 168078 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
18436038 76006 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059408 76006 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 8 1 4 5.6 CCCCOc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
57522947 76019 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059422 76019 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
11556070 193808 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 580 9 1 5 6.5 COc1ccc(C(NC(=O)CC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)c2ccc(F)cc2)cn1 10.1016/j.bmcl.2009.05.067
CHEMBL553196 193808 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 580 9 1 5 6.5 COc1ccc(C(NC(=O)CC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)c2ccc(F)cc2)cn1 10.1016/j.bmcl.2009.05.067
11628328 193856 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 2 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL554332 193856 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 2 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
46933537 15872 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 485 8 2 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223770 15872 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 485 8 2 5 5.8 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
57522703 76008 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059410 76008 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 8 1 4 5.6 Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
11583747 81069 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1cccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)c1 10.1016/j.bmcl.2006.07.040
CHEMBL216010 81069 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1cccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)c1 10.1016/j.bmcl.2006.07.040
11677277 141235 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.07.040
CHEMBL386117 141235 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.07.040
11598355 141259 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 490 8 3 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL386247 141259 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 490 8 3 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1C 10.1016/j.bmcl.2006.07.040
44390726 121876 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 449 7 2 7 3.9 COc1cc(OC)cc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
CHEMBL360081 121876 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 449 7 2 7 3.9 COc1cc(OC)cc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
11562138 70159 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL194697 70159 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 484 7 2 7 4.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
10047339 70047 2 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 412 4 1 6 4.3 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194564 70047 2 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 412 4 1 6 4.3 O=c1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44417962 81660 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 4 2 3 5.6 CC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216565 81660 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 4 2 3 5.6 CC(C)c1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11495754 71573 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL197245 71573 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
44573822 186872 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 505 6 0 3 6.4 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CC2)OCc2ccccc23)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL494009 186872 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 505 6 0 3 6.4 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CC2)OCc2ccccc23)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
44573821 192121 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 503 6 0 2 6.8 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL522037 192121 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 503 6 0 2 6.8 Cc1ccc(N(C(=O)N(C)CCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
10224210 62966 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 424 5 2 3 5.0 CN1CCC(CNC(=O)Nc2ccccc2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL179353 62966 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 424 5 2 3 5.0 CN1CCC(CNC(=O)Nc2ccccc2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
11353174 80170 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 536 7 1 5 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL215030 80170 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 536 7 1 5 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
44394798 123853 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 391 5 1 6 3.6 CC(Cc1ccc2c(c1)OCO2)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
CHEMBL363909 123853 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 391 5 1 6 3.6 CC(Cc1ccc2c(c1)OCO2)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
21939950 64381 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 438 6 1 3 6.0 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818811 64381 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 438 6 1 3 6.0 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
21939937 64371 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818800 64371 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 1 2 6.7 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
45267576 194947 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 402 4 1 4 5.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL564286 194947 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 402 4 1 4 5.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
18436115 74509 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cc2)cc1 10.1021/jm201596h
CHEMBL2031715 74509 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 421 5 1 3 6.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cc2)cc1 10.1021/jm201596h
44417843 81535 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 457 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(I)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216510 81535 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 457 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(I)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11511219 65789 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL184084 65789 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11496739 69964 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194459 69964 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
11655872 71358 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL196567 71358 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
11511219 65789 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL184084 65789 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44408117 139016 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379693 139016 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
21939898 64380 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 422 5 1 2 6.3 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818810 64380 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 422 5 1 2 6.3 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
44408109 75177 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204428 75177 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
57522946 76018 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059421 76018 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
57523087 1132 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
7754 1132 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
CHEMBL2059513 1132 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](c1cnc2c(c1)ccc(c2C)NC(=O)c1ccc(cc1)OCC1CC1)C 10.1021/jm300167z
44402677 71374 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 3 5 6.0 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCNC2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL196599 71374 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 3 5 6.0 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCNC2CCCC2)c1 10.1016/j.bmcl.2005.03.114
21940083 64372 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818801 64372 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 456 5 1 2 7.1 O=C(Nc1ccc2c(c1)CCC(CN1CCCCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
23120550 194921 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL564106 194921 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
57522816 76015 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.6 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3C)cnc12 10.1021/jm300167z
CHEMBL2059417 76015 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.6 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3C)cnc12 10.1021/jm300167z
10273126 60803 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 412 8 2 3 5.1 CN(C)CCC(CNC(=O)Nc1ccccc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL176548 60803 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 412 8 2 3 5.1 CN(C)CCC(CNC(=O)Nc1ccccc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2019.126741
45487640 195558 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 454 4 1 4 4.8 CC(O)(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL568361 195558 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 454 4 1 4 4.8 CC(O)(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
44469273 195871 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 394 10 1 4 4.3 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL570296 195871 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 394 10 1 4 4.3 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
44394770 123309 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 3 1 6 3.2 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL362501 123309 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 3 1 6 3.2 Nc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11583744 71365 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196581 71365 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
22251624 64366 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818795 64366 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 5 1 2 6.2 CN(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
9887476 192810 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 5 2 5 4.3 CC(C)N(C)c1nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL526083 192810 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 5 2 5 4.3 CC(C)N(C)c1nc2ccc(NC(=O)c3cnc(-c4ccc(F)cc4)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
10391177 188655 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.04.016
CHEMBL511747 188655 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.04.016
10159452 74480 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2nc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031575 74480 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2nc(CN3CCCC3)ccc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
57523086 76023 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
CHEMBL2059426 76023 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 447 9 3 5 5.0 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCC(C)(C)O)cnc12 10.1021/jm300167z
10391177 188655 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL511747 188655 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 497 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)N1CCCC1=O 10.1016/j.bmcl.2009.03.102
10310316 80693 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 6 1 3 6.1 CCCc1cc(N2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215649 80693 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 6 1 3 6.1 CCCc1cc(N2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
21939902 64373 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 471 5 1 3 5.8 CN1CCN(CC2=Cc3ccc(NC(=O)c4ccc(-c5ccc(Cl)cc5)cc4)cc3CC2)CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818802 64373 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 471 5 1 3 5.8 CN1CCN(CC2=Cc3ccc(NC(=O)c4ccc(-c5ccc(Cl)cc5)cc4)cc3CC2)CC1 10.1016/j.bmc.2011.07.038
18436075 74481 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
CHEMBL2031576 74481 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 425 5 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)cc1 10.1021/jm201596h
44417877 80710 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 6 2 3 5.5 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215696 80710 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 6 2 3 5.5 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10073934 186897 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cncn1 10.1016/j.bmcl.2009.04.016
CHEMBL494155 186897 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 481 7 0 6 3.5 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cncn1 10.1016/j.bmcl.2009.04.016
71226400 128648 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 nan
CHEMBL3670640 128648 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 nan
44413472 138149 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 586 4 1 4 8.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)c4cccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL377864 138149 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 586 4 1 4 8.1 N#Cc1cccc(-c2ccc(C(=C3CCN(C(=O)c4cccs4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
71731671 130690 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 418 8 1 6 2.8 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686753 130690 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 418 8 1 6 2.8 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730917 130702 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 436 9 0 8 3.0 COc1ccc(COc2cnn(CC(=O)c3ccc(C(C)N(C)C)cc3C)c(=O)c2)nc1 nan
CHEMBL3686765 130702 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 436 9 0 8 3.0 COc1ccc(COc2cnn(CC(=O)c3ccc(C(C)N(C)C)cc3C)c(=O)c2)nc1 nan
71730134 130741 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 511 8 1 7 3.3 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686805 130741 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 511 8 1 7 3.3 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
71730787 130787 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 540 9 1 8 3.5 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686850 130787 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 540 9 1 8 3.5 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71730792 130794 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 408 9 1 8 2.1 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
CHEMBL3686857 130794 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 408 9 1 8 2.1 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
44394922 65795 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL184116 65795 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
44394959 66859 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL187854 66859 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44417905 82046 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL217637 82046 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
44405618 71656 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1cccnc1 10.1016/j.bmcl.2005.08.049
CHEMBL197497 71656 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1cccnc1 10.1016/j.bmcl.2005.08.049
44405560 72088 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 495 5 1 9 4.6 O=C(c1cscn1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL198835 72088 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 495 5 1 9 4.6 O=C(c1cscn1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
44405646 96412 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 511 6 1 9 3.5 O=C(CN1CCOCC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL265540 96412 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 511 6 1 9 3.5 O=C(CN1CCOCC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
44405557 132217 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 489 5 1 8 4.6 O=C(c1cccnc1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL369986 132217 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 489 5 1 8 4.6 O=C(c1cccnc1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
44405612 134943 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 481 6 1 5 6.4 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4ccccc4c3)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
CHEMBL372848 134943 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 481 6 1 5 6.4 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4ccccc4c3)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
11653882 140761 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL383359 140761 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 384 4 2 5 4.0 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
10083869 65228 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL183159 65228 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
10083869 65228 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65228 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44417888 79980 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 5 2 3 4.9 CNc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214541 79980 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 5 2 3 4.9 CNc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44417857 141112 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 376 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc([N+](=O)[O-])cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385389 141112 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 376 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc([N+](=O)[O-])cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11632484 69976 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 388 7 1 4 4.2 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)ccc3c2)cc1 10.1021/jm050103y
CHEMBL194477 69976 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 388 7 1 4 4.2 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)ccc3c2)cc1 10.1021/jm050103y
60169095 87317 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 6 4.9 COc1cc(N2Cc3ccc(Sc4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337724 87317 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 6 4.9 COc1cc(N2Cc3ccc(Sc4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
57396018 69263 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 520 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccsc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934814 69263 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 520 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccsc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57394271 69264 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934815 69264 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57394272 69270 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(Cl)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934820 69270 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(Cl)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57401249 69271 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 528 7 1 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(C)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934821 69271 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 528 7 1 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(C)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57402992 69272 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 582 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(Cl)c(Cl)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934822 69272 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 582 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(Cl)c(Cl)cc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
70691725 73215 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 10 3 6 5.0 Cc1nc(NCCCC(=O)NC2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017618 73215 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 10 3 6 5.0 Cc1nc(NCCCC(=O)NC2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
122184692 121958 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 9 1 6 4.0 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCOCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601032 121958 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 9 1 6 4.0 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCOCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
16742747 121960 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 9 2 6 4.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCC(O)CC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601034 121960 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 9 2 6 4.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCC(O)CC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
89691439 137707 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770359 137707 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
10386162 121894 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 398 6 0 4 4.6 COc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600827 121894 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 398 6 0 4 4.6 COc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
10388352 121946 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 5 0 3 5.9 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3Cl)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601016 121946 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 5 0 3 5.9 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3Cl)nc2)cc1 10.1016/j.bmcl.2015.05.077
21062999 64272 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
CHEMBL1817681 64272 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 478 6 1 2 7.7 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)c1ccccc1 10.1016/j.bmc.2011.07.038
57398087 67718 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 376 6 1 3 4.2 O=C(CCCN1CCC(c2ccccc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914624 67718 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 376 6 1 3 4.2 O=C(CCCN1CCC(c2ccccc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
21108117 67798 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 424 5 1 3 4.4 O=C(CCC(=O)N1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914858 67798 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 424 5 1 3 4.4 O=C(CCC(=O)N1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCNCC2 10.1016/j.bmc.2011.09.007
44438740 93490 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 499 9 1 6 3.8 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL248296 93490 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 499 9 1 6 3.8 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
44442153 93600 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c(C#N)cccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248863 93600 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c(C#N)cccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44562545 188504 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cnc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL510193 188504 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cnc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)[nH]2)cc1 10.1016/j.bmcl.2008.07.079
11583835 73120 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016731 73120 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
57522948 76020 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 458 7 1 5 4.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCN(C)CC3)cnc12 10.1021/jm300167z
CHEMBL2059423 76020 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 458 7 1 5 4.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCN(C)CC3)cnc12 10.1021/jm300167z
44455414 96955 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2013.05.017
CHEMBL269939 96955 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2013.05.017
44397194 66632 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186825 66632 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
44407710 73577 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202095 73577 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
58646147 78660 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@@H](C)NC[C@@H]2C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL2113218 78660 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@@H](C)NC[C@@H]2C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44403493 69434 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 442 7 2 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
CHEMBL193576 69434 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 442 7 2 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
44403454 71384 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 492 6 2 6 4.1 O=C(Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccn1 10.1016/j.bmcl.2005.06.089
CHEMBL196620 71384 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 492 6 2 6 4.1 O=C(Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccn1 10.1016/j.bmcl.2005.06.089
44403522 123527 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL363169 123527 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403487 124658 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 444 7 2 6 3.9 CC(C)CNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL364522 124658 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 444 7 2 6 3.9 CC(C)CNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403507 126240 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1ncc[nH]1 10.1016/j.bmcl.2005.06.089
CHEMBL365360 126240 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1ncc[nH]1 10.1016/j.bmcl.2005.06.089
44403474 126692 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 430 6 2 6 3.7 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL365788 126692 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 430 6 2 6 3.7 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403505 133034 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 467 8 2 7 3.3 COc1ccc(NCC2CCOC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL371129 133034 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 467 8 2 7 3.3 COc1ccc(NCC2CCOC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403445 165813 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 474 8 2 7 3.8 COc1ccc(NCc2ccccn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL427542 165813 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 474 8 2 7 3.8 COc1ccc(NCc2ccccn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403468 167855 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 491 7 2 6 5.4 O=C(NC1CCN(Cc2ccc3ncccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL434934 167855 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 491 7 2 6 5.4 O=C(NC1CCN(Cc2ccc3ncccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
44403493 69434 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 442 7 2 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
CHEMBL193576 69434 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 442 7 2 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
44403523 70061 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 474 9 2 7 3.7 CC(C)OCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL194583 70061 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 474 9 2 7 3.7 CC(C)OCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403528 70186 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 472 7 2 7 3.4 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC[C@H]1CCCO1 10.1016/j.bmcl.2005.06.089
CHEMBL194731 70186 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 472 7 2 7 3.4 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC[C@H]1CCCO1 10.1016/j.bmcl.2005.06.089
44403513 133743 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
CHEMBL371700 133743 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
44394799 65907 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 347 5 1 4 4.4 CCC(c1ccccc1)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
CHEMBL184609 65907 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 347 5 1 4 4.4 CCC(c1ccccc1)N1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.035
44394948 65898 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 484 10 3 5 5.0 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(SC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184585 65898 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 484 10 3 5 5.0 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(SC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44405459 132622 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 374 4 2 3 4.9 Clc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1 10.1016/j.bmcl.2005.08.049
CHEMBL370360 132622 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 374 4 2 3 4.9 Clc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc1 10.1016/j.bmcl.2005.08.049
9895868 69224 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=3)Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=3)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193438 69224 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=3)Inhibitory activity against human wild type Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH (n=3)
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
44403477 71469 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 387 4 2 5 3.0 Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196898 71469 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 387 4 2 5 3.0 Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44424072 85183 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 402 8 1 2 5.8 Fc1ccc(-c2ccc(CNCCc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228293 85183 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 402 8 1 2 5.8 Fc1ccc(-c2ccc(CNCCc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
71719524 87343 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 5.0 CCc1ccccc1-c1ccc2c(n1)C(=O)N(c1ccc(OCCN3CCCC3)c(OC)c1)C2 10.1016/j.bmcl.2013.01.053
CHEMBL2337750 87343 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 5.0 CCc1ccccc1-c1ccc2c(n1)C(=O)N(c1ccc(OCCN3CCCC3)c(OC)c1)C2 10.1016/j.bmcl.2013.01.053
10421933 124112 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 3 1 3 3.6 CC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL364104 124112 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 3 1 3 3.6 CC(C)(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70695914 73195 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 494 7 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017598 73195 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 494 7 2 6 4.9 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44417936 81166 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 438 4 1 7 3.0 O=C(NC1CCN(Cc2ccc3oc(=O)oc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216323 81166 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 438 4 1 7 3.0 O=C(NC1CCN(Cc2ccc3oc(=O)oc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
71720121 87349 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1cccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)c1 10.1016/j.bmcl.2013.01.053
CHEMBL2337756 87349 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1cccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)c1 10.1016/j.bmcl.2013.01.053
44403473 70121 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 407 4 1 5 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1Cl 10.1016/j.bmcl.2005.06.089
CHEMBL194630 70121 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 407 4 1 5 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1Cl 10.1016/j.bmcl.2005.06.089
70689595 73199 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 476 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017602 73199 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 476 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70687536 73188 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 512 6 2 6 5.2 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017591 73188 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 512 6 2 6 5.2 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70695859 73140 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 454 6 2 6 4.4 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016778 73140 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 454 6 2 6 4.4 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
11272081 81032 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 504 7 1 5 4.7 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL215964 81032 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 504 7 1 5 4.7 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
71732074 130711 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 390 9 1 5 3.7 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)c(C)c1 nan
CHEMBL3686774 130711 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 390 9 1 5 3.7 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccccc3)cc2=O)c(C)c1 nan
71730664 130786 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686849 130786 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
91759587 130791 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 9 1 8 3.1 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686854 130791 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 9 1 8 3.1 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
44417899 141029 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 477 3 2 6 3.1 O=C1COc2cc3c(cc2N1)C(N1CCC(NC(=O)c2cc(=O)c4ccc(F)cc4o2)CC1)CC3 10.1016/j.bmcl.2006.11.061
CHEMBL384919 141029 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 477 3 2 6 3.1 O=C1COc2cc3c(cc2N1)C(N1CCC(NC(=O)c2cc(=O)c4ccc(F)cc4o2)CC1)CC3 10.1016/j.bmcl.2006.11.061
11563383 70156 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL194691 70156 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
70681216 73251 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 554 6 1 6 4.8 Cc1nc(N2CCC(N3CCN(C)C3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017753 73251 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 554 6 1 6 4.8 Cc1nc(N2CCC(N3CCN(C)C3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
122184672 121919 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 404 8 1 4 5.3 Fc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600979 121919 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 404 8 1 4 5.3 Fc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
54585863 60304 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 456 8 1 4 5.2 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760246 60304 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 456 8 1 4 5.2 COc1ccc([C@H]2CN(CCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
23593468 64358 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818785 64358 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 6 1 2 5.8 CCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
89690864 138896 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793944 138896 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45267714 194352 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 497 5 1 4 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1c1cccnc1 10.1016/j.bmcl.2009.05.066
CHEMBL560283 194352 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 497 5 1 4 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1c1cccnc1 10.1016/j.bmcl.2009.05.066
45267430 193135 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 1 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc[n+]([O-])c1 10.1016/j.bmcl.2009.05.067
CHEMBL538993 193135 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 566 8 1 4 5.8 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1ccc[n+]([O-])c1 10.1016/j.bmcl.2009.05.067
49865654 15852 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 467 8 2 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccccc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223710 15852 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 467 8 2 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccccc3)CC2)c1 10.1016/j.bmcl.2010.07.086
24952055 91075 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 515 5 2 4 6.2 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403859 91075 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 515 5 2 4 6.2 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
10070680 71750 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 418 4 1 4 5.7 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL197797 71750 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 418 4 1 4 5.7 O=c1cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44394604 124517 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 299 5 2 4 3.5 CC(CNC1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL364399 124517 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 299 5 2 4 3.5 CC(CNC1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394807 65871 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 425 4 1 5 4.0 CC(C)(C)c1ccc(S(=O)(=O)N2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL184482 65871 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 425 4 1 5 4.0 CC(C)(C)c1ccc(S(=O)(=O)N2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
44417975 141316 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 440 5 2 4 4.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CN4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL386548 141316 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 440 5 2 4 4.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CC3CN4)ccc2c1 10.1016/j.bmcl.2006.08.006
71718317 87345 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 471 9 0 5 5.3 CCCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337752 87345 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 471 9 0 5 5.3 CCCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
127025096 137686 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 419 5 0 5 5.2 Cc1cn(-c2ccc3nc(C4CC4)c(C)n3c2)c(=O)cc1OCc1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01704
CHEMBL3770175 137686 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 419 5 0 5 5.2 Cc1cn(-c2ccc3nc(C4CC4)c(C)n3c2)c(=O)cc1OCc1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01704
23593472 64359 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818786 64359 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
117798688 138925 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 407 6 0 5 5.1 CCCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
CHEMBL3794208 138925 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 407 6 0 5 5.1 CCCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
89691193 138867 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 5 0 5 4.7 Cn1c(C2CCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793700 138867 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 5 0 5 4.7 Cn1c(C2CCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44408081 74692 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 454 8 1 5 5.6 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(Oc4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203549 74692 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 454 8 1 5 5.6 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(Oc4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407934 75563 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 418 6 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3cc4ccccc4s3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205112 75563 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 418 6 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3cc4ccccc4s3)cc12 10.1016/j.bmcl.2005.10.066
25114724 60456 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 582 8 1 4 8.5 O=C(Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1)c1cccc(Cl)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761126 60456 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 582 8 1 4 8.5 O=C(Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1)c1cccc(Cl)c1 10.1016/j.bmcl.2011.02.099
70695854 73108 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 440 6 1 6 4.2 COC1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016719 73108 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 440 6 1 6 4.2 COC1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
70689527 73149 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 571 7 2 8 4.9 Cc1nc(N2CCC(O)(c3ccc(F)cn3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016786 73149 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 571 7 2 8 4.9 Cc1nc(N2CCC(O)(c3ccc(F)cn3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442062 93945 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 5 1 5 4.4 COc1ccc2nc(N3CCC(NCc4ccsc4)CC3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250926 93945 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 5 1 5 4.4 COc1ccc2nc(N3CCC(NCc4ccsc4)CC3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
44562480 185314 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cn(-c3ccc(C(F)(F)F)cc3)cn2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL486878 185314 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cn(-c3ccc(C(F)(F)F)cc3)cn2)CC1 10.1016/j.bmcl.2008.07.079
70681115 73098 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 483 7 1 7 2.9 COCC(=O)N1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016709 73098 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 483 7 1 7 2.9 COCC(=O)N1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
89790062 130701 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 512 8 1 8 2.7 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686764 130701 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 512 8 1 8 2.7 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71730918 130703 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 9 1 8 2.7 CNC(C)c1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
CHEMBL3686766 130703 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 9 1 8 2.7 CNC(C)c1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
44417873 81033 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215965 81033 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
6621104 66453 5 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 438 6 1 5 4.4 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL185997 66453 5 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 438 6 1 5 4.4 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1021/jm050103y
11634230 69816 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL194046 69816 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
122184705 121973 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 458 10 1 5 4.2 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(Cc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601046 121973 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 458 10 1 5 4.2 CC(=O)NC1CCN(Cc2ccc(OCCCc3ccc(Cc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
44193625 122019 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 456 8 0 7 2.9 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601375 122019 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 456 8 0 7 2.9 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
71714121 122021 3 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601377 122021 3 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
9844702 64361 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818788 64361 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 6 1 3 5.3 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
11510887 81843 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL217105 81843 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
44442118 93861 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 426 6 2 5 5.6 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cncc5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250530 93861 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 426 6 2 5 5.6 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cncc5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11577588 194156 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 6 2 4 5.4 O=C(NCc1ccc(Cl)cc1O)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL558442 194156 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 6 2 4 5.4 O=C(NCc1ccc(Cl)cc1O)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
90666267 108877 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 524 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc(C)c(C)n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219276 108877 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 524 7 1 5 6.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc(C)c(C)n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
11662906 73117 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 475 6 2 7 3.8 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016728 73117 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 475 6 2 7 3.8 Cc1nc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11684745 15900 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 499 9 2 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223830 15900 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 499 9 2 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44408028 140360 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 518 11 2 6 6.0 Cc1cc(NCCN(C(C)C)C(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL382161 140360 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 518 11 2 6 6.0 Cc1cc(NCCN(C(C)C)C(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70691333 77603 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 453 9 1 4 5.5 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL2096766 77603 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 453 9 1 4 5.5 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm0490890
44405487 71516 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 375 4 2 6 3.2 N#Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197059 71516 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 375 4 2 6 3.2 N#Cc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
70691723 73204 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 466 6 3 6 4.0 Cc1nc(N2CCC(O)(CCO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017607 73204 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 466 6 3 6 4.0 Cc1nc(N2CCC(O)(CCO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
21062991 64355 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818782 64355 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4cccc(Cl)c4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
69603769 73088 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 425 5 1 6 3.4 Cc1nc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016698 73088 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 425 5 1 6 3.4 Cc1nc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44403491 71408 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 458 7 3 4 4.3 COc1ccc(NC(=O)NC(C)C)c(C(=O)NC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL196686 71408 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 458 7 3 4 4.3 COc1ccc(NC(=O)NC(C)C)c(C(=O)NC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2005.06.089
44403516 69936 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2ncc[nH]2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL194342 69936 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2ncc[nH]2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
11204090 69478 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(NC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193771 69478 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(NC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
44403750 133377 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 449 6 2 5 3.8 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)CCC(=O)Nc3ccc(F)cc3)cc12 10.1021/jm050103y
CHEMBL371576 133377 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 449 6 2 5 3.8 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)CCC(=O)Nc3ccc(F)cc3)cc12 10.1021/jm050103y
70691737 73254 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 489 6 2 5 4.7 Cc1nc(N2CCC(NC(=O)C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017756 73254 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 489 6 2 5 4.7 Cc1nc(N2CCC(NC(=O)C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
70689519 73095 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 481 6 1 6 3.9 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016706 73095 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 481 6 1 6 3.9 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44562521 186168 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 479 7 2 4 5.3 O=C(COc1ccc(F)c(F)c1)N[C@H]1CC[C@H](Nc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL488886 186168 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 479 7 2 4 5.3 O=C(COc1ccc(F)c(F)c1)N[C@H]1CC[C@H](Nc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
155562407 174625 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 405 7 0 3 4.0 CN(C)Cc1ccc(CCN2CCn3cc(Cc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4571110 174625 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 405 7 0 3 4.0 CN(C)Cc1ccc(CCN2CCn3cc(Cc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
71226938 128654 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56CCOC6)cc4)C3)o2)cc1 nan
CHEMBL3670646 128654 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 490 7 0 8 3.4 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56CCOC6)cc4)C3)o2)cc1 nan
71226243 128661 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.4 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCC4(CCCO4)C3)cc2)C1 nan
CHEMBL3670652 128661 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.4 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCC4(CCCO4)C3)cc2)C1 nan
71731050 130744 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686808 130744 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 525 8 1 7 3.7 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
10389978 69256 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL193473 69256 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
21062990 64354 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818781 64354 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4Cl)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
117798744 138930 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3794256 138930 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
11713742 93117 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 552 8 2 6 4.3 O=C(CCN1CCCCC1)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL246464 93117 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 552 8 2 6 4.3 O=C(CCN1CCCCC1)Nc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
44408013 74691 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203544 74691 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
44143499 187334 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 459 6 2 4 4.7 CN1CCC(N(C)c2nc3ccc(NC(=O)CCc4ccc(C(F)(F)F)cc4)cc3[nH]2)CC1 10.1016/j.bmcl.2009.04.147
CHEMBL496815 187334 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 459 6 2 4 4.7 CN1CCC(N(C)c2nc3ccc(NC(=O)CCc4ccc(C(F)(F)F)cc4)cc3[nH]2)CC1 10.1016/j.bmcl.2009.04.147
45272014 193638 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 464 5 2 4 3.9 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(CO)C1 10.1016/j.bmcl.2009.05.066
CHEMBL551543 193638 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 464 5 2 4 3.9 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(CO)C1 10.1016/j.bmcl.2009.05.066
18435988 74519 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 428 4 1 3 5.6 Cc1ccc(C2CCN(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)CC2)cc1 10.1021/jm201596h
CHEMBL2031725 74519 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 428 4 1 3 5.6 Cc1ccc(C2CCN(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)CC2)cc1 10.1021/jm201596h
70695855 73114 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 503 7 2 7 3.6 Cc1nc(N2CCC(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016725 73114 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 503 7 2 7 3.6 Cc1nc(N2CCC(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11613073 75562 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205111 75562 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
21939881 64362 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 428 6 2 3 5.0 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(C(=O)O)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818789 64362 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 428 6 2 3 5.0 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(C(=O)O)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
117798680 138834 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)n4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793142 138834 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)n4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
59135486 91076 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 505 5 2 4 6.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403860 91076 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 505 5 2 4 6.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
73356649 91086 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 4 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2013.05.017
CHEMBL2403870 91086 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 4 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2013.05.017
22421749 65959 3 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 486 6 1 5 5.4 CCN1CCN(c2cc(C)c3cc(NC(=O)C(C)Oc4ccc(Cl)cc4Cl)ccc3n2)CC1 10.1021/jm040762v
CHEMBL184860 65959 3 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 486 6 1 5 5.4 CCN1CCN(c2cc(C)c3cc(NC(=O)C(C)Oc4ccc(Cl)cc4Cl)ccc3n2)CC1 10.1021/jm040762v
11620005 81030 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215958 81030 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
44397048 67083 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1ccccc1CNC(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
CHEMBL188991 67083 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1ccccc1CNC(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
44442061 93910 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 4.8 COc1ccc2nc(N(C)[C@H]3CC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250730 93910 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 4.8 COc1ccc2nc(N(C)[C@H]3CC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
17545006 174654 5 None - 0 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 426 4 1 3 4.9 Cc1c(C(=O)NC2CCN(Cc3ccccc3)CC2)oc2ccc(Br)cc12 10.1016/j.bmcl.2019.126741
CHEMBL4571855 174654 5 None - 0 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 426 4 1 3 4.9 Cc1c(C(=O)NC2CCN(Cc3ccccc3)CC2)oc2ccc(Br)cc12 10.1016/j.bmcl.2019.126741
17173466 174661 11 None - 0 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 372 6 1 3 3.8 Cc1cc(Cl)ccc1OCC(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL4572083 174661 11 None - 0 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 372 6 1 3 3.8 Cc1cc(Cl)ccc1OCC(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2019.126741
44442093 93820 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 425 8 2 6 5.6 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(OC(C)C)cc12 10.1016/j.bmcl.2007.05.034
CHEMBL250311 93820 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 425 8 2 6 5.6 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(OC(C)C)cc12 10.1016/j.bmcl.2007.05.034
70693793 73192 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 496 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017595 73192 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 496 5 2 5 5.4 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44562416 176382 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 397 6 2 3 4.0 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462352 176382 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 397 6 2 3 4.0 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2008.07.079
45271103 193596 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 505 5 1 5 3.6 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCCOCC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL551281 193596 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 505 5 1 5 3.6 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCCOCC2)C1 10.1016/j.bmcl.2009.05.066
70687478 73139 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 440 5 2 6 4.0 Cc1nc(N2CCC(C)(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016777 73139 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 440 5 2 6 4.0 Cc1nc(N2CCC(C)(O)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
9848699 60299 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
CHEMBL176024 60299 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
44417904 79952 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 487 7 0 3 4.6 CN(CC(=O)N(C)C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2019.126741
CHEMBL214432 79952 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 487 7 0 3 4.6 CN(CC(=O)N(C)C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3ccc(F)cc3)cc1)C2 10.1016/j.bmcl.2019.126741
71730661 122018 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 426 8 0 7 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3601374 122018 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 426 8 0 7 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
91759544 130708 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 2.7 Cc1cc(CN2CCN(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686771 130708 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 461 9 1 7 2.7 Cc1cc(CN2CCN(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759585 130784 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686847 130784 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 526 8 1 8 3.1 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Br)cn2)cc1=O nan
71730916 130795 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 10 1 8 2.5 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
CHEMBL3686858 130795 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 10 1 8 2.5 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
10344176 66834 4 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL187756 66834 4 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
25115856 60449 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)c(Cl)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761118 60449 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)c(Cl)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
122184696 121963 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 9 2 6 4.3 OC1CCN(Cc2ccc(NCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601037 121963 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 9 2 6 4.3 OC1CCN(Cc2ccc(NCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
89690396 137711 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770396 137711 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
71730661 122018 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 426 8 0 7 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601374 122018 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 426 8 0 7 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
1314 3657 18 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
9865843 3657 18 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
CHEMBL178707 3657 18 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.07.038
11640515 80083 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL214768 80083 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
20817762 76957 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 450 4 1 7 3.9 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL208340 76957 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 450 4 1 7 3.9 Cn1c(=O)c(C#N)c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11640515 80083 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1021/jm060683e
CHEMBL214768 80083 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1021/jm060683e
11975327 141217 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)cccc2o1 10.1021/jm060683e
CHEMBL386021 141217 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)cccc2o1 10.1021/jm060683e
44143494 183662 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 402 6 2 3 4.8 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CC1 10.1016/j.bmcl.2009.04.147
CHEMBL483673 183662 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 402 6 2 3 4.8 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CC1 10.1016/j.bmcl.2009.04.147
53318801 56392 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 406 8 0 6 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCOCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642468 56392 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 406 8 0 6 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCOCC2)cc1 10.1016/j.bmc.2010.12.002
49865679 15870 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 492 8 2 6 5.5 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223768 15870 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 492 8 2 6 5.5 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
10250850 72051 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4cc[nH]c4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL198727 72051 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4cc[nH]c4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
11419666 122025 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0490890
CHEMBL360142 122025 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0490890
44394855 66929 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 490 12 3 5 5.6 CCOc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCN(CC)CC 10.1016/j.bmcl.2004.07.077
CHEMBL188179 66929 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 490 12 3 5 5.6 CCOc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCN(CC)CC 10.1016/j.bmcl.2004.07.077
44405412 71515 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 388 5 2 4 4.4 COc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c(F)c1 10.1016/j.bmcl.2005.08.049
CHEMBL197058 71515 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 388 5 2 4 4.4 COc1ccc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)c(F)c1 10.1016/j.bmcl.2005.08.049
44417982 82086 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 359 4 2 3 4.4 Nc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL217751 82086 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 359 4 2 3 4.4 Nc1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
89690239 137666 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 413 6 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(C)C)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769899 137666 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 413 6 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(C)C)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
127025110 137750 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3cccc(Oc4ccc(OC(F)(F)F)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770776 137750 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3cccc(Oc4ccc(OC(F)(F)F)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
89690292 137647 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 372 5 0 6 3.6 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769682 137647 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 372 5 0 6 3.6 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccn4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89691193 138867 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 5 0 5 4.7 Cn1c(C2CCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793700 138867 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 5 0 5 4.7 Cn1c(C2CCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44403548 70034 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 465 8 3 5 4.3 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(Cl)ccc3NCc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.06.089
CHEMBL194531 70034 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 465 8 3 5 4.3 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(Cl)ccc3NCc3c[nH]cn3)CC2)cc1 10.1016/j.bmcl.2005.06.089
11656044 140593 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 486 9 1 5 5.3 CCc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL382755 140593 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 486 9 1 5 5.3 CCc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
10319824 66731 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 417 8 2 4 3.9 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL187288 66731 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 417 8 2 4 3.9 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN(C)C 10.1016/j.bmcl.2004.07.077
44407710 73577 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202095 73577 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70689596 73201 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 464 6 2 5 5.4 CCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017604 73201 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 464 6 2 5 5.4 CCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
70695915 73205 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 480 7 2 6 4.6 COCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017608 73205 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 480 7 2 6 4.6 COCCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
44394973 65880 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 456 10 1 6 5.3 CCN(CC)CCNC(=O)c1ccc(-c2noc(-c3ccc(Oc4ccccc4)cc3)n2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184528 65880 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 456 10 1 6 5.3 CCN(CC)CCNC(=O)c1ccc(-c2noc(-c3ccc(Oc4ccccc4)cc3)n2)cc1 10.1016/j.bmcl.2004.07.077
122184570 121892 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 399 8 0 3 5.5 CCN(CC)CCOc1ccc(C#Cc2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600825 121892 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 399 8 0 3 5.5 CCN(CC)CCOc1ccc(C#Cc2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
22421750 70032 6 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 507 5 1 6 6.2 CCN1CCN(c2cc(C)c3cc(NC(=O)c4cc(-c5cccs5)nc5ccccc45)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194530 70032 6 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 507 5 1 6 6.2 CCN1CCN(c2cc(C)c3cc(NC(=O)c4cc(-c5cccs5)nc5ccccc45)ccc3n2)CC1 10.1021/jm050103y
91759582 130779 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 1 8 3.0 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686842 130779 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 1 8 3.0 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
71730790 130790 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 456 8 1 7 2.9 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686853 130790 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 456 8 1 7 2.9 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
71731049 130793 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 448 9 0 8 3.0 COc1ccc(COc2cnn(CC(=O)c3ccc(CN4CCCC4)cc3C)c(=O)c2)nc1 nan
CHEMBL3686856 130793 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 448 9 0 8 3.0 COc1ccc(COc2cnn(CC(=O)c3ccc(CN4CCCC4)cc3C)c(=O)c2)nc1 nan
16665072 98073 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
CHEMBL276393 98073 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 449 8 1 6 3.6 CN(C)CCN(C)c1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
44417917 81670 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 489 6 1 3 6.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL216576 81670 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 489 6 1 3 6.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(c4ccccc4)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
89690607 137636 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769582 137636 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
122184885 122017 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 412 8 0 7 2.8 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601373 122017 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 412 8 0 7 2.8 CN(C)Cc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
11419666 122025 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0512286
CHEMBL360142 122025 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2c1cnn2CCN1CCCC1 10.1021/jm0512286
11635187 194051 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 536 8 2 5 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1ccnc1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL557263 194051 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 536 8 2 5 5.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1ccnc1)c1ccccc1 10.1016/j.bmcl.2009.05.066
18436123 74511 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 426 5 1 4 5.3 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)nc1 10.1021/jm201596h
CHEMBL2031717 74511 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 426 5 1 4 5.3 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(F)cc2)nc1 10.1021/jm201596h
44562564 188539 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)no2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL510667 188539 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)no2)cc1 10.1016/j.bmcl.2008.07.079
56597991 138633 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 481 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCN(C)CC5)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787461 138633 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 481 7 0 8 2.5 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCN(C)CC5)c(F)c4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11511219 65789 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL184084 65789 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407991 168875 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL442794 168875 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
44394864 125664 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 377 4 1 6 3.7 CNc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364983 125664 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 377 4 1 6 3.7 CNc1ccc2cccc(OC3CCN(c4ccc5c(c4)OCCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
9955811 65825 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 458 8 3 4 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184292 65825 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 458 8 3 4 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
44394986 122809 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 462 9 3 4 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Br)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL361654 122809 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 462 9 3 4 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Br)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
11452268 81147 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL216228 81147 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 396 5 1 5 4.2 Cc1nc(N2CCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2006.11.092
54580457 60240 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760059 60240 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.1 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
56673714 64374 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 502 5 1 3 7.5 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)C(=O)OC(C)(C)C 10.1016/j.bmc.2011.07.038
CHEMBL1818804 64374 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 502 5 1 3 7.5 CN(CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1)C(=O)OC(C)(C)C 10.1016/j.bmc.2011.07.038
22422406 67098 2 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 418 6 1 5 3.9 COc1ccc(CCC(=O)Nc2ccc3nc(N4CCN(C)CC4)cc(C)c3c2)cc1 10.1021/jm040762v
CHEMBL189083 67098 2 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 418 6 1 5 3.9 COc1ccc(CCC(=O)Nc2ccc3nc(N4CCN(C)CC4)cc(C)c3c2)cc1 10.1021/jm040762v
11583925 165207 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL424720 165207 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11342160 122407 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360671 122407 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11342160 122407 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL360671 122407 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
44394972 65854 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(OC(F)(F)F)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184418 65854 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(OC(F)(F)F)c2)cc1OC 10.1016/j.bmcl.2004.07.077
22421743 66474 4 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 432 7 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)CCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL186077 66474 4 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 432 7 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)CCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
122184687 121955 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(C(=O)N(C)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601024 121955 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(C(=O)N(C)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
70687470 73099 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 3.7 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016710 73099 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 3.7 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442068 93912 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 2 5 4.8 CC(=O)N(C)c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250746 93912 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 2 5 4.8 CC(=O)N(C)c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
122184674 121922 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 387 8 1 5 4.6 c1cc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)ccn1 10.1016/j.bmcl.2015.05.074
CHEMBL3600982 121922 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 387 8 1 5 4.6 c1cc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)ccn1 10.1016/j.bmcl.2015.05.074
44407479 73300 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 422 7 1 4 4.8 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccccc3Cl)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL201813 73300 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 422 7 1 4 4.8 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccccc3Cl)cc12 10.1016/j.bmcl.2005.10.066
11662657 80697 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
CHEMBL215661 80697 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
70685346 73135 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 493 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016772 73135 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 493 6 1 6 5.1 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
86695564 130693 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686756 130693 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC(C)(O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730532 130699 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 9 1 8 3.0 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686762 130699 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 9 1 8 3.0 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
71731945 130716 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 9 1 6 3.6 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686779 130716 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 9 1 6 3.6 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759556 130726 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 465 8 0 6 4.7 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686789 130726 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 465 8 0 6 4.7 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
71730921 130728 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 451 8 0 6 4.3 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686791 130728 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 451 8 0 6 4.3 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
71732075 130730 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 425 9 1 6 3.8 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
CHEMBL3686793 130730 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 425 9 1 6 3.8 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
71730135 130745 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 455 8 1 6 3.5 CNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686809 130745 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 455 8 1 6 3.5 CNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
91759580 130777 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 496 9 1 8 3.3 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686840 130777 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 496 9 1 8 3.3 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
91759589 130796 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 9 0 7 3.6 COc1ccc(COc2ccn(CC(=O)c3ccc(CN4CCCC4)cc3C)c(=O)c2)nc1 nan
CHEMBL3686859 130796 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 9 0 7 3.6 COc1ccc(COc2ccn(CC(=O)c3ccc(CN4CCCC4)cc3C)c(=O)c2)nc1 nan
44417995 82015 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 414 6 1 3 5.9 CCCc1cc(OC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217495 82015 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 414 6 1 3 5.9 CCCc1cc(OC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
57402993 69275 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4cccc(Cl)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934825 69275 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4cccc(Cl)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
70687552 73259 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 529 7 3 7 3.6 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017761 73259 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 529 7 3 7 3.6 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
89691439 137707 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770359 137707 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
11740891 121942 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 386 4 0 2 5.4 Clc1ccc(-c2ccc(C#Cc3ccc(CCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601012 121942 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 386 4 0 2 5.4 Clc1ccc(-c2ccc(C#Cc3ccc(CCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
89691439 137707 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1016/j.bmc.2016.04.011
CHEMBL3770359 137707 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1016/j.bmc.2016.04.011
90469437 120744 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578244 120744 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
44438755 93057 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 550 9 2 7 3.2 COc1cc(C(=O)NCCN2CCCC2)ccc1CN1CCC(NC(=O)c2cc(=O)c3ccc(F)cc3o2)CC1 10.1016/j.bmcl.2006.11.068
CHEMBL246259 93057 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 550 9 2 7 3.2 COc1cc(C(=O)NCCN2CCCC2)ccc1CN1CCC(NC(=O)c2cc(=O)c3ccc(F)cc3o2)CC1 10.1016/j.bmcl.2006.11.068
45271829 193601 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 449 5 1 3 6.7 CCc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551332 193601 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 449 5 1 3 6.7 CCc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
11634886 194980 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 511 6 1 4 5.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1Cc1cccnc1 10.1016/j.bmcl.2009.05.066
CHEMBL564501 194980 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 511 6 1 4 5.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1Cc1cccnc1 10.1016/j.bmcl.2009.05.066
18436125 74513 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 438 6 1 5 5.2 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cn2)cc1 10.1021/jm201596h
CHEMBL2031719 74513 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 438 6 1 5 5.2 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cn2)cc1 10.1021/jm201596h
11165058 154083 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 385 6 2 5 5.0 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(F)cc12 10.1016/j.bmcl.2007.05.034
CHEMBL399367 154083 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 385 6 2 5 5.0 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccc(F)cc12 10.1016/j.bmcl.2007.05.034
44562600 172550 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 480 5 1 4 5.8 Cc1c(-c2ccccc2)[nH]c(=O)n1C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL452087 172550 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 480 5 1 4 5.8 Cc1c(-c2ccccc2)[nH]c(=O)n1C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
11155432 82061 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 461 8 1 6 4.0 Cc1nc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
CHEMBL217712 82061 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 461 8 1 6 4.0 Cc1nc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2006.11.092
45267565 194601 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 461 5 1 3 7.0 O=C(Nc1ccc2nc(C3CC3)c(C3CC3)n2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL562073 194601 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 461 5 1 3 7.0 O=C(Nc1ccc2nc(C3CC3)c(C3CC3)n2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
11678370 136029 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373886 136029 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44403484 70229 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 461 7 2 7 2.2 COc1ccc(NS(C)(=O)=O)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL194950 70229 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 461 7 2 7 2.2 COc1ccc(NS(C)(=O)=O)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
49865790 15951 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 462 7 1 4 6.5 Fc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223969 15951 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 462 7 1 4 6.5 Fc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
59135479 91067 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 393 3 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@H](NC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403851 91067 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 393 3 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@H](NC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
15987638 126244 4 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 438 5 1 5 4.6 CCN1CCN(c2cc(C)c3cc(NC(=O)c4cc(Cl)ccc4OC)ccc3n2)CC1 10.1021/jm050103y
CHEMBL365374 126244 4 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 438 5 1 5 4.6 CCN1CCN(c2cc(C)c3cc(NC(=O)c4cc(Cl)ccc4OC)ccc3n2)CC1 10.1021/jm050103y
44562544 173259 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 509 8 1 5 4.2 O=C(COc1ccc(F)c(F)c1)NCC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CCO1 10.1016/j.bmcl.2008.07.079
CHEMBL453886 173259 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 509 8 1 5 4.2 O=C(COc1ccc(F)c(F)c1)NCC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CCO1 10.1016/j.bmcl.2008.07.079
49865708 15898 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 545 9 2 7 5.1 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(S(C)(=O)=O)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223828 15898 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 545 9 2 7 5.1 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(S(C)(=O)=O)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
91759577 130772 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 454 8 1 8 2.2 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686835 130772 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 454 8 1 8 2.2 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
57396022 69285 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4Cl)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934836 69285 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 548 7 1 5 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4Cl)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57397820 69290 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 534 7 1 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4cc(F)cc(F)c4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934840 69290 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 534 7 1 5 5.7 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4cc(F)cc(F)c4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
44143497 183520 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 432 6 2 4 4.4 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCOC1 10.1016/j.bmcl.2009.04.147
CHEMBL482636 183520 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 432 6 2 4 4.4 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCOC1 10.1016/j.bmcl.2009.04.147
45267739 194870 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 522 7 3 4 5.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ncc[nH]1 10.1016/j.bmcl.2009.05.066
CHEMBL563791 194870 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 522 7 3 4 5.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ncc[nH]1 10.1016/j.bmcl.2009.05.066
90666263 108873 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cn3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219272 108873 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 547 7 1 6 6.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cn3)CC2)c1 10.1039/C1MD00015B
11531660 135058 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 410 4 1 5 4.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)CCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL372919 135058 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 410 4 1 5 4.5 O=c1cc(NC2CCN(Cc3ccc4c(c3)CCO4)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
12020156 194598 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 486 8 1 5 5.4 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL562016 194598 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 486 8 1 5 5.4 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2019.126741
70685397 73202 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 450 5 2 5 5.0 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017605 73202 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 450 5 2 5 5.0 CCC1(O)CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
127025110 137750 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3cccc(Oc4ccc(OC(F)(F)F)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770776 137750 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3cccc(Oc4ccc(OC(F)(F)F)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
70683237 73091 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 451 6 1 6 3.9 Cc1nc(N2CCN(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016701 73091 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 451 6 1 6 3.9 Cc1nc(N2CCN(C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44417942 82027 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 401 6 2 3 4.8 CCCc1cc(N)c2cc(C(=O)NCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217560 82027 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 401 6 2 3 4.8 CCCc1cc(N)c2cc(C(=O)NCCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44401395 135450 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 558 7 2 6 5.2 O=S(=O)(NC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL373157 135450 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 558 7 2 6 5.2 O=S(=O)(NC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
90666254 108863 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 492 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CC4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219263 108863 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 492 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CC4)cc3)CC2)c1 10.1039/C1MD00015B
44408099 75336 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 469 7 2 4 4.6 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)NCc3ccc(Br)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204798 75336 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 469 7 2 4 4.6 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)NCc3ccc(Br)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407950 140012 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 446 7 1 5 4.7 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL381143 140012 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 446 7 1 5 4.7 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
71717086 87346 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 485 10 0 5 5.7 CCCCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337753 87346 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 485 10 0 5 5.7 CCCCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
71714121 122021 3 None - 1 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 nan
CHEMBL3601377 122021 3 None - 1 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 nan
71730533 130775 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 412 8 1 7 2.8 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
CHEMBL3686838 130775 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 412 8 1 7 2.8 CNCc1ccc(C(=O)Cn2ncc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
89690379 137639 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 389 5 0 5 4.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769602 137639 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 389 5 0 5 4.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89690318 137765 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 371 5 0 5 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770954 137765 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 371 5 0 5 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44193624 122002 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 455 8 0 6 3.5 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601299 122002 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 455 8 0 6 3.5 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
89691162 138828 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793111 138828 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
71660915 138870 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793767 138870 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45273777 194169 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 525 5 1 4 5.2 CN1CCN(C(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C(c2ccccc2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL558532 194169 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 525 5 1 4 5.2 CN1CCN(C(=O)NC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C(c2ccccc2)C1 10.1016/j.bmcl.2009.05.066
44442121 93826 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 483 7 2 5 5.8 COc1ccc(Br)c(CN[C@H]2CCC[C@H](Nc3cc(C)c4ccc(OC)cc4n3)C2)c1 10.1016/j.bmcl.2007.05.034
CHEMBL250326 93826 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 483 7 2 5 5.8 COc1ccc(Br)c(CN[C@H]2CCC[C@H](Nc3cc(C)c4ccc(OC)cc4n3)C2)c1 10.1016/j.bmcl.2007.05.034
45270841 195048 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 550 8 1 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1cccnc1 10.1016/j.bmcl.2009.05.067
CHEMBL565073 195048 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 550 8 1 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1cccnc1 10.1016/j.bmcl.2009.05.067
11563017 80635 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215418 80635 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
11713027 80747 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 498 8 3 4 5.4 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.040
CHEMBL215819 80747 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 498 8 3 4 5.4 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.040
23567290 63129 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccc(Cl)cc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
CHEMBL179872 63129 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccc(Cl)cc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
44405488 132478 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 414 5 2 6 4.0 COc1cc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc2c1OCO2 10.1016/j.bmcl.2019.126741
CHEMBL370222 132478 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 414 5 2 6 4.0 COc1cc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc2c1OCO2 10.1016/j.bmcl.2019.126741
44405488 132478 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 414 5 2 6 4.0 COc1cc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc2c1OCO2 10.1016/j.bmcl.2005.08.049
CHEMBL370222 132478 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 414 5 2 6 4.0 COc1cc(CN2CCC(Nc3[nH]nc4ccc(Cl)cc34)CC2)cc2c1OCO2 10.1016/j.bmcl.2005.08.049
70695929 73253 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 590 6 1 7 4.0 Cc1nc(N2CCC(N3CCN(C)S3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017755 73253 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 590 6 1 7 4.0 Cc1nc(N2CCC(N3CCN(C)S3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
21940052 64365 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 385 5 0 3 5.2 CN(C)CC1CCc2cc(OC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818794 64365 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 385 5 0 3 5.2 CN(C)CC1CCc2cc(OC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
57401531 67795 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 444 6 0 4 5.1 CC(=O)N1CCc2cc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)sc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914855 67795 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 444 6 0 4 5.1 CC(=O)N1CCc2cc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)sc2C1 10.1016/j.bmc.2011.09.007
44397606 123541 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 7 1 6 3.0 COc1cc(C(=O)NC[C@H]2CCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
CHEMBL363256 123541 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 7 1 6 3.0 COc1cc(C(=O)NC[C@H]2CCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
90666253 108862 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 466 6 1 5 5.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219262 108862 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 466 6 1 5 5.1 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C)cc3)CC2)c1 10.1039/C1MD00015B
71731943 130712 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686775 130712 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759547 130715 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 460 9 1 6 4.0 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686778 130715 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 460 9 1 6 4.0 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
11568782 71540 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 8 1 5 4.8 CN(C)CCN(C)c1ccc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL197145 71540 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 8 1 5 4.8 CN(C)CCN(C)c1ccc2cc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
11705485 167958 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 470 6 1 5 4.9 CCN1CCN(c2ccc3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL435494 167958 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 470 6 1 5 4.9 CCN1CCN(c2ccc3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
11511219 65789 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL184084 65789 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
11655872 71358 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL196567 71358 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 475 8 1 6 4.9 CC(=O)OCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
25115621 60430 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 466 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761099 60430 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 466 8 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
60130302 121833 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 7 1 2 5.6 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600390 121833 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 7 1 2 5.6 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2015.05.077
89691162 138828 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793111 138828 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
89691065 138918 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794150 138918 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
16739263 92968 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 538 8 2 6 3.3 O=C(NC1CCN(Cc2ccc(C(=O)NCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL245846 92968 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 538 8 2 6 3.3 O=C(NC1CCN(Cc2ccc(C(=O)NCCN3CCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
11712898 178599 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL472363 178599 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
23657037 94075 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 415 6 2 6 4.6 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251701 94075 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 415 6 2 6 4.6 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44442071 154065 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 380 6 2 5 4.9 CN(C)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL399244 154065 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 380 6 2 5 4.9 CN(C)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
11712898 178599 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
11712898 178599 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL472363 178599 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472363 178599 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 7 1 4 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
44562500 186143 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 479 7 1 4 4.5 O=C(COc1ccc(F)c(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL488721 186143 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 479 7 1 4 4.5 O=C(COc1ccc(F)c(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
45487330 196965 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 422 9 0 5 4.1 O=c1cc(OCc2ccc(F)cc2)ccn1Cc1cccc(OCCN2CCCC2)c1 10.1016/j.bmcl.2009.07.023
CHEMBL579232 196965 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 422 9 0 5 4.1 O=c1cc(OCc2ccc(F)cc2)ccn1Cc1cccc(OCCN2CCCC2)c1 10.1016/j.bmcl.2009.07.023
11656489 15950 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223968 15950 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
11511219 65789 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL184084 65789 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
70695917 73210 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 488 9 2 6 5.1 Cc1nc(N(CCCO)C(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017613 73210 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 488 9 2 6 5.1 Cc1nc(N(CCCO)C(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44401508 69463 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 433 10 2 6 3.6 CCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
CHEMBL193666 69463 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 433 10 2 6 3.6 CCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
44401552 165342 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 572 8 2 6 5.5 O=S(=O)(NCC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL425012 165342 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 572 8 2 6 5.5 O=S(=O)(NCC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
11604236 176117 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 423 7 1 4 4.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cccc(-n3cccc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL459897 176117 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 423 7 1 4 4.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cccc(-n3cccc3)c2)CC1 10.1016/j.bmcl.2008.07.079
44388559 60380 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 469 10 2 6 4.7 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ncn(CCN3CCCC3)c2c1 10.1021/jm0490890
CHEMBL176081 60380 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 469 10 2 6 4.7 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ncn(CCN3CCCC3)c2c1 10.1021/jm0490890
44402768 69444 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese miceInhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice
ChEMBL 468 10 2 5 5.3 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL193583 69444 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese miceInhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice
ChEMBL 468 10 2 5 5.3 O=C(CNCc1ccc(Oc2ccccc2)cc1)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
44442060 154257 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 4.9 COc1ccc2nc(NCC3CCCN(Cc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL400297 154257 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 1 5 4.9 COc1ccc2nc(NCC3CCCN(Cc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
44397454 123571 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 414 6 1 7 3.2 COc1cc(OC)cc(OC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL363337 123571 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 414 6 1 7 3.2 COc1cc(OC)cc(OC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
44424070 85310 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 390 7 0 2 4.9 CN(C)Cc1ccc(CCN(C)C(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL229093 85310 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 390 7 0 2 4.9 CN(C)Cc1ccc(CCN(C)C(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
11520239 3562 4 None 2 4 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
1313 3562 4 None 2 4 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
CHEMBL185271 3562 4 None 2 4 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmcl.2004.07.034
44394698 65894 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 346 6 2 5 2.9 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL184581 65894 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 346 6 2 5 2.9 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(N)nc23)c1 10.1016/j.bmcl.2004.07.034
10360874 64588 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL182261 64588 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 355 6 2 4 3.7 Nc1ccc2cccc(OCCCNC(=O)c3cccc(Cl)c3)c2n1 10.1016/j.bmcl.2004.07.035
11539096 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.065
1303 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.065
CHEMBL214021 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.065
11662657 80697 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
CHEMBL215661 80697 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
11554412 96560 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 461 4 1 6 3.2 Cn1c(=O)ccc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc21 10.1016/j.bmcl.2006.11.065
CHEMBL266725 96560 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 461 4 1 6 3.2 Cn1c(=O)ccc2ccc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)cc21 10.1016/j.bmcl.2006.11.065
10150955 80492 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 5 1 3 5.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL215331 80492 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 413 5 1 3 5.4 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44417930 81874 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217207 81874 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 453 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CC4CCC3CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
44417945 141253 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 508 7 3 5 3.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NS(=O)(=O)O)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL386211 141253 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 508 7 3 5 3.8 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC(NS(=O)(=O)O)C3)ccc2c1 10.1016/j.bmcl.2006.08.006
11648240 71102 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196196 71102 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 8 2 5 5.1 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
25113835 60437 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C(F)(F)F)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761106 60437 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C(F)(F)F)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25116082 60448 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761117 60448 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
16745235 121910 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 8 1 2 7.0 Clc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600970 121910 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 418 8 1 2 7.0 Clc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.074
122184695 121962 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 10 2 6 4.1 OC1CCN(Cc2ccc(NCCCc3ccc(OCc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601036 121962 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 10 2 6 4.1 OC1CCN(Cc2ccc(NCCCc3ccc(OCc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
127029624 137649 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 6 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769702 137649 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 6 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn12 10.1021/acs.jmedchem.5b01704
57403784 68498 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 421 3 1 3 4.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922262 68498 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 421 3 1 3 4.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
57890370 121879 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 7 1 2 5.1 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600812 121879 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 7 1 2 5.1 O=C(NCCc1ccc(CN2CCCC2)cc1)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2015.05.077
122184561 121882 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 473 8 2 3 4.6 CC(=O)NC1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600815 121882 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 473 8 2 3 4.6 CC(=O)NC1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
11539096 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
1303 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
CHEMBL214021 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1016/j.bmcl.2006.11.068
11649549 93491 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 539 9 1 6 4.7 O=C(NC1CCN(Cc2ccc(OCCCN3CCCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL248297 93491 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 539 9 1 6 4.7 O=C(NC1CCN(Cc2ccc(OCCCN3CCCCC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
11619850 75409 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm0512286
CHEMBL204828 75409 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm0512286
11539096 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
1303 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
CHEMBL214021 181 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 Fc1ccc2c(c1)oc(cc2=O)C(=O)NC1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1021/jm060683e
11619850 75409 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm060683e
CHEMBL204828 75409 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)c(Cl)cc2o1 10.1021/jm060683e
22348261 76695 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 421 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)cc(=O)n2C 10.1016/j.bmcl.2006.02.044
CHEMBL207300 76695 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 421 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)cc(=O)n2C 10.1016/j.bmcl.2006.02.044
11775505 141443 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(Cl)cc2o1 10.1021/jm060683e
CHEMBL387418 141443 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 458 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(Cl)cc2o1 10.1021/jm060683e
44442053 154357 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL400883 154357 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
24808474 91077 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403861 91077 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
24952765 91082 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 402 4 1 4 4.8 Cc1nc2cc(F)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403866 91082 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 402 4 1 4 4.8 Cc1nc2cc(F)ccc2n1[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
71226964 128646 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3670638 128646 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCCO6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11236807 81140 0 None 1 3 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81140 0 None 1 3 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11598355 141259 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 490 8 3 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL386247 141259 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 490 8 3 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1C 10.1016/j.bmcl.2006.07.040
44397476 67073 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 6 1 6 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
CHEMBL188937 67073 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 6 1 6 3.1 COc1cc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)cc(OC)c1C 10.1016/j.bmcl.2005.05.023
11553316 71275 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ocnc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL196350 71275 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ocnc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
11340348 128925 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 468 5 2 3 5.8 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL367156 128925 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 468 5 2 3 5.8 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2019.126741
44143503 187476 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 453 5 2 4 5.7 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497830 187476 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 453 5 2 4 5.7 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
44408027 74702 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 490 11 2 6 5.2 CCN(CC)CCNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2005.10.066
CHEMBL203586 74702 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 490 11 2 6 5.2 CCN(CC)CCNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2005.10.066
18436119 76014 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059416 76014 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 8 1 3 5.6 Cc1c(NC(=O)CCCCc2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
11222404 193698 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 368 4 1 4 4.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccccn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551934 193698 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 368 4 1 4 4.8 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccccn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
45487383 195297 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 12 0 4 5.4 CCCN(CCC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL566662 195297 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 12 0 4 5.4 CCCN(CCC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
23593464 64356 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64356 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
58646147 78660 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@@H](C)NC[C@@H]2C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL2113218 78660 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@@H](C)NC[C@@H]2C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
57522945 76017 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059419 76017 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
57522468 76026 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCNC(C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059511 76026 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCNC(C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
1305 508 10 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
9934033 508 10 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
CHEMBL182150 508 10 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
11570040 77401 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 530 5 1 3 7.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL209109 77401 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 530 5 1 3 7.6 N#Cc1cccc(-c2ccc(C(=C3CCN(CC4CC4)CC3)c3nc4cc(C(F)(F)F)c(F)cc4[nH]3)cc2)c1 10.1016/j.bmcl.2019.126741
10027853 71503 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197026 71503 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 474 6 2 6 4.4 Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
23593464 64356 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64356 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
23120540 194455 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL561134 194455 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
45487652 198042 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 426 4 0 4 5.3 Fc1cc2c(cn1)C1(CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC1)OC2 10.1016/j.bmcl.2009.07.132
CHEMBL593521 198042 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 426 4 0 4 5.3 Fc1cc2c(cn1)C1(CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC1)OC2 10.1016/j.bmcl.2009.07.132
45487283 195785 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 462 11 0 4 6.0 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)C1CCCC1 10.1016/j.bmcl.2009.07.023
CHEMBL569852 195785 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 462 11 0 4 6.0 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)C1CCCC1 10.1016/j.bmcl.2009.07.023
45487309 196118 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 10 0 4 4.7 CCCN(C)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL572090 196118 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 10 0 4 4.7 CCCN(C)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
21939950 64381 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 438 6 1 3 6.0 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818811 64381 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 438 6 1 3 6.0 COc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN3CCCC3)=C4)cc2)cc1 10.1016/j.bmc.2011.07.038
44407710 73577 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202095 73577 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 1 6 4.6 Cc1cc(N2CCCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407875 74697 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203558 74697 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
18436112 74483 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 437 6 1 4 5.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cc2)cc1 10.1021/jm201596h
CHEMBL2031578 74483 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 437 6 1 4 5.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)cc2)cc1 10.1021/jm201596h
11583744 71365 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196581 71365 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 476 10 2 6 4.8 Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
127029623 137794 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 379 5 1 5 3.9 Cc1nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3771335 137794 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 379 5 1 5 3.9 Cc1nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn2c1C 10.1021/acs.jmedchem.5b01704
57522950 76022 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 9 3 5 4.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCCO)cnc12 10.1021/jm300167z
CHEMBL2059425 76022 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 419 9 3 5 4.2 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)NCCO)cnc12 10.1021/jm300167z
53321223 56409 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 440 10 0 5 4.9 CN(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)Cc1ccccc1 10.1016/j.bmc.2010.12.002
CHEMBL1642487 56409 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 440 10 0 5 4.9 CN(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)Cc1ccccc1 10.1016/j.bmc.2010.12.002
57399740 67727 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914633 67727 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
71731807 130710 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 1 6 3.2 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686773 130710 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 1 6 3.2 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71730394 130760 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 0 7 3.2 Cc1cc(CN2CCOC(C)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686824 130760 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 447 8 0 7 3.2 Cc1cc(CN2CCOC(C)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
91759584 130773 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686836 130773 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
71730659 130781 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 496 9 1 8 3.4 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686844 130781 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 496 9 1 8 3.4 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
44405415 72209 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 394 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2C 10.1016/j.bmcl.2005.08.049
CHEMBL199222 72209 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 394 5 1 7 3.4 COc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2C 10.1016/j.bmcl.2005.08.049
44405486 139969 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 409 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL381013 139969 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 409 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44394860 65901 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 285 5 2 4 3.1 CC(CNC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184590 65901 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 285 5 2 4 3.1 CC(CNC1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394606 66902 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 351 6 2 6 3.1 CC(CNCc1ccc2c(c1)OCO2)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL188058 66902 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 351 6 2 6 3.1 CC(CNCc1ccc2c(c1)OCO2)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
60169096 87318 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 479 8 0 6 5.0 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337725 87318 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 479 8 0 6 5.0 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
57396019 69268 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(F)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934819 69268 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c4cc(F)ccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57401250 69273 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 480 7 1 5 5.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccccc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934823 69273 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 480 7 1 5 5.3 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccccc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57401252 69291 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 570 7 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4c(F)c(F)c(F)c(F)c4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934841 69291 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 570 7 1 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4c(F)c(F)c(F)c(F)c4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
54584181 60436 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761105 60436 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70693807 73240 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 555 6 1 7 4.3 Cc1nc(N2CCC(N3CCOCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017742 73240 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 555 6 1 7 4.3 Cc1nc(N2CCC(N3CCOCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
89690365 137634 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769550 137634 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
54585864 60306 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 493 10 1 5 3.7 COc1ccc([C@H]2CN(CCCN(C)S(C)(=O)=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760249 60306 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 493 10 1 5 3.7 COc1ccc([C@H]2CN(CCCN(C)S(C)(=O)=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
21108118 67799 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 5 0 3 4.7 CN1CCc2ccc(C(=O)CCC(=O)N3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914859 67799 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 5 0 3 4.7 CN1CCc2ccc(C(=O)CCC(=O)N3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
45273623 193951 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 425 4 2 4 5.3 CC(O)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL556296 193951 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 425 4 2 4 5.3 CC(O)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
44143498 187191 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 473 6 2 4 4.2 CC(=O)N1CCC(N(C)c2nc3ccc(NC(=O)CCc4ccc(C(F)(F)F)cc4)cc3[nH]2)C1 10.1016/j.bmcl.2009.04.147
CHEMBL495789 187191 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 473 6 2 4 4.2 CC(=O)N1CCC(N(C)c2nc3ccc(NC(=O)CCc4ccc(C(F)(F)F)cc4)cc3[nH]2)C1 10.1016/j.bmcl.2009.04.147
45271642 193475 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 6 2 4 5.4 O=C(NCc1ccc(O)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL550308 193475 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 491 6 2 4 5.4 O=C(NCc1ccc(O)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
45487366 196094 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 10 0 5 4.5 O=c1cc(OCc2ccc(F)cc2)ccn1Cc1cccc(OCCCN2CCCC2)c1 10.1016/j.bmcl.2009.07.023
CHEMBL571830 196094 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 10 0 5 4.5 O=c1cc(OCc2ccc(F)cc2)ccn1Cc1cccc(OCCCN2CCCC2)c1 10.1016/j.bmcl.2009.07.023
6621104 66453 5 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 438 6 1 5 4.4 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1021/jm040762v
CHEMBL185997 66453 5 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 438 6 1 5 4.4 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1021/jm040762v
44397262 67153 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 406 4 1 4 4.1 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189496 67153 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 406 4 1 4 4.1 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.023
44403480 70191 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 442 6 2 6 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
CHEMBL194759 70191 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 442 6 2 6 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
44403506 70775 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 464 8 2 5 4.8 COc1ccc(CNc2ncc(Cl)cc2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.06.089
CHEMBL195511 70775 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 464 8 2 5 4.8 COc1ccc(CNc2ncc(Cl)cc2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.06.089
44403474 126692 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 430 6 2 6 3.7 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL365788 126692 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 430 6 2 6 3.7 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403468 167855 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 491 7 2 6 5.4 O=C(NC1CCN(Cc2ccc3ncccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL434934 167855 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 491 7 2 6 5.4 O=C(NC1CCN(Cc2ccc3ncccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
20779426 60210 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 405 4 2 2 5.1 Cc1ccc(C2(CNC(=O)Nc3cc(Cl)cc(Cl)c3)CCN(C)CC2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL175874 60210 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 405 4 2 2 5.1 Cc1ccc(C2(CNC(=O)Nc3cc(Cl)cc(Cl)c3)CCN(C)CC2)cc1 10.1016/j.bmcl.2019.126741
44417892 79811 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 500 5 0 4 4.2 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cn2)C3)CC1 10.1016/j.bmcl.2019.126741
CHEMBL213771 79811 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 500 5 0 4 4.2 CC(=O)N1CCN(Cc2ccc3c(c2)CC[C@H](N(C)C(=O)c2ccc(-c4ccc(F)cc4)cn2)C3)CC1 10.1016/j.bmcl.2019.126741
71720118 87328 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cc(C)ccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337735 87328 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cc(C)ccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
25114948 60455 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 562 8 1 4 8.2 Cc1ccc(C(=O)Nc2cccc(C3CCN(CCCn4c(-c5ccc(Cl)cc5)nc5ccccc54)CC3)c2)cc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761125 60455 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 562 8 1 4 8.2 Cc1ccc(C(=O)Nc2cccc(C3CCN(CCCn4c(-c5ccc(Cl)cc5)nc5ccccc54)CC3)c2)cc1 10.1016/j.bmcl.2011.02.099
45267654 194397 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 381 3 1 3 5.3 O=C(Nc1ccc2nccn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL560677 194397 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 381 3 1 3 5.3 O=C(Nc1ccc2nccn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
9828622 96193 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 536 9 1 5 5.3 O=C1c2cc(OCCC3CCN(Cc4ccc(C5=NCCN5)cc4)CC3)ccc2CCCN1Cc1ccccc1 10.1021/jm040762v
CHEMBL263702 96193 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 536 9 1 5 5.3 O=C1c2cc(OCCC3CCN(Cc4ccc(C5=NCCN5)cc4)CC3)ccc2CCCN1Cc1ccccc1 10.1021/jm040762v
44397175 125854 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 6 1 2 4.3 O=C(Cc1ccccc1Br)NC1CCN(C/C=C/c2ccccc2)CC1 10.1016/j.bmcl.2005.05.023
CHEMBL365094 125854 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 412 6 1 2 4.3 O=C(Cc1ccccc1Br)NC1CCN(C/C=C/c2ccccc2)CC1 10.1016/j.bmcl.2005.05.023
11330800 81848 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 592 10 2 6 4.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCC[C@H]5CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL217132 81848 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 592 10 2 6 4.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCC[C@H]5CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
11569340 71291 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 486 8 0 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(N(C)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL196360 71291 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 486 8 0 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(N(C)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44562543 173257 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 8 1 5 5.0 O=C(COc1cccc(Cl)c1)NCC1CCCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL453885 173257 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 8 1 5 5.0 O=C(COc1cccc(Cl)c1)NCC1CCCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)C1 10.1016/j.bmcl.2008.07.079
70681117 73103 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 507 6 1 6 4.4 Cc1nc(N2CCN(C(=O)C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016714 73103 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 507 6 1 6 4.4 Cc1nc(N2CCN(C(=O)C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44402593 71252 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 477 7 2 5 5.8 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCC(F)(F)C2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL196332 71252 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 477 7 2 5 5.8 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCC(F)(F)C2)c1 10.1016/j.bmcl.2005.03.114
44562499 186142 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL488720 186142 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)C1 10.1016/j.bmcl.2008.07.079
44394774 66861 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 274 4 1 4 3.4 CC(COC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL187859 66861 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 274 4 1 4 3.4 CC(COC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
45272040 193427 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 474 7 2 5 4.0 CC(Cn1ccnc1)NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL549930 193427 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 474 7 2 5 4.0 CC(Cn1ccnc1)NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
71731944 130714 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686777 130714 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 446 8 1 6 3.6 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71732077 130734 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 453 8 1 7 2.8 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686797 130734 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 453 8 1 7 2.8 Cc1cc(CN2CC(O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
91759583 130780 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 1 8 3.0 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686843 130780 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 482 8 1 8 3.0 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
44424069 85289 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 376 7 1 2 4.5 CN(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228987 85289 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 376 7 1 2 4.5 CN(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
44424071 141553 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 416 7 1 2 6.1 O=C(CCc1ccc(CN2CCCCC2)cc1)Nc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL388181 141553 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 416 7 1 2 6.1 O=C(CCc1ccc(CN2CCCCC2)cc1)Nc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2006.12.028
70687551 73255 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 499 6 2 6 3.8 Cc1nc(N2CCC(NS(C)(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017757 73255 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 499 6 2 6 3.8 Cc1nc(N2CCC(NS(C)(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
117798744 138930 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3794256 138930 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 405 5 0 5 5.1 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
44438747 92929 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 485 8 1 7 3.5 CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
CHEMBL245642 92929 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 485 8 1 7 3.5 CO/N=C/COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1F 10.1016/j.bmcl.2006.11.068
11974231 81994 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 410 5 1 5 3.3 COc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1021/jm060683e
CHEMBL217400 81994 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 410 5 1 5 3.3 COc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1021/jm060683e
11511776 188701 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 507 8 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(OC(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL512185 188701 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 507 8 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(OC(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2008.07.079
11570031 73136 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 529 7 1 7 4.9 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016774 73136 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 529 7 1 7 4.9 Cc1nc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44408117 139016 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379693 139016 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 476 9 1 6 4.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11778029 65862 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 272 4 1 3 4.5 CNc1ccc2cccc(OC(C)CC(C)(C)C)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184446 65862 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 272 4 1 3 4.5 CNc1ccc2cccc(OC(C)CC(C)(C)C)c2n1 10.1016/j.bmcl.2004.07.032
71717084 87338 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 447 7 0 5 4.5 COc1cc(N2Cc3ccc(-c4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337745 87338 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 447 7 0 5 4.5 COc1cc(N2Cc3ccc(-c4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44562542 172646 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 8 1 5 5.0 O=C(COc1cccc(Cl)c1)NCC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL452335 172646 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 8 1 5 5.0 O=C(COc1cccc(Cl)c1)NCC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
11597758 193492 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 7 1 4 4.8 Cn1cccc1CNC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL550455 193492 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 7 1 4 4.8 Cn1cccc1CNC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
71731948 122001 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 425 8 0 6 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3601298 122001 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 425 8 0 6 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
91759581 130778 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686841 130778 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
22254604 123345 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCCCC1Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL362713 123345 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCCCC1Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
25115173 60443 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 480 8 1 4 6.5 CCc1ccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)cc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761112 60443 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 480 8 1 4 6.5 CCc1ccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)cc1 10.1016/j.bmcl.2011.02.099
70691738 73260 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 543 8 2 7 4.2 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017762 73260 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 543 8 2 7 4.2 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
11569300 82056 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Br)cc2o1 10.1021/jm060683e
CHEMBL217706 82056 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 484 4 1 6 3.7 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Br)cc2o1 10.1021/jm060683e
23022394 76012 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 444 8 2 4 5.5 CCCCC(=O)Nc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059414 76012 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 444 8 2 4 5.5 CCCCC(=O)Nc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
59135478 91074 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 471 5 2 4 6.1 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403858 91074 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 471 5 2 4 6.1 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
11296279 80124 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 591 9 1 6 4.5 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCN(C)CC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL214858 80124 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 591 9 1 6 4.5 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCN(C)CC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
71719522 87326 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 485 7 0 5 5.7 COc1cc(N2Cc3ccc(-c4ccc(C(C)(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337733 87326 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 485 7 0 5 5.7 COc1cc(N2Cc3ccc(-c4ccc(C(C)(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
45268457 194454 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 463 5 1 4 6.4 CC(=O)c1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL561133 194454 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 463 5 1 4 6.4 CC(=O)c1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
49865738 15925 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 537 9 2 5 7.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C(C)(C)C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223884 15925 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 537 9 2 5 7.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C(C)(C)C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44417017 79955 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 497 9 2 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)[C@@H]2C[C@H]2c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214442 79955 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 497 9 2 4 5.7 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)[C@@H]2C[C@H]2c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
44397480 67019 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 388 4 1 4 4.0 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.023
CHEMBL188655 67019 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 388 4 1 4 4.0 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.023
44397215 67152 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 413 6 2 6 3.2 COc1cc(NC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc(OC)c1 10.1016/j.bmcl.2005.05.023
CHEMBL189492 67152 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 413 6 2 6 3.2 COc1cc(NC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc(OC)c1 10.1016/j.bmcl.2005.05.023
44390752 122467 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 523 6 1 6 5.4 CN(C)c1nc(NC2CCN(Cc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360876 122467 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 523 6 1 6 5.4 CN(C)c1nc(NC2CCN(Cc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44394925 65838 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 409 9 3 5 3.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C#N)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184353 65838 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 409 9 3 5 3.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C#N)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
137635978 155503 0 None - 2 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 409 5 0 5 4.0 O=C1COc2ccccc2N1CCCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm5013243
CHEMBL4062602 155503 0 None - 2 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 409 5 0 5 4.0 O=C1COc2ccccc2N1CCCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm5013243
70681116 73101 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 493 6 1 6 4.1 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016712 73101 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 493 6 1 6 4.1 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
90666258 108867 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 614 7 1 5 7.8 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C(F)(F)F)CC2)c1 10.1039/C1MD00015B
CHEMBL3219267 108867 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 614 7 1 5 7.8 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C(F)(F)F)CC2)c1 10.1039/C1MD00015B
137635978 155503 0 None - 2 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 409 5 0 5 4.0 O=C1COc2ccccc2N1CCCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm5013243
CHEMBL4062602 155503 0 None - 2 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 409 5 0 5 4.0 O=C1COc2ccccc2N1CCCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm5013243
10353807 66002 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.4 CCC(CC)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL185096 66002 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.4 CCC(CC)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
22427041 69953 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 497 7 2 5 4.8 CCN1CCN(c2cc(C)c3cc(NC(=O)CCC(=O)Nc4ccc(F)c(Cl)c4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194417 69953 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 497 7 2 5 4.8 CCN1CCN(c2cc(C)c3cc(NC(=O)CCC(=O)Nc4ccc(F)c(Cl)c4)ccc3n2)CC1 10.1021/jm050103y
70689526 73145 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 558 7 2 7 5.8 Cc1nc(N2CCC(O)(C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016782 73145 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 558 7 2 7 5.8 Cc1nc(N2CCC(O)(C3CCCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44408014 75027 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 452 8 1 4 5.4 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)Cc3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203929 75027 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 452 8 1 4 5.4 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)Cc3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
71731948 122001 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 425 8 0 6 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601298 122001 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 425 8 0 6 3.7 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
56666756 64378 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 473 6 2 2 6.3 CCNC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818808 64378 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 473 6 2 2 6.3 CCNC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
122184566 121887 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 10 1 4 5.3 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600820 121887 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 418 10 1 4 5.3 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccc(OC)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
44407711 75564 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205115 75564 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
44442151 93559 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cc(C#N)ccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL248673 93559 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5cc(C#N)ccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44407944 165438 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL425407 165438 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11677277 141235 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.07.040
CHEMBL386117 141235 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)cc1 10.1016/j.bmcl.2006.07.040
44405409 72040 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1cccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c12 10.1016/j.bmcl.2005.08.049
CHEMBL198692 72040 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1cccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c12 10.1016/j.bmcl.2005.08.049
45270147 193713 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 465 5 2 4 6.2 CC(O)c1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL552010 193713 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 465 5 2 4 6.2 CC(O)c1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
11583925 165207 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL424720 165207 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
44397636 66852 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 430 6 1 5 4.6 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187814 66852 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 430 6 1 5 4.6 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2005.05.023
49865977 16027 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 456 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224231 16027 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 456 6 1 4 5.5 CC(=O)Nc1cccc(C2CCN(CCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
11568741 194385 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 456 7 1 4 4.5 O=C(NCCc1ccccn1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL560584 194385 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 456 7 1 4 4.5 O=C(NCCc1ccccn1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
71226289 128656 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CCCC12COC2 nan
CHEMBL3670648 128656 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1cc(OC2CN(C(=O)c3nnc(-c4ccccc4)o3)C2)ccc1CN1CCCC12COC2 nan
91759559 130731 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 1 7 3.9 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686794 130731 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 1 7 3.9 Cc1cc(CN2CCC(CO)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
71732076 130732 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 1 7 3.6 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686795 130732 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 1 7 3.6 Cc1cc(CN2CCC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
71730791 130792 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 478 9 1 9 2.4 COc1ccc(COc2cnn(CC(=O)c3ccc(CN4CCC(O)CC4)cc3C)c(=O)c2)nc1 nan
CHEMBL3686855 130792 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 478 9 1 9 2.4 COc1ccc(COc2cnn(CC(=O)c3ccc(CN4CCC(O)CC4)cc3C)c(=O)c2)nc1 nan
57396021 69278 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 505 7 1 6 5.2 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C#N)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934828 69278 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 505 7 1 6 5.2 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C#N)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
89690957 138782 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792697 138782 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
89691535 138839 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 391 6 0 5 4.4 CCCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3793182 138839 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 391 6 0 5 4.4 CCCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
89691247 138865 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 6 0 5 5.3 CCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793625 138865 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 6 0 5 5.3 CCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44410878 77739 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 475 5 1 7 4.2 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL210273 77739 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 475 5 1 7 4.2 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2006.02.044
45487392 195300 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 396 10 1 5 3.7 CCCNCc1ccc(COn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL566674 195300 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 396 10 1 5 3.7 CCCNCc1ccc(COn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
90666098 108830 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 562 7 1 5 7.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(Cl)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219001 108830 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 562 7 1 5 7.2 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(Cl)cc4)cc3)CC2)c1 10.1039/C1MD00015B
11454184 70730 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 2 5 5.3 O=C(NCCc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL195319 70730 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 2 5 5.3 O=C(NCCc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
71717700 87350 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337757 87350 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
59135490 91069 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 373 4 1 3 5.1 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403853 91069 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 373 4 1 3 5.1 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
11563153 136030 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373887 136030 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
11591542 79978 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
CHEMBL214535 79978 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
70691720 73191 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 442 5 2 5 4.6 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017594 73191 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 442 5 2 5 4.6 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCC(O)(C5CC5)CC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2012.03.049
11705485 167958 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 470 6 1 5 4.9 CCN1CCN(c2ccc3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL435494 167958 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 470 6 1 5 4.9 CCN1CCN(c2ccc3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1021/jm050103y
44562479 186139 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 475 7 1 5 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2csc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL488711 186139 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 475 7 1 5 5.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2csc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.bmcl.2008.07.079
10244148 65892 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCC(Oc2cccc3ccc(N)nc23)CC1 10.1016/j.bmcl.2004.07.032
CHEMBL184573 65892 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCC(Oc2cccc3ccc(N)nc23)CC1 10.1016/j.bmcl.2004.07.032
91759572 130761 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 462 8 1 8 2.5 Cc1cc(CN2C[C@H](C)O[C@H](N)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3686825 130761 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 462 8 1 8 2.5 Cc1cc(CN2C[C@H](C)O[C@H](N)C2)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
71731047 130767 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 450 8 0 7 3.5 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686830 130767 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 450 8 0 7 3.5 Cc1cc(CN2CCCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
91759584 130773 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686836 130773 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
11153928 165216 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 404 5 2 4 4.2 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)[nH]c2c1 10.1016/j.bmcl.2006.11.092
CHEMBL424739 165216 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 404 5 2 4 4.2 O=C(COc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCC3)[nH]c2c1 10.1016/j.bmcl.2006.11.092
59835766 121891 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 400 8 0 4 4.9 CCN(CC)CCOc1ccc(C#Cc2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600824 121891 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 400 8 0 4 4.9 CCN(CC)CCOc1ccc(C#Cc2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
89690864 138896 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793944 138896 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
86582974 120742 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3578242 120742 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117816804 120743 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.5 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578243 120743 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.5 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
45270139 193617 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 466 5 1 4 5.3 CC(=O)N(C)Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL551408 193617 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 466 5 1 4 5.3 CC(=O)N(C)Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
11533195 194062 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 486 7 3 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N[C@H](CO)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL557329 194062 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 486 7 3 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N[C@H](CO)c1ccccc1 10.1016/j.bmcl.2009.05.066
18435984 74516 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 432 4 1 3 5.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccc(F)cc2)CC1 10.1021/jm201596h
CHEMBL2031722 74516 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 432 4 1 3 5.4 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccc(F)cc2)CC1 10.1021/jm201596h
11292322 153865 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@H]3C[C@H]4C[C@H](NCc5ccsc5)[C@@H]3C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL398864 153865 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@H]3C[C@H]4C[C@H](NCc5ccsc5)[C@@H]3C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
49865680 15871 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 481 8 2 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223769 15871 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 481 8 2 5 6.0 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(C)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
49865739 15926 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(OC(F)(F)F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223885 15926 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 565 10 2 6 6.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(OC(F)(F)F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44390733 62150 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 537 7 2 6 5.9 CN(C)c1nc(NC2CCC(NCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL178084 62150 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 537 7 2 6 5.9 CN(C)c1nc(NC2CCC(NCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
21939887 64363 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 399 5 2 3 4.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(N)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818790 64363 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 399 5 2 3 4.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(N)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
44417960 81370 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 472 5 1 4 3.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)nc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2019.126741
CHEMBL216429 81370 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 472 5 1 4 3.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)nc1)[C@H]1CCc2cc(CN3CCNC(=O)C3)ccc2C1 10.1016/j.bmcl.2019.126741
44394997 64210 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 446 10 3 4 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL181492 64210 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 446 10 3 4 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.07.077
1562 884 8 None - 2 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
5312114 884 8 None - 2 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
CHEMBL17645 884 8 None - 2 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
CHEMBL195380 884 8 None - 2 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
11974034 81671 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(C(F)(F)F)ccc2o1 10.1021/jm060683e
CHEMBL216577 81671 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(C(F)(F)F)ccc2o1 10.1021/jm060683e
70687537 73189 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 526 6 2 6 5.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017592 73189 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 526 6 2 6 5.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
70691656 73146 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 552 7 2 7 5.3 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016783 73146 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 552 7 2 7 5.3 Cc1nc(N2CCC(O)(c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442050 93799 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 327 7 2 5 3.8 COc1ccc2nc(NCCNCc3ccsc3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250118 93799 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 327 7 2 5 3.8 COc1ccc2nc(NCCNCc3ccsc3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
71731946 130722 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 9 1 7 3.6 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686785 130722 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 9 1 7 3.6 Cc1cc(CN2CCC[C@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
91759557 130727 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 1 7 3.6 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686790 130727 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 1 7 3.6 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
10466405 123346 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.2 CCC(C)COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL362720 123346 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.2 CCC(C)COc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44418009 81437 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL216455 81437 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 441 5 1 3 6.2 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCCCCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
70683287 73209 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 446 8 3 6 4.3 Cc1nc(NCCCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017612 73209 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 446 8 3 6 4.3 Cc1nc(NCCCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
122184564 121885 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 467 8 2 2 5.3 CCNC(=O)N(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2F)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600818 121885 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 467 8 2 2 5.3 CCNC(=O)N(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2F)cc1 10.1016/j.bmcl.2015.05.077
86582974 120742 1 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3578242 120742 1 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1c2cc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
45271114 193683 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 526 5 2 4 5.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCC(c2ccccc2O)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL551886 193683 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 526 5 2 4 5.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCC(c2ccccc2O)CC1 10.1016/j.bmcl.2009.05.066
70691650 73096 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016707 73096 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCN(C(=O)C(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
122184569 121890 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 404 11 0 4 5.3 CCN(CC)CCOc1ccc(CCc2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600823 121890 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 404 11 0 4 5.3 CCN(CC)CCOc1ccc(CCc2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
24952419 91084 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403868 91084 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
10399494 66155 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 2 1 3 3.5 Nc1ccc2cccc(OC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL185235 66155 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 2 1 3 3.5 Nc1ccc2cccc(OC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
11581666 75560 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 378 7 1 5 3.3 COc1ccc(CC(=O)Nc2ccc3cnn(CCN4CCCC4)c3c2)cc1 10.1021/jm0512286
CHEMBL205106 75560 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 378 7 1 5 3.3 COc1ccc(CC(=O)Nc2ccc3cnn(CCN4CCCC4)c3c2)cc1 10.1021/jm0512286
44143490 192067 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 416 6 1 4 5.1 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cnc2n1 10.1016/j.bmcl.2009.04.147
CHEMBL521903 192067 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 416 6 1 4 5.1 CC(C)N(C)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cnc2n1 10.1016/j.bmcl.2009.04.147
11246373 93859 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@H]3C[C@@H]4C[C@H](NCc5ccsc5)[C@H]3C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250528 93859 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@H]3C[C@@H]4C[C@H](NCc5ccsc5)[C@H]3C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
91759558 130729 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 411 8 1 6 3.4 CNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
CHEMBL3686792 130729 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 411 8 1 6 3.4 CNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)c(C)c1 nan
91759560 130733 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 1 7 4.0 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686796 130733 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 1 7 4.0 Cc1cc(CN2CCCC[C@@H]2CO)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
89690365 137634 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769550 137634 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)nc3=O)cn12 10.1021/acs.jmedchem.5b01704
54579973 60303 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 470 9 1 4 5.6 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760245 60303 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 470 9 1 4 5.6 COc1ccc([C@H]2CN(CCCC3CCOCC3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
89691247 138865 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 6 0 5 5.3 CCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793625 138865 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 6 0 5 5.3 CCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44562563 173778 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)n[nH]2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL455144 173778 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 468 5 1 3 6.4 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)n[nH]2)cc1 10.1016/j.bmcl.2008.07.079
11555572 194519 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 8 0 4 5.2 CCN(CC)C(=O)C1CCCN(C(=O)CC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C1 10.1016/j.bmcl.2009.05.067
CHEMBL561463 194519 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 8 0 4 5.2 CCN(CC)C(=O)C1CCCN(C(=O)CC2CCN(Cc3ccn(-c4ccc(C(F)(F)F)cc4)c3)CC2)C1 10.1016/j.bmcl.2009.05.067
44394939 65806 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 445 10 2 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184205 65806 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 445 10 2 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44403454 71384 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 492 6 2 6 4.1 O=C(Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccn1 10.1016/j.bmcl.2005.06.089
CHEMBL196620 71384 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 492 6 2 6 4.1 O=C(Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccn1 10.1016/j.bmcl.2005.06.089
44403445 165813 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 474 8 2 7 3.8 COc1ccc(NCc2ccccn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL427542 165813 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 474 8 2 7 3.8 COc1ccc(NCc2ccccn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44424073 85184 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 7 0 3 3.3 O=C1CN(C(=O)Cc2ccc(F)cc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228294 85184 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 7 0 3 3.3 O=C1CN(C(=O)Cc2ccc(F)cc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
44417907 81046 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 449 6 1 3 6.6 CN(c1ccccc1)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL215989 81046 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 449 6 1 3 6.6 CN(c1ccccc1)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44143489 187356 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 416 6 1 4 5.1 CC(C)N(C)c1ccc2nc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2009.04.147
CHEMBL497005 187356 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 416 6 1 4 5.1 CC(C)N(C)c1ccc2nc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2009.04.147
71226696 128660 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 526 8 0 8 4.0 COc1cc(OC2CN(C(=O)c3nnc(-c4ccc(C(F)F)cc4)o3)C2)ccc1CN1CCCC12COC2 nan
CHEMBL3670651 128660 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 526 8 0 8 4.0 COc1cc(OC2CN(C(=O)c3nnc(-c4ccc(C(F)F)cc4)o3)C2)ccc1CN1CCCC12COC2 nan
71731046 130698 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 436 8 0 7 3.1 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686761 130698 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 436 8 0 7 3.1 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
71731947 130724 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 7 3.2 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686787 130724 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 7 3.2 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
11589812 81136 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 419 4 2 4 3.8 O=C(NC1CCN(Cc2ccc3[nH]ccc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216180 81136 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 419 4 2 4 3.8 O=C(NC1CCN(Cc2ccc3[nH]ccc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
10126754 81131 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 402 5 3 3 5.1 CCCc1cc(N)c2cc(NC(=O)NCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216145 81131 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 402 5 3 3 5.1 CCCc1cc(N)c2cc(NC(=O)NCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
59691557 121914 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 7 1 2 6.6 O=C(CCc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600974 121914 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 7 1 2 6.6 O=C(CCc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
90469437 120744 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578244 120744 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 445 5 0 6 5.5 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
117816748 138880 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793841 138880 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
71660914 138769 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 5 4.0 CCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3792485 138769 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 5 4.0 CCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
45272853 194050 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 537 8 2 6 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1cncn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL557262 194050 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 537 8 2 6 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(Cn1cncn1)c1ccccc1 10.1016/j.bmcl.2009.05.066
11634823 15948 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 506 9 2 6 5.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223966 15948 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 506 9 2 6 5.6 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(C#N)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44424067 142643 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of MCHR1Inhibition of MCHR1
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(C(F)(F)F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL389618 142643 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of MCHR1Inhibition of MCHR1
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(C(F)(F)F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44390787 122037 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 443 5 2 5 4.3 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360159 122037 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 443 5 2 5 4.3 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)c(F)c3F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44394705 124788 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(O[C@@H]3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364540 124788 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 385 3 1 6 3.8 Nc1ccc2cccc(O[C@@H]3CCN(c4ccc5c(c4)OC(F)(F)O5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11397595 124083 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 485 9 2 6 5.6 COC[C@@H]1CCCN1CCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
CHEMBL364071 124083 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 485 9 2 6 5.6 COC[C@@H]1CCCN1CCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
57392548 69283 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 522 8 1 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C(C)C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934833 69283 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 522 8 1 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C(C)C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
21939940 64364 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 409 5 1 3 5.1 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(C#N)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818791 64364 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 409 5 1 3 5.1 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(C#N)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
21939935 64367 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 6 1 3 6.1 CON(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818796 64367 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 6 1 3 6.1 CON(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
89690368 138953 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)nn12 10.1016/j.bmc.2016.04.011
CHEMBL3794523 138953 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)nn12 10.1016/j.bmc.2016.04.011
11591542 79978 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
CHEMBL214535 79978 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
20779429 60206 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 454 5 3 3 5.5 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCNCC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
CHEMBL175860 60206 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 454 5 3 3 5.5 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCNCC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
91759554 130723 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 7 3.2 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686786 130723 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 7 3.2 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
89691535 138839 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 391 6 0 5 4.4 CCCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3793182 138839 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 391 6 0 5 4.4 CCCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
11974346 140956 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 422 5 1 5 3.5 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
CHEMBL384487 140956 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 422 5 1 5 3.5 CC(=O)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1021/jm060683e
11712583 193487 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 474 6 2 3 5.1 O=C(NCc1cccc(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL550410 193487 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 474 6 2 3 5.1 O=C(NCc1cccc(F)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
11719912 194203 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 2 4 4.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCCC1CCO 10.1016/j.bmcl.2009.05.066
CHEMBL558928 194203 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 2 4 4.4 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCCC1CCO 10.1016/j.bmcl.2009.05.066
44442156 153842 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(C#N)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL398748 153842 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 439 6 2 6 5.0 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(C#N)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11706442 194123 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 7 2 3 6.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.05.067
CHEMBL558052 194123 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 7 2 3 6.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.05.067
127030071 138634 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 506 7 1 8 3.6 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CC(O)C(C)(C)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787462 138634 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 506 7 1 8 3.6 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CC(O)C(C)(C)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
127031356 138648 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 7 1 8 3.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCC(O)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787642 138648 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 7 1 8 3.0 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCC(O)C5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
11440762 81715 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 392 6 1 6 3.6 COc1ccc(OCC(=O)Nc2ccc3nc(N4CCCC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2006.11.092
CHEMBL216754 81715 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 392 6 1 6 3.6 COc1ccc(OCC(=O)Nc2ccc3nc(N4CCCC4)nc(C)c3c2)cc1 10.1016/j.bmcl.2006.11.092
44403533 71097 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 469 8 3 5 4.6 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL196168 71097 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 469 8 3 5 4.6 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
44395021 65860 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 436 9 3 4 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(F)c(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184439 65860 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 436 9 3 4 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(F)c(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
11974132 79780 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 420 4 1 6 3.2 Cc1ccc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2c1 10.1021/jm060683e
CHEMBL213658 79780 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 420 4 1 6 3.2 Cc1ccc2oc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc(=O)c2c1 10.1021/jm060683e
44408013 74691 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203544 74691 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
70693796 73206 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 420 5 1 4 5.6 Cc1nc(N(C)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017609 73206 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 420 5 1 4 5.6 Cc1nc(N(C)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11464405 80070 18 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL214731 80070 18 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
11662657 80697 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
CHEMBL215661 80697 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 463 4 2 5 3.8 CC(=O)Nc1ccc2c(c1)C(N1CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC1)CC2 10.1016/j.bmcl.2006.11.061
11510399 81122 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 436 4 1 5 4.5 O=C(NC1CCN(Cc2ccc3sccc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216104 81122 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 436 4 1 5 4.5 O=C(NC1CCN(Cc2ccc3sccc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
44417847 82009 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 7 2 3 5.4 CCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
CHEMBL217462 82009 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 373 7 2 3 5.4 CCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
44417911 82013 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 1 3 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL217487 82013 1 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 1 3 5.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCC3)ccc2c1 10.1016/j.bmcl.2006.08.006
44418002 82139 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 409 5 2 3 5.2 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Br)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217845 82139 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 409 5 2 3 5.2 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Br)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
10456755 70739 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195351 70739 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
25114287 60235 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 504 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)cc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1760012 60235 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 504 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)cc4Cl)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25114067 60451 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 488 7 1 4 6.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)c(F)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761120 60451 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 488 7 1 4 6.2 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)c(F)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70685409 73246 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 575 6 1 7 4.5 Cc1nc(N2CCC(N3CCCS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017748 73246 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 575 6 1 7 4.5 Cc1nc(N2CCC(N3CCCS3(=O)=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
122184671 121918 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 420 8 1 4 5.8 Clc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600978 121918 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 420 8 1 4 5.8 Clc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
122184699 121967 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 451 9 1 5 5.0 OCC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601040 121967 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 451 9 1 5 5.0 OCC1CCN(Cc2ccc(OCCCc3ccc(-c4ccc(Cl)cc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
59835780 121952 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 448 5 0 3 6.1 CC1CCN(CCOc2ccc(C#Cc3ncc(-c4ccc(Cl)cc4)cc3F)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3601021 121952 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 448 5 0 3 6.1 CC1CCN(CCOc2ccc(C#Cc3ncc(-c4ccc(Cl)cc4)cc3F)cc2)CC1 10.1016/j.bmcl.2015.05.077
59835879 121954 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 446 6 1 4 4.9 Cc1cc(C#Cc2ccc(-c3ccc(Cl)cc3)cn2)ccc1OCCN1CCC[C@H]1CO 10.1016/j.bmcl.2015.05.077
CHEMBL3601023 121954 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 446 6 1 4 4.9 Cc1cc(C#Cc2ccc(-c3ccc(Cl)cc3)cn2)ccc1OCCN1CCC[C@H]1CO 10.1016/j.bmcl.2015.05.077
44438750 92967 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 571 9 1 8 3.9 O=C(NC1CCN(Cc2ccc(OCCCN3C(=O)CSC3=O)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL245844 92967 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 571 9 1 8 3.9 O=C(NC1CCN(Cc2ccc(OCCCN3C(=O)CSC3=O)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
11442761 139640 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 469 7 2 5 6.3 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCCCC2)c1 10.1021/jm0512286
CHEMBL380429 139640 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 469 7 2 5 6.3 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCCCC2)c1 10.1021/jm0512286
10075375 75634 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 520 5 1 7 4.9 O=c1nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL205493 75634 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 520 5 1 7 4.9 O=c1nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
20817761 76900 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 411 4 2 6 4.4 Oc1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1 10.1016/j.bmcl.2006.02.044
CHEMBL208028 76900 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 411 4 2 6 4.4 Oc1cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n1 10.1016/j.bmcl.2006.02.044
45268470 194611 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL562136 194611 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
23120586 195052 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL565105 195052 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 436 4 1 4 5.9 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
44143495 183663 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 430 6 2 3 5.5 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL483674 183663 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 430 6 2 3 5.5 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCC1 10.1016/j.bmcl.2009.04.147
45270802 193398 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 531 10 1 4 5.6 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N(CCCO)Cc1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL549635 193398 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 531 10 1 4 5.6 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N(CCCO)Cc1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
49866036 16040 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 520 8 1 4 6.9 CC(=O)Nc1cccc(C2CCN(CCCC(F)(F)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224306 16040 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 520 8 1 4 6.9 CC(=O)Nc1cccc(C2CCN(CCCC(F)(F)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44403517 71158 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1cscn1 10.1016/j.bmcl.2005.06.089
CHEMBL196277 71158 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1cscn1 10.1016/j.bmcl.2005.06.089
20817800 70059 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 390 5 1 5 4.2 COc1ccc2oc(O)c/c(=N\C3CCN(C/C=C/c4ccccc4)CC3)c2c1 10.1021/jm050598r
CHEMBL194576 70059 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 390 5 1 5 4.2 COc1ccc2oc(O)c/c(=N\C3CCN(C/C=C/c4ccccc4)CC3)c2c1 10.1021/jm050598r
9910346 64386 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818901 64386 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 1 2 6.2 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2011.07.038
10050565 75338 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204801 75338 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCN[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
18436120 74515 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 442 5 1 4 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)nc1 10.1021/jm201596h
CHEMBL2031721 74515 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 442 5 1 4 5.8 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccc(Cl)cc2)nc1 10.1021/jm201596h
53322555 56398 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2cccc(Cl)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642474 56398 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 424 8 0 5 4.5 O=c1cc(OCc2cccc(Cl)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
23022536 76016 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059418 76016 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCC3)cnc12 10.1021/jm300167z
11634230 69816 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL194046 69816 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 472 8 2 5 5.5 Cc1cc(NC(C)CN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
23022509 76013 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 433 8 1 4 5.3 Cc1c(NC(=O)CCCC(=O)c2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059415 76013 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 433 8 1 4 5.3 Cc1c(NC(=O)CCCC(=O)c2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
44417821 80132 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 421 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214888 80132 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 421 5 2 3 6.3 CCCc1cc(N)c2cc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)ccc2n1 10.1016/j.bmcl.2006.08.008
57403785 68505 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 448 5 1 2 6.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922271 68505 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 448 5 1 2 6.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCCC3CCOCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
23120512 193628 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL551470 193628 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
57522704 76009 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 7 1 4 5.4 Cc1c(NC(=O)c2ccc(OCC(C)C)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059411 76009 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 7 1 4 5.4 Cc1c(NC(=O)c2ccc(OCC(C)C)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
24780883 56404 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 404 8 0 5 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642482 56404 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 404 8 0 5 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCCC2)cc1 10.1016/j.bmc.2010.12.002
45487284 195974 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 422 11 0 4 5.0 CCCN(CC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL570987 195974 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 422 11 0 4 5.0 CCCN(CC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
10173726 80418 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 449 5 2 3 6.7 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215258 80418 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 449 5 2 3 6.7 CCCc1cc(N)c2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
57396294 67731 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914637 67731 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44390750 63133 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 423 5 2 5 4.5 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL179878 63133 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 423 5 2 5 4.5 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
56666755 64376 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 6 1 2 6.5 CCC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818806 64376 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 6 1 2 6.5 CCC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
45273703 194096 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 395 3 1 3 5.6 Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL557731 194096 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 395 3 1 3 5.6 Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
45487657 197305 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 425 4 1 4 5.3 Fc1cc2c(cn1)C1(CCN(Cc3ccc(Nc4ccc(F)c(F)c4)cc3)CC1)OC2 10.1016/j.bmcl.2009.07.132
CHEMBL585509 197305 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 425 4 1 4 5.3 Fc1cc2c(cn1)C1(CCN(Cc3ccc(Nc4ccc(F)c(F)c4)cc3)CC1)OC2 10.1016/j.bmcl.2009.07.132
44390778 63933 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 403 5 2 5 4.2 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
CHEMBL180962 63933 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 403 5 2 5 4.2 Cc1cccc(C(=O)N[C@H]2CC[C@@H](Nc3nc(N(C)C)c4ccccc4n3)CC2)c1 10.1016/j.bmcl.2005.05.121
57392824 67726 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914632 67726 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44407836 74901 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203699 74901 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 504 10 2 6 5.5 Cc1cc(NCC(C)(C)CN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11635274 138146 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 544 5 1 3 7.4 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(CC3CC3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL377843 138146 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 544 5 1 3 7.4 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(CC3CC3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
44417999 81780 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 7 2 3 6.3 CCCc1cc(NCC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217061 81780 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 7 2 3 6.3 CCCc1cc(NCC)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
23120564 194860 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 435 4 1 3 6.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563725 194860 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 435 4 1 3 6.5 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cn12 10.1016/j.bmcl.2009.06.101
45271839 194862 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 382 4 1 4 5.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
CHEMBL563728 194862 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 382 4 1 4 5.1 Cc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
155531314 171036 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL4465399 171036 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
45487391 197340 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 450 12 0 4 5.7 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)CC(C)C 10.1016/j.bmcl.2009.07.023
CHEMBL585879 197340 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 450 12 0 4 5.7 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)CC(C)C 10.1016/j.bmcl.2009.07.023
9807658 64200 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 551 8 2 6 6.1 CN(C)c1nc(NC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181466 64200 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 551 8 2 6 6.1 CN(C)c1nc(NC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
155538229 171793 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 492 8 1 3 6.8 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5ccccc5c4)CC3)cc2)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4476156 171793 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 492 8 1 3 6.8 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5ccccc5c4)CC3)cc2)cc1 10.1016/j.bmcl.2019.126741
91759543 130706 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 0 6 3.5 Cc1cc(CN2CCOCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686769 130706 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 0 6 3.5 Cc1cc(CN2CCOCC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
44405645 72105 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 452 5 1 7 4.5 O=C(C1CC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
CHEMBL198890 72105 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 452 5 1 7 4.5 O=C(C1CC1)n1nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2005.08.049
44405468 132898 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 474 6 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL370576 132898 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 474 6 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
44405518 139816 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 390 4 2 3 5.4 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5ccccc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL380782 139816 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 390 4 2 3 5.4 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5ccccc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44394569 65870 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 285 4 1 4 3.1 CC(CN1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184477 65870 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 285 4 1 4 3.1 CC(CN1CCCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
11281523 81376 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 418 5 1 5 4.2 Cn1c(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2006.11.092
CHEMBL216430 81376 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 418 5 1 5 4.2 Cn1c(N2CCCC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2006.11.092
44418010 81137 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 7 2 3 6.4 CCCc1cc(NC2CC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL216184 81137 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 439 7 2 3 6.4 CCCc1cc(NC2CC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
60169097 87319 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 495 8 0 6 5.5 COc1cc(N2Cc3ccc(Sc4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337726 87319 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 495 8 0 6 5.5 COc1cc(N2Cc3ccc(Sc4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
57390738 69261 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 492 7 1 5 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c(C)c(C)c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934812 69261 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 492 7 1 5 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4)c(C)c(C)c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57395050 68499 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 419 3 1 2 5.3 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCCCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922265 68499 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 419 3 1 2 5.3 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCCCC3)C[C@@H]21 10.1016/j.bmcl.2011.09.110
52917998 60293 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760234 60293 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 508 10 1 5 5.7 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
70683781 74586 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 478 5 2 3 5.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3(C(=O)O)CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032047 74586 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 478 5 2 3 5.4 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCCC3(C(=O)O)CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
71660915 138870 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793767 138870 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 389 5 0 5 4.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45271111 193654 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 531 5 1 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL551684 193654 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 531 5 1 4 4.5 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.066
45273401 194090 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 463 6 2 4 4.5 O=C(NCC1(O)CCCCC1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL557715 194090 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 463 6 2 4 4.5 O=C(NCC1(O)CCCCC1)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
24952056 91073 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 5 2 4 5.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403857 91073 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 5 2 4 5.4 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2013.05.017
127031354 138562 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCOCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786662 138562 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 7 0 8 3.3 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCOCC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
11627122 141194 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 480 8 3 4 5.2 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2006.07.040
CHEMBL385831 141194 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 480 8 3 4 5.2 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2006.07.040
44407860 75055 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204082 75055 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44407870 75546 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204968 75546 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44403467 70183 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 490 7 2 5 6.0 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL194726 70183 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 490 7 2 5 6.0 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
44403505 133034 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 467 8 2 7 3.3 COc1ccc(NCC2CCOC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL371129 133034 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 467 8 2 7 3.3 COc1ccc(NCC2CCOC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44402350 71669 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 512 9 3 6 5.1 NC(=O)C1CCN(CCCn2ncc3cc(NC(=O)Nc4ccc(Oc5ccccc5)cc4)ccc32)CC1 10.1016/j.bmcl.2005.03.114
CHEMBL197571 71669 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 512 9 3 6 5.1 NC(=O)C1CCN(CCCn2ncc3cc(NC(=O)Nc4ccc(Oc5ccccc5)cc4)ccc32)CC1 10.1016/j.bmcl.2005.03.114
11678370 136029 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373886 136029 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 548 9 3 4 7.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(-c3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44417824 141307 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)Cc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386509 141307 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 5 2 3 5.0 CCCc1cc(N)c2cc(NC(=O)Cc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11410594 96740 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 576 9 1 5 5.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL268385 96740 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 576 9 1 5 5.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
11562129 70718 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195250 70718 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 5 2 5 5.3 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44394826 66257 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 585 9 1 5 9.0 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCc5ccc(-c6cccc(C(F)(F)F)c6)o5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL185266 66257 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 585 9 1 5 9.0 CC(C)Cc1ccc(N2CCC(Oc3cccc4ccc(NCc5ccc(-c6cccc(C(F)(F)F)c6)o5)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
10083869 65228 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65228 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
11201645 71512 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL197050 71512 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 445 7 2 5 4.5 Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
70687549 73248 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 541 6 1 7 4.9 Cc1nc(N2CCC(N3CCOC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017750 73248 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 541 6 1 7 4.9 Cc1nc(N2CCC(N3CCOC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
70693808 73257 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 479 6 3 6 3.3 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017759 73257 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 479 6 3 6 3.3 Cc1nc(N2CCC(NC(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44193451 122000 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 411 8 0 6 3.4 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601297 122000 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 411 8 0 6 3.4 CN(C)Cc1ccc(C(=O)Cn2ccc(OCc3ccc(Cl)cn3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
89691065 138918 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794150 138918 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 445 5 0 6 5.3 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44143502 187390 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 405 6 2 4 4.4 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497221 187390 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 405 6 2 4 4.4 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cn3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
44562404 176380 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 1 3 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462347 176380 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 1 3 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.07.079
11706443 194539 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 8 1 4 6.4 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ccccn1 10.1016/j.bmcl.2009.05.067
CHEMBL561585 194539 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 532 8 1 4 6.4 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccccc1)c1ccccn1 10.1016/j.bmcl.2009.05.067
44402484 132994 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL370839 132994 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.4 O=C(Nc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
11282448 62231 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2nn(CCN3CCCC3)cc12 10.1021/jm0490890
CHEMBL178259 62231 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1cccc2nn(CCN3CCCC3)cc12 10.1021/jm0490890
60168817 87332 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 5 4.5 COc1cc(N2Cc3ccc(Cc4cccc(F)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337739 87332 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 5 4.5 COc1cc(N2Cc3ccc(Cc4cccc(F)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89690239 137666 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 413 6 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(C)C)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769899 137666 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 413 6 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(C)C)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44403547 133078 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 433 7 3 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
CHEMBL371355 133078 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 433 7 3 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccccc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
44403500 134678 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 432 7 2 4 4.6 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
CHEMBL372245 134678 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 432 7 2 4 4.6 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCC1CC1 10.1016/j.bmcl.2005.06.089
44442054 93824 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@@H]3CCC[C@@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250321 93824 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 381 6 2 5 5.1 COc1ccc2nc(N[C@@H]3CCC[C@@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
45268644 194533 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 514 8 3 4 5.0 O=C(O)CC(NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL561546 194533 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 514 8 3 4 5.0 O=C(O)CC(NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
71716477 87337 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 447 7 0 5 4.5 COc1cc(N2Cc3ccc(-c4ccccc4F)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337744 87337 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 447 7 0 5 4.5 COc1cc(N2Cc3ccc(-c4ccccc4F)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
11662564 132990 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 459 8 1 5 5.0 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370820 132990 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 459 8 1 5 5.0 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
137644041 157891 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
CHEMBL4090568 157891 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
45269996 194737 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 531 5 0 4 4.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCN(C(=O)N2CCCC2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL562905 194737 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 531 5 0 4 4.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCN(C(=O)N2CCCC2)CC1 10.1016/j.bmcl.2009.05.067
137644041 157891 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
CHEMBL4090568 157891 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 0 6 3.2 O=C1COc2ccccc2N1CCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm5013243
25114064 60446 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 544 9 1 5 7.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Oc5ccccc5)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761115 60446 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 544 9 1 5 7.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Oc5ccccc5)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
89690318 137765 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 371 5 0 5 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770954 137765 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 371 5 0 5 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44574358 178121 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 467 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(C)cc2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL468299 178121 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 467 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(C)cc2)cc1 10.1016/j.bmcl.2009.04.016
44574359 178148 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2cccc(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL468509 178148 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2cccc(F)c2)cc1 10.1016/j.bmcl.2009.04.016
11634061 191745 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 463 7 1 4 4.5 O=C(COc1cccc(Cl)c1)NC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
CHEMBL520714 191745 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 463 7 1 4 4.5 O=C(COc1cccc(Cl)c1)NC1CN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)C1 10.1016/j.bmcl.2008.07.079
127033945 138411 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 491 7 0 8 3.2 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCN(C)CC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3785118 138411 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from human MCHR1 expressed in CHO cell membranes after 60 mins by microbeta scintillation counting analysis
ChEMBL 491 7 0 8 3.2 COc1ccc(-c2nnc(C(=O)N3CCC(Oc4ccc(CN5CCN(C)CC5)cc4)CC3)o2)cc1 10.1021/acs.jmedchem.5b01654
44407991 168875 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL442794 168875 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
71225876 128657 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1cc(CN2CCCC23COC3)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 nan
CHEMBL3670649 128657 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1cc(CN2CCCC23COC3)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 nan
122184568 121889 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 10 0 4 5.6 CCN(CC)CCOc1ccc(/C=C/c2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600822 121889 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 10 0 4 5.6 CCN(CC)CCOc1ccc(/C=C/c2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
57394273 69281 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 523 8 1 6 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(N(C)C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934831 69281 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 523 8 1 6 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(N(C)C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
44408013 74691 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203544 74691 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 478 7 1 4 6.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc12 10.1016/j.bmcl.2005.10.066
137657882 159115 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
CHEMBL4104013 159115 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
137657882 159115 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
CHEMBL4104013 159115 0 None - 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 6 2.1 O=C1COc2ccccc2N1CCCN1CCN(c2cccc3[nH]c(=O)oc23)CC1 10.1021/jm5013243
11973798 79873 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 6 1 6 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1OC 10.1021/jm060683e
CHEMBL214075 79873 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 6 1 6 3.3 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1OC 10.1021/jm060683e
44143501 187389 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 418 5 2 4 4.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCOCC3)[nH]c2c1 10.1016/j.bmcl.2009.04.147
CHEMBL497220 187389 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 418 5 2 4 4.0 O=C(CCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc(N3CCOCC3)[nH]c2c1 10.1016/j.bmcl.2009.04.147
44417910 82002 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 4 2 6 2.8 O=C(NC1CCN(Cc2ccc3oc(=O)[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL217435 82002 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 4 2 6 2.8 O=C(NC1CCN(Cc2ccc3oc(=O)[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
44417992 82031 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 6 1 3 5.9 CCCc1cc(N(C)C)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217575 82031 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 6 1 3 5.9 CCCc1cc(N(C)C)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11495754 71573 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL197245 71573 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 433 7 2 5 4.3 Cc1cc(N(C)CCO)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
117816804 120743 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 389 5 0 5 4.5 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
CHEMBL3578243 120743 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 389 5 0 5 4.5 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C1CC1 10.1016/j.bmc.2016.04.013
89691032 138898 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 371 5 0 5 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793953 138898 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 371 5 0 5 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44562442 178600 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 505 7 1 4 5.9 CC(c1ccn(-c2ccc(C(F)(F)F)cc2)c1)N1CCC(NC(=O)COc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472379 178600 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 505 7 1 4 5.9 CC(c1ccn(-c2ccc(C(F)(F)F)cc2)c1)N1CCC(NC(=O)COc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2008.07.079
155524512 170389 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 370 4 3 6 2.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(O)cc(O)c1 10.1016/j.bmcl.2019.126741
CHEMBL4455933 170389 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 370 4 3 6 2.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(O)cc(O)c1 10.1016/j.bmcl.2019.126741
44397033 66789 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 370 4 3 6 2.2 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(O)cc(O)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187553 66789 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 370 4 3 6 2.2 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cc(O)cc(O)c1 10.1016/j.bmcl.2005.05.023
702501 157030 18 None - 0 Human 4.4 pIC50 = 4.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 312 4 1 2 3.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4080696 157030 18 None - 0 Human 4.4 pIC50 = 4.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 312 4 1 2 3.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2019.126741
22254575 65975 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 3 1 3 3.0 Nc1ccc2cccc(OCC3CCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184980 65975 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 3 1 3 3.0 Nc1ccc2cccc(OCC3CCC3)c2n1 10.1016/j.bmcl.2004.07.032
10198125 126110 2 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 202 2 1 3 2.6 CC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL365254 126110 2 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 202 2 1 3 2.6 CC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44403748 70266 3 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.4 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OCCC(C)C)cc3)cc12 10.1021/jm050103y
CHEMBL194997 70266 3 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 8 1 5 5.4 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OCCC(C)C)cc3)cc12 10.1021/jm050103y
11527169 77011 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 587 3 1 3 7.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(C(=O)N3CCCC3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL208635 77011 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 587 3 1 3 7.2 N#Cc1cccc(-c2ccc(C3(c4nc5cc(C(F)(F)F)c(F)cc5[nH]4)CC34CCN(C(=O)N3CCCC3)CC4)cc2)c1 10.1016/j.bmcl.2019.126741
89691416 138917 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2cnc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1016/j.bmc.2016.04.011
CHEMBL3794147 138917 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2cnc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1016/j.bmc.2016.04.011
45269336 194298 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL559801 194298 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
44407956 74497 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203161 74497 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11627085 193730 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.5 O=C(NCC1(O)CCCCC1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL552143 193730 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.5 O=C(NCC1(O)CCCCC1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
44405517 71502 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 350 4 2 5 3.4 c1ccc2c(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)[nH]nc2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197023 71502 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 350 4 2 5 3.4 c1ccc2c(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)[nH]nc2c1 10.1016/j.bmcl.2005.08.049
71718319 87353 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337760 87353 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44403749 165657 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 433 6 2 5 4.0 CCN1CCN(c2cc(C)c3cc(NC(=O)NCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL426648 165657 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 433 6 2 5 4.0 CCN1CCN(c2cc(C)c3cc(NC(=O)NCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm050103y
45267386 194325 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 510 6 1 4 5.7 O=C(NCc1ccc(Cl)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL560063 194325 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 510 6 1 4 5.7 O=C(NCc1ccc(Cl)cc1Cl)C1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2009.05.067
71227161 128652 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 nan
CHEMBL3670644 128652 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 476 7 0 8 3.0 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC56COC6)cc4)C3)o2)cc1 nan
44417848 141078 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 8 2 3 5.8 CCCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
CHEMBL385221 141078 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 387 8 2 3 5.8 CCCCc1ccc(/C=C/C(=O)Nc2ccc3nc(CCC)cc(N)c3c2)cc1 10.1016/j.bmcl.2006.08.008
11516903 69922 3 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 400 4 1 4 4.3 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCN(C)CC4)cc(C)c3c2)cc1 10.1021/jm050103y
CHEMBL194253 69922 3 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 400 4 1 4 4.3 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCN(C)CC4)cc(C)c3c2)cc1 10.1021/jm050103y
70681217 73258 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 493 7 2 6 4.0 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017760 73258 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 493 7 2 6 4.0 COCC(=O)NC1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
70693809 73261 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 557 8 1 7 4.6 COCC(=O)N(C)C1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
CHEMBL2017763 73261 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 557 8 1 7 4.6 COCC(=O)N(C)C1CCN(c2nc(C)c3cc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.049
89691032 138898 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 371 5 0 5 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793953 138898 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 371 5 0 5 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
45487641 197341 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cc(=O)n(C)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585880 197341 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cc(=O)n(C)cc23)cn1 10.1016/j.bmcl.2009.07.132
70691649 73093 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 6 1 7 3.9 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016703 73093 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 495 6 1 7 3.9 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
49865653 15851 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223709 15851 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 501 8 2 5 6.3 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3cccc(Cl)c3)CC2)c1 10.1016/j.bmcl.2010.07.086
57402500 67797 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 426 9 1 3 4.9 CC(=O)NCCc1ccc(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.09.007
CHEMBL1914857 67797 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 426 9 1 3 4.9 CC(=O)NCCc1ccc(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.09.007
46899579 16794 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253956 16794 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@H](OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
44402599 125651 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 446 7 2 5 3.9 O=C(Nc1ccc2cnn(CCN3CCCC3)c2c1)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.03.114
CHEMBL364936 125651 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 446 7 2 5 3.9 O=C(Nc1ccc2cnn(CCN3CCCC3)c2c1)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.03.114
52918017 60308 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 469 9 1 4 4.4 COc1ccc([C@H]2CN(CCCN3CCCC3=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760251 60308 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 469 9 1 4 4.4 COc1ccc([C@H]2CN(CCCN3CCCC3=O)C[C@@H]2CC(=O)Nc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
57391045 67791 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.5 CC(=O)N1CCCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914851 67791 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.5 CC(=O)N1CCCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
11419338 74082 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2nn(CCN3CCCC3)cc2c1 10.1021/jm0512286
CHEMBL202741 74082 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2nn(CCN3CCCC3)cc2c1 10.1021/jm0512286
45270303 194941 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.3 O=C(NC[C@@H]1CCCC[C@H]1O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL564243 194941 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.3 O=C(NC[C@@H]1CCCC[C@H]1O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
90666260 108869 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 564 7 1 5 6.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3F)CC2)c1 10.1039/C1MD00015B
CHEMBL3219269 108869 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 564 7 1 5 6.9 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3F)CC2)c1 10.1039/C1MD00015B
89691216 138858 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 417 5 0 5 5.1 Cn1c(C2CCCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793395 138858 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 417 5 0 5 5.1 Cn1c(C2CCCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11563153 136030 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373887 136030 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44417938 96876 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1016/j.bmcl.2006.11.065
CHEMBL269352 96876 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 437 5 2 5 3.3 CC(=O)Nc1cccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c1 10.1016/j.bmcl.2006.11.065
89690379 137639 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 389 5 0 5 4.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769602 137639 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 389 5 0 5 4.4 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89691144 138902 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793989 138902 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11974131 141442 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 431 4 1 7 2.8 N#Cc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL387417 141442 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 431 4 1 7 2.8 N#Cc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
70687473 73112 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCC(C(=O)N(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016723 73112 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 531 7 1 7 4.2 Cc1nc(N2CCC(C(=O)N(C)C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
122184559 121874 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 461 8 2 3 4.7 NC(=O)c1cc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc1CN1CCCC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600808 121874 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 461 8 2 3 4.7 NC(=O)c1cc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc1CN1CCCC1 10.1016/j.bmcl.2015.05.077
66877080 91085 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 4 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@H](NC[C@H]2Cc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2013.05.017
CHEMBL2403869 91085 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 437 4 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@H](NC[C@H]2Cc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2013.05.017
44394910 66657 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 430 10 3 5 4.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(SC)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL186947 66657 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 430 10 3 5 4.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(SC)c2)cc1OC 10.1016/j.bmcl.2004.07.077
44407967 74128 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202854 74128 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
11591169 71387 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2nc3ccc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)cc3cc2C)CC1 10.1021/jm050103y
CHEMBL196627 71387 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2nc3ccc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)cc3cc2C)CC1 10.1021/jm050103y
44407667 74042 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
CHEMBL202563 74042 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
71731804 130707 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 445 8 0 6 3.4 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686770 130707 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 445 8 0 6 3.4 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
71660914 138769 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 5 4.0 CCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3792485 138769 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 5 4.0 CCc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
45268465 194876 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 446 5 1 6 4.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(S(C)(=O)=O)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL563836 194876 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 446 5 1 6 4.2 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(S(C)(=O)=O)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
18435986 74518 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 444 5 1 4 5.3 COc1ccc(C2CCN(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)CC2)cc1 10.1021/jm201596h
CHEMBL2031724 74518 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 444 5 1 4 5.3 COc1ccc(C2CCN(C(=O)Nc3ccc4cc(CN5CCCC5)cnc4c3)CC2)cc1 10.1021/jm201596h
11554989 178475 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL471514 178475 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 492 7 1 5 4.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1 10.1016/j.bmcl.2008.07.079
44407667 74042 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
CHEMBL202563 74042 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 402 7 1 4 4.5 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)cc(C)c3c2)cc1 10.1016/j.bmcl.2005.10.066
57391030 67735 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 453 6 0 4 4.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCN(c4ccccc4Cl)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914648 67735 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 453 6 0 4 4.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCN(c4ccccc4Cl)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
10258364 193106 0 None 1 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 193106 0 None 1 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 193106 0 None 1 2 Human 6.3 pIC50 = 6.3 Binding
Displacement of[125I]MCH from human MCH1R expressed in CHO cellsDisplacement of[125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
44395022 165590 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cc(Cl)cc(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL426252 165590 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cc(Cl)cc(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
44442069 154261 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 405 5 2 4 5.8 FC(F)(F)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL400321 154261 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 405 5 2 4 5.8 FC(F)(F)c1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
91759575 123860 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 452 8 1 8 2.1 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3639387 123860 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 452 8 1 8 2.1 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
45272816 194106 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 528 7 1 5 4.9 COc1ccc(OC2CN(C(=O)NC3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)C2)cc1 10.1016/j.bmcl.2009.05.066
CHEMBL557873 194106 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 528 7 1 5 4.9 COc1ccc(OC2CN(C(=O)NC3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)C2)cc1 10.1016/j.bmcl.2009.05.066
70693732 73100 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 529 7 1 7 3.9 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016711 73100 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 529 7 1 7 3.9 Cc1nc(N2CCN(C(=O)C3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44418008 81428 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 443 9 1 3 6.5 CCCN(CCC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL216454 81428 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 443 9 1 3 6.5 CCCN(CCC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
44397278 66950 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1cccc(CNC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL188340 66950 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1cccc(CNC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.05.023
22254580 66658 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 4 1 3 3.0 Nc1ccc2cccc(OCCC3CC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186949 66658 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 228 4 1 3 3.0 Nc1ccc2cccc(OCCC3CC3)c2n1 10.1016/j.bmcl.2004.07.032
44417963 165447 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4cccc(C(F)(F)F)c4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
CHEMBL425445 165447 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 513 9 1 5 4.7 CCN(CC)Cc1ccc(CCN2CCn3nc(C(=O)Nc4cccc(C(F)(F)F)c4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
44405464 165787 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 485 7 1 8 4.8 O=[N+]([O-])c1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL427367 165787 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 485 7 1 8 4.8 O=[N+]([O-])c1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccc1 10.1016/j.bmcl.2005.08.049
44394856 65788 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 380 6 3 6 3.1 Nc1ccc2cccc(OCCCNC(=O)Nc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184080 65788 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 380 6 3 6 3.1 Nc1ccc2cccc(OCCCNC(=O)Nc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
44394824 123736 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5cccc(Cl)c5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
CHEMBL363464 123736 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 536 10 2 6 6.8 N#Cc1cccc(C(=O)NCCCOc2cccc3ccc(NCc4ccc(-c5cccc(Cl)c5)o4)nc23)c1 10.1016/j.bmcl.2004.07.034
44394611 123815 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363664 123815 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
44394611 123815 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL363664 123815 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 409 7 2 4 5.0 Nc1ccc2cccc(OCCCNCc3ccc(Cl)c(C(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.035
16721015 79996 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL214585 79996 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
11495432 97734 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 419 4 2 4 3.8 O=C(NC1CCN(Cc2ccc3cc[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL274168 97734 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 419 4 2 4 3.8 O=C(NC1CCN(Cc2ccc3cc[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
22018932 79881 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.8 CC1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL214125 79881 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 5 1 3 5.8 CC1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
22018914 80488 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 470 6 2 4 4.5 CC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL215316 80488 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 470 6 2 4 4.5 CC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
44417956 96190 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
CHEMBL263686 96190 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 594 15 1 2 9.8 O=C(CCCCCCCCCCCCc1ccc(C(F)(F)F)cc1)Nc1ccc2nc([N+]34CCC(CC3)CC4)ccc2c1 10.1016/j.bmcl.2006.08.006
10388797 71400 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196667 71400 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 444 5 2 5 4.3 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
57392547 69276 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 498 7 1 5 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(F)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934826 69276 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 498 7 1 5 5.4 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(F)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
25115855 60433 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4cccc(Cl)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761102 60433 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4cccc(Cl)c4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25116079 60442 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 530 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Br)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761111 60442 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 530 7 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Br)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
25114722 60453 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 514 8 1 4 7.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761123 60453 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 514 8 1 4 7.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
122184563 121884 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 487 10 2 4 4.6 CC(=O)CNC1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600817 121884 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 487 10 2 4 4.6 CC(=O)CNC1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
59835728 121897 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 430 5 0 3 5.9 CC1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600830 121897 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 430 5 0 3 5.9 CC1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
9978428 121941 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 401 5 1 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(NCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601011 121941 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 401 5 1 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(NCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
10388351 121947 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 5 0 3 5.9 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)c(Cl)c3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601017 121947 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 436 5 0 3 5.9 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)c(Cl)c3)nc2)cc1 10.1016/j.bmcl.2015.05.077
11408441 140711 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 455 7 2 5 6.0 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCCC2)c1 10.1021/jm0512286
CHEMBL383078 140711 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 455 7 2 5 6.0 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCCC2)c1 10.1021/jm0512286
44410823 75188 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 500 5 1 5 5.8 O=c1nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
CHEMBL204508 75188 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 500 5 1 5 5.8 O=c1nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc2n1CC(F)(F)F 10.1016/j.bmcl.2006.02.044
22348219 76156 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 457 6 1 7 3.9 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)F)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL206030 76156 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 457 6 1 7 3.9 Cn1c(=O)cc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(OC(F)F)ccc21 10.1016/j.bmcl.2006.02.044
20817821 76491 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 431 4 1 4 5.4 Cn1c(=O)cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL206953 76491 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 431 4 1 4 5.4 Cn1c(=O)cc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44410821 76755 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 426 4 1 7 3.4 Cn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207668 76755 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 426 4 1 7 3.4 Cn1c(=O)nc(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
11259253 82119 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Cl)cc2o1 10.1021/jm060683e
CHEMBL217789 82119 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(Cl)cc2o1 10.1021/jm060683e
44442144 154145 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 480 8 2 6 5.8 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OC(F)F)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL399721 154145 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 480 8 2 6 5.8 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OC(F)F)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
45270014 193433 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 11 1 5 6.6 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(OC)nc1 10.1016/j.bmcl.2009.05.067
CHEMBL549984 193433 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 11 1 5 6.6 CCCCC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(OC)nc1 10.1016/j.bmcl.2009.05.067
45487372 195230 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 406 8 0 4 4.4 O=c1cc(OCc2ccc(F)cc2)ccn1CCc1ccc(CN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL566232 195230 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 406 8 0 4 4.4 O=c1cc(OCc2ccc(F)cc2)ccn1CCc1ccc(CN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
9829942 65824 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 589 13 2 4 6.7 O=C(CNC(=O)OCc1ccccc1)NCC(CCCN1CCC(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm040762v
CHEMBL184291 65824 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 589 13 2 4 6.7 O=C(CNC(=O)OCc1ccccc1)NCC(CCCN1CCC(c2ccccc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm040762v
11236807 81140 0 None -1 3 Mouse 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81140 0 None -1 3 Mouse 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11563017 80635 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215418 80635 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 550 8 3 4 6.3 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Br)cc2)cc1C 10.1016/j.bmcl.2006.07.040
11613073 75562 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205111 75562 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 8 2 7 3.6 Cc1cc(N2CCN(CCO)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44390715 123289 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 457 5 2 5 5.2 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL362400 123289 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 457 5 2 5 5.2 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(Cl)c(Cl)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
53325164 56408 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 420 10 0 5 4.9 CC(C)N(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)C(C)C 10.1016/j.bmc.2010.12.002
CHEMBL1642486 56408 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 420 10 0 5 4.9 CC(C)N(CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1)C(C)C 10.1016/j.bmc.2010.12.002
11752320 67375 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 496 6 1 3 6.5 N#Cc1cccc(-c2ccc(N(CCN3CCCC3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL190780 67375 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 496 6 1 3 6.5 N#Cc1cccc(-c2ccc(N(CCN3CCCC3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1016/j.bmcl.2019.126741
57398088 67725 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914631 67725 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
45487390 195400 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 11 0 4 5.4 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)C(C)C 10.1016/j.bmcl.2009.07.023
CHEMBL567514 195400 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 436 11 0 4 5.4 CCCN(Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1)C(C)C 10.1016/j.bmcl.2009.07.023
44394907 165428 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 422 8 3 3 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL425359 165428 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 422 8 3 3 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
23593464 64356 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64356 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
23593464 64356 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64356 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
21939902 64373 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 471 5 1 3 5.8 CN1CCN(CC2=Cc3ccc(NC(=O)c4ccc(-c5ccc(Cl)cc5)cc4)cc3CC2)CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818802 64373 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 471 5 1 3 5.8 CN1CCN(CC2=Cc3ccc(NC(=O)c4ccc(-c5ccc(Cl)cc5)cc4)cc3CC2)CC1 10.1016/j.bmc.2011.07.038
44408108 139271 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 462 9 2 6 4.4 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL379886 139271 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 462 9 2 6 4.4 Cc1cc(NCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
57521366 76027 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
CHEMBL2059512 76027 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 10 3 5 4.4 CC(=O)NCCN[C@@H](C)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1 10.1021/jm300167z
44407944 165438 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL425407 165438 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 502 9 2 6 5.4 Cc1cc(NCCN2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
10186375 78523 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 8 2 3 7.3 N#Cc1cccc(-c2ccc(C(CCN3CCCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2019.126741
CHEMBL2112988 78523 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 520 8 2 3 7.3 N#Cc1cccc(-c2ccc(C(CCN3CCCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2019.126741
11683259 194083 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 423 4 1 3 6.4 CC(C)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL557664 194083 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 423 4 1 3 6.4 CC(C)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
45267577 194284 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL559680 194284 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 386 4 1 4 5.0 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)cn4)cc3)cn12 10.1016/j.bmcl.2009.06.101
45487331 197114 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 452 13 0 5 4.7 CCCN(CCOC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL583348 197114 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 452 13 0 5 4.7 CCCN(CCOC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
10141528 122422 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 495 6 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C=O)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL360731 122422 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 495 6 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C=O)c3)cc2)CC1 10.1016/j.bmcl.2019.126741
4219492 71078 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196091 71078 1 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
56673713 66107 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818803 66107 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1852093 66107 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
1314 3657 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.09.007
9865843 3657 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.09.007
CHEMBL178707 3657 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2011.09.007
9978508 187447 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 403 5 2 4 4.9 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497637 187447 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 403 5 2 4 4.9 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccc(F)cc4)nc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
57522949 76021 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 445 7 2 5 4.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CC[C@H](O)C3)cnc12 10.1021/jm300167z
CHEMBL2059424 76021 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 445 7 2 5 4.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CC[C@H](O)C3)cnc12 10.1021/jm300167z
1314 3657 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2010.12.002
9865843 3657 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2010.12.002
CHEMBL178707 3657 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmc.2010.12.002
1314 3657 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm040762v
9865843 3657 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm040762v
CHEMBL178707 3657 18 None - 1 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1021/jm040762v
56589628 67792 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914852 67792 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
23120576 194095 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 421 4 1 3 6.2 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL557730 194095 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 421 4 1 3 6.2 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.06.101
11654412 197230 22 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL584538 197230 22 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11654412 197230 22 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL584538 197230 22 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmcl.2009.07.023
57522947 76019 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059422 76019 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 457 7 1 4 6.5 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCCC3)cnc12 10.1021/jm300167z
44407991 168875 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL442794 168875 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 438 7 1 4 5.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
44417944 141266 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 4 2 3 6.1 CC(C)(C)Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL386284 141266 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 427 4 2 3 6.1 CC(C)(C)Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
11502008 56263 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 390 8 0 5 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1641614 56263 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 390 8 0 5 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
11512135 69950 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194408 69950 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
10024171 187452 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 6 2 3 5.0 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497646 187452 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 404 6 2 3 5.0 CC(C)N(C)c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
53317306 56396 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2cccc(F)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642472 56396 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2cccc(F)c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
45487382 195711 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 10 0 4 4.7 CCN(CC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
CHEMBL569458 195711 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 408 10 0 4 4.7 CCN(CC)Cc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)cc1 10.1016/j.bmcl.2009.07.023
59135482 91078 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403862 91078 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 462 5 2 5 5.3 CC(C)(O)c1nc2cc(Cl)ccc2n1[C@H]1CC[C@@H](NC[C@@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44390706 121506 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 467 5 2 5 4.6 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Br)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL359510 121506 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 467 5 2 5 4.6 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(Br)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11612403 71051 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 465 7 0 7 4.9 O=c1n(-c2ccc(Oc3ccccc3)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL195914 71051 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 465 7 0 7 4.9 O=c1n(-c2ccc(Oc3ccccc3)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
10185187 62954 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 495 9 3 2 7.5 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
CHEMBL179325 62954 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 495 9 3 2 7.5 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2019.126741
71730133 130739 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 469 9 1 6 3.9 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
CHEMBL3686803 130739 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 469 9 1 6 3.9 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(Br)cn3)cc2=O)c(C)c1 nan
89798653 130770 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 410 8 0 7 2.6 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686833 130770 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 410 8 0 7 2.6 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
9806086 64861 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL182554 64861 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 502 10 3 5 5.7 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
10434776 125848 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL365055 125848 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 468 10 3 5 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44394959 66859 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL187854 66859 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44405570 71633 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 6 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5nsnc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197395 71633 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 6 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5nsnc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44405408 72074 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 376 5 3 5 3.5 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c[nH]nc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL198789 72074 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 376 5 3 5 3.5 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c[nH]nc5c4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44405463 132623 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 460 5 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2-c1ccccc1 10.1016/j.bmcl.2005.08.049
CHEMBL370361 132623 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 460 5 1 6 5.5 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2-c1ccccc1 10.1016/j.bmcl.2005.08.049
10083869 65228 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL183159 65228 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394859 65899 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 257 5 2 4 2.3 CC(CNC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL184589 65899 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 257 5 2 4 2.3 CC(CNC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394573 123152 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 570 10 3 7 7.1 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.07.034
CHEMBL362150 123152 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 570 10 3 7 7.1 O=C(NCCCOc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.07.034
11591169 71387 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2nc3ccc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)cc3cc2C)CC1 10.1021/jm050103y
CHEMBL196627 71387 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 484 6 1 5 5.2 CCN1CCN(c2nc3ccc(NC(=O)/C=C/c4ccc(OC(F)(F)F)cc4)cc3cc2C)CC1 10.1021/jm050103y
60169184 87323 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(F)c(F)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337730 87323 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(F)c(F)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
60169263 87325 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 513 8 0 6 5.7 COc1cc(N2Cc3ccc(Sc4ccc(F)c(Cl)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337732 87325 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 513 8 0 6 5.7 COc1cc(N2Cc3ccc(Sc4ccc(F)c(Cl)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
71719525 87344 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 5.0 CCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
CHEMBL2337751 87344 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 5.0 CCc1ccc(-c2ccc3c(n2)C(=O)N(c2ccc(OCCN4CCCC4)c(OC)c2)C3)cc1 10.1016/j.bmcl.2013.01.053
57396020 69277 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 558 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Br)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934827 69277 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 558 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Br)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
57394275 69287 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934838 69287 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)cc4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
54586089 60435 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4C(F)(F)F)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761104 60435 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 520 7 1 4 7.0 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccccc4C(F)(F)F)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
56683679 64377 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 474 6 1 3 6.7 CCOC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818807 64377 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 474 6 1 3 6.7 CCOC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
44442135 153878 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 487 7 2 6 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc(S(C)(=O)=O)cc4Cl)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL398964 153878 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 487 7 2 6 5.1 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4ccc(S(C)(=O)=O)cc4Cl)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11511219 65789 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL184084 65789 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 474 6 1 6 4.2 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
11496313 71953 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL198361 71953 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
59135471 91068 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 451 4 1 3 5.9 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403852 91068 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 451 4 1 3 5.9 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(Br)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
11304816 65932 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1021/jm040762v
CHEMBL184717 65932 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1021/jm040762v
44397008 66553 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 368 5 1 5 2.8 COc1cccc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186469 66553 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 368 5 1 5 2.8 COc1cccc(C(=O)NC2CCCN(Cc3ccc4c(c3)OCO4)C2)c1 10.1016/j.bmcl.2005.05.023
44397127 66733 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 350 6 1 3 3.6 COc1cccc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187296 66733 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 350 6 1 3 3.6 COc1cccc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2005.05.023
44397026 126636 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1ccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL365714 126636 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1ccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.bmcl.2005.05.023
44403528 70186 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 472 7 2 7 3.4 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC[C@H]1CCCO1 10.1016/j.bmcl.2005.06.089
CHEMBL194731 70186 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 472 7 2 7 3.4 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC[C@H]1CCCO1 10.1016/j.bmcl.2005.06.089
44403499 70758 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 479 8 2 6 4.8 COc1ccc(NCC2CCCCC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL195435 70758 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 479 8 2 6 4.8 COc1ccc(NCC2CCCCC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403522 123527 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL363169 123527 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403487 124658 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 444 7 2 6 3.9 CC(C)CNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL364522 124658 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 444 7 2 6 3.9 CC(C)CNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44442056 93858 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@@H]3C[C@@H]4C[C@H]3[C@H](NCc3ccsc3)C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250527 93858 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 393 6 2 5 5.0 COc1ccc2nc(N[C@@H]3C[C@@H]4C[C@H]3[C@H](NCc3ccsc3)C4)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
44402549 71439 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.2 O=C(NCc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL196781 71439 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.2 O=C(NCc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
70681213 73241 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 6 5.5 Cc1nc(N2CCC(N3CCCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017743 73241 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 6 5.5 Cc1nc(N2CCC(N3CCCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
44438745 93412 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 551 11 1 6 4.9 O=C(NC1CCN(Cc2ccc(OCCCN(C3CC3)C3CC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL247891 93412 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 551 11 1 6 4.9 O=C(NC1CCN(Cc2ccc(OCCCN(C3CC3)C3CC3)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
53325165 56410 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 378 8 0 5 3.7 CC(CN(C)C)Oc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642488 56410 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 378 8 0 5 3.7 CC(CN(C)C)Oc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
71716479 87351 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccccc4Cl)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337758 87351 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4ccccc4Cl)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
44397120 66540 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1ccc(CNC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL186417 66540 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 397 6 2 5 2.9 COc1ccc(CNC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
44403472 71370 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 388 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1O 10.1016/j.bmcl.2005.06.089
CHEMBL196591 71370 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 388 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1O 10.1016/j.bmcl.2005.06.089
155522708 170209 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 566 8 1 2 8.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc(-c4ccccc4)cc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
CHEMBL4452982 170209 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 566 8 1 2 8.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc(-c4ccccc4)cc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.bmcl.2019.126741
44442100 154138 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 371 5 2 4 5.5 Clc1cccc2ccc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc12 10.1016/j.bmcl.2007.05.034
CHEMBL399712 154138 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 371 5 2 4 5.5 Clc1cccc2ccc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)nc12 10.1016/j.bmcl.2007.05.034
101007561 155836 0 None - 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 381 6 0 5 2.6 COc1ccccc1N1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL4066435 155836 0 None - 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 381 6 0 5 2.6 COc1ccccc1N1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
101007561 155836 0 None - 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 381 6 0 5 2.6 COc1ccccc1N1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL4066435 155836 0 None - 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 381 6 0 5 2.6 COc1ccccc1N1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
44397099 66760 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 327 5 1 4 3.1 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1cscn1 10.1016/j.bmcl.2005.05.023
CHEMBL187413 66760 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 327 5 1 4 3.1 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1cscn1 10.1016/j.bmcl.2005.05.023
11510669 188700 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 448 7 1 5 4.2 N#Cc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL512180 188700 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 448 7 1 5 4.2 N#Cc1ccc(-n2ccc(CN3CCC(NC(=O)COc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
44394638 123269 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 6 2 6 2.7 Nc1ccc2cccc(OCCNCc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL362309 123269 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 337 6 2 6 2.7 Nc1ccc2cccc(OCCNCc3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
49865869 15986 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 528 8 1 5 7.3 FC(F)(F)Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224080 15986 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 528 8 1 5 7.3 FC(F)(F)Oc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
86695569 130704 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 477 9 1 8 3.0 COc1ccc(COc2ccn(CC(=O)c3ccc(CN4CCC(O)CC4)cc3C)c(=O)c2)nc1 nan
CHEMBL3686767 130704 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 477 9 1 8 3.0 COc1ccc(COc2ccn(CC(=O)c3ccc(CN4CCC(O)CC4)cc3C)c(=O)c2)nc1 nan
91759546 130713 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 1 6 3.2 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
CHEMBL3686776 130713 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 432 8 1 6 3.2 Cc1cc(CN2CC[C@@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccccc2)cc1=O nan
91759563 130742 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 538 9 0 7 3.9 CCN1CCN(Cc2ccc(C(=O)Cn3ccc(OCc4ccc(Br)cn4)cc3=O)c(C)c2)CC1 nan
CHEMBL3686806 130742 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 538 9 0 7 3.9 CCN1CCN(Cc2ccc(C(=O)Cn3ccc(OCc4ccc(Br)cn4)cc3=O)c(C)c2)CC1 nan
22254582 66623 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 3 1 3 3.4 Nc1ccc2cccc(OCC3CCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL186770 66623 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 3 1 3 3.4 Nc1ccc2cccc(OCC3CCCC3)c2n1 10.1016/j.bmcl.2004.07.032
11973801 141424 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(F)c1 10.1021/jm060683e
CHEMBL387309 141424 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 428 5 1 5 3.5 COc1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)c(F)c1 10.1021/jm060683e
10480652 64975 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 488 9 3 5 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL182913 64975 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 488 9 3 5 5.3 CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44394607 123821 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 333 5 3 5 3.6 CC(CNc1ccc2[nH]ncc2c1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL363701 123821 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 333 5 3 5 3.6 CC(CNc1ccc2[nH]ncc2c1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
70685395 73184 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 476 5 2 5 5.4 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017587 73184 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 476 5 2 5 5.4 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)(C4CC4)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
11599681 69986 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 598 10 0 5 7.0 Cc1cc(N(C)CCN(C)C)nc2ccc(N(Cc3ccc(F)c(F)c3)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL194484 69986 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 598 10 0 5 7.0 Cc1cc(N(C)CCN(C)C)nc2ccc(N(Cc3ccc(F)c(F)c3)C(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
54583209 60452 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1ccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)cc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761122 60452 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 486 7 1 4 6.6 CC(=O)Nc1ccc(C2CCN(CCCn3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)cc1 10.1016/j.bmcl.2011.02.099
91759590 130798 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 421 10 1 7 3.1 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
CHEMBL3686860 130798 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 421 10 1 7 3.1 CCNCc1ccc(C(=O)Cn2ccc(OCc3ccc(OC)cn3)cc2=O)c(C)c1 nan
70687538 73212 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 523 10 3 7 3.8 Cc1nc(NCCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017615 73212 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 523 10 3 7 3.8 Cc1nc(NCCCNS(C)(=O)=O)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
89690607 137636 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769582 137636 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccsc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44574357 178120 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)cc2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL468298 178120 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 471 6 1 2 6.4 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)cc2)cc1 10.1016/j.bmcl.2009.04.016
44442097 93563 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1cccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc12 10.1016/j.bmcl.2007.05.034
CHEMBL248694 93563 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1cccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc12 10.1016/j.bmcl.2007.05.034
44394908 66858 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 490 11 2 5 5.2 CCN(CC)CCNC(=O)c1ccc(N(C)C(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL187850 66858 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 490 11 2 5 5.2 CCN(CC)CCNC(=O)c1ccc(N(C)C(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
71720119 87339 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 7 0 5 5.4 COc1cc(N2Cc3ccc(-c4ccc(C(F)(F)F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337746 87339 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 7 0 5 5.4 COc1cc(N2Cc3ccc(-c4ccc(C(F)(F)F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
46899581 16810 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 548 14 4 7 1.8 COC[C@H]1O[C@H](OCCc2ccccc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254141 16810 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 548 14 4 7 1.8 COC[C@H]1O[C@H](OCCc2ccccc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
11620005 81030 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL215958 81030 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 483 9 2 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)/C=C/c2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11591542 79978 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
CHEMBL214535 79978 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 507 10 2 4 6.0 O=C(CCc1ccccc1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc2ccccc2c1 10.1016/j.bmcl.2006.07.040
44402419 71314 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 2 5 5.3 O=C(NCCc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL196390 71314 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 2 5 5.3 O=C(NCCc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2005.03.114
45267385 193256 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 569 8 1 5 5.2 O=C(CN1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
CHEMBL541944 193256 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 569 8 1 5 5.2 O=C(CN1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cn3)c2)CC1)NC(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.067
90666256 108865 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 536 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CCOCC4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219265 108865 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 536 7 1 6 6.0 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4C4CCOCC4)cc3)CC2)c1 10.1039/C1MD00015B
10083869 65228 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL183159 65228 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 258 3 1 3 4.0 CC(CC(C)(C)C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70695916 73208 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 382 6 3 5 3.6 Cc1nc(NCCO)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017611 73208 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 382 6 3 5 3.6 Cc1nc(NCCO)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
11270984 63422 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
CHEMBL180168 63422 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
11270984 63422 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0490890
CHEMBL180168 63422 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cellsInhibition of melanin concentrating hormone receptor 1 from human neuronal IMR-32 cells
ChEMBL 454 9 1 5 4.9 O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0490890
5817261 69968 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 403 5 1 5 4.0 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCOCC4)cc(C)c3c2)cc1 10.1021/jm050103y
CHEMBL194468 69968 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 403 5 1 5 4.0 COc1ccc(/C=C/C(=O)Nc2ccc3nc(N4CCOCC4)cc(C)c3c2)cc1 10.1021/jm050103y
25114065 60441 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 470 7 1 4 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761110 60441 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 470 7 1 4 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(F)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
59135485 91071 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 441 4 1 3 6.2 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403855 91071 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 441 4 1 3 6.2 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(C(F)(F)F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44403483 70018 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 465 6 2 6 2.8 CS(=O)(=O)Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL194521 70018 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 465 6 2 6 2.8 CS(=O)(=O)Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44390456 64555 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 579 9 1 6 6.7 CN(Cc1ccc(Br)cc1OC(F)(F)F)CC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.05.121
CHEMBL182235 64555 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 579 9 1 6 6.7 CN(Cc1ccc(Br)cc1OC(F)(F)F)CC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.05.121
71716480 87352 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cccc(Cl)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337759 87352 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 463 7 0 5 5.0 COc1cc(N2Cc3ccc(-c4cccc(Cl)c4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
11974233 81716 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccccc2F)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL216777 81716 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 398 4 1 4 3.5 O=C(NC1CCN(Cc2ccccc2F)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
49866087 16052 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 1 6 6.2 CCOC(=O)c1ccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)cc1O 10.1016/j.bmcl.2010.07.086
CHEMBL1224387 16052 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 1 6 6.2 CCOC(=O)c1ccc(C2CCN(CCCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)cc1O 10.1016/j.bmcl.2010.07.086
44408020 75066 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 457 8 1 6 4.7 Cc1oc(-c2ccccc2)nc1CC(=O)Nc1ccc2nc(N(C)CCN(C)C)cc(C)c2c1 10.1016/j.bmcl.2005.10.066
CHEMBL204168 75066 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 457 8 1 6 4.7 Cc1oc(-c2ccccc2)nc1CC(=O)Nc1ccc2nc(N(C)CCN(C)C)cc(C)c2c1 10.1016/j.bmcl.2005.10.066
91759588 122005 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 421 9 0 7 3.1 COc1ccc(COc2ccn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 nan
CHEMBL3601302 122005 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 421 9 0 7 3.1 COc1ccc(COc2ccn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 nan
54579974 3177 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
7756 3177 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
CHEMBL1760248 3177 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 472 8 2 5 4.3 COc1ccc(cc1)[C@H]1CN(C[C@@H]1CC(=O)Nc1cccc(c1)Cl)CCC1(O)CCOCC1 10.1016/j.bmcl.2011.02.046
91759588 122005 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 421 9 0 7 3.1 COc1ccc(COc2ccn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601302 122005 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 421 9 0 7 3.1 COc1ccc(COc2ccn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
11525369 140710 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 457 7 3 6 4.5 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2nn(CCN3CC[C@H](O)C3)cc2c1 10.1021/jm0512286
CHEMBL383076 140710 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 457 7 3 6 4.5 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2nn(CCN3CC[C@H](O)C3)cc2c1 10.1021/jm0512286
11974229 82057 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 460 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OC(F)(F)O3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL217707 82057 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 460 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OC(F)(F)O3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
45272837 194197 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 492 6 2 4 4.8 CN(CC1(O)CCCCC1)C(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL558863 194197 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 492 6 2 4 4.8 CN(CC1(O)CCCCC1)C(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
44442065 93862 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250540 93862 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
24952417 91070 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 407 4 1 3 5.8 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403854 91070 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 407 4 1 3 5.8 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44442066 93863 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 371 5 2 4 5.5 Clc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250541 93863 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 371 5 2 4 5.5 Clc1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
71226436 128655 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.4 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCCC34CCOC4)cc2)C1 nan
CHEMBL3670647 128655 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 460 6 0 7 3.4 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCCC34CCOC4)cc2)C1 nan
91759574 130769 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 466 8 1 8 2.5 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686832 130769 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 466 8 1 8 2.5 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(F)cn2)cc1=O nan
11304816 65932 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1021/jm050103y
CHEMBL184717 65932 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1021/jm050103y
44442130 93744 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 519 6 2 6 6.2 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C(=O)N(C)C)c5ccc(Cl)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL249714 93744 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 519 6 2 6 6.2 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C(=O)N(C)C)c5ccc(Cl)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44394684 126760 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL365876 126760 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 319 4 1 4 3.5 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccccc4)C3)c2n1 10.1016/j.bmcl.2004.07.035
10353806 66555 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 5 1 3 3.4 CCCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186481 66555 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 5 1 3 3.4 CCCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44395001 65918 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 490 11 2 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)N(C)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184658 65918 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 490 11 2 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)N(C)c2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44390369 64264 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 629 9 1 7 5.9 CN(C)c1nc(NCC2CCC(CN(C)S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181727 64264 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 629 9 1 7 5.9 CN(C)c1nc(NCC2CCC(CN(C)S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44402433 134682 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL372291 134682 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 441 7 2 5 5.6 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
91759564 130743 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 511 8 0 7 3.6 Cc1cc(CN2CCOCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686807 130743 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 511 8 0 7 3.6 Cc1cc(CN2CCOCC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
91759573 130768 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 410 9 1 7 2.7 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(F)cn3)cc2=O)c(C)c1 nan
CHEMBL3686831 130768 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 410 9 1 7 2.7 CCNCc1ccc(C(=O)Cn2ncc(OCc3ccc(F)cn3)cc2=O)c(C)c1 nan
4219492 71078 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL196091 71078 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 445 5 1 5 4.7 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
11974130 79937 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 434 5 1 6 3.5 CCc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
CHEMBL214377 79937 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 434 5 1 6 3.5 CCc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm060683e
44394944 64529 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 480 10 3 5 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(=O)C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL182161 64529 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 480 10 3 5 4.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(C(=O)C(F)(F)F)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
45267399 194999 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 6 1 4 4.4 O=C(CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1)N1CCCC(CO)C1 10.1016/j.bmcl.2009.05.067
CHEMBL564674 194999 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 6 1 4 4.4 O=C(CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1)N1CCCC(CO)C1 10.1016/j.bmcl.2009.05.067
44405482 71492 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 395 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL196973 71492 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 395 5 2 7 3.3 O=[N+]([O-])c1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44394792 124207 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 405 7 2 5 3.9 Nc1ccc2cccc(OCCCNC(=O)c3cccc(OC(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL364210 124207 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 405 7 2 5 3.9 Nc1ccc2cccc(OCCCNC(=O)c3cccc(OC(F)(F)F)c3)c2n1 10.1016/j.bmcl.2004.07.034
9799244 80158 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214985 80158 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 365 5 2 3 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
22018997 141164 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 485 6 3 4 4.3 CNC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
CHEMBL385661 141164 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 485 6 3 4 4.3 CNC(=O)NC1CCN(c2ccc3cc(NC(=O)CCc4ccc(C(F)(F)F)cc4)ccc3n2)C1 10.1016/j.bmcl.2006.08.006
57397819 69288 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)c(F)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934839 69288 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 532 7 1 5 6.1 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(Cl)c(F)c4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
122184693 121959 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 9 2 6 4.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCC(O)C4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601033 121959 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 432 9 2 6 4.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCC(O)C4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
10433825 121872 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 448 8 1 3 5.6 COc1cc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc1CN1CCCC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600806 121872 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 448 8 1 3 5.6 COc1cc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)ccc1CN1CCCC1 10.1016/j.bmcl.2015.05.077
60130337 121881 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 475 7 1 3 4.6 CC(=O)N1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600814 121881 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 475 7 1 3 4.6 CC(=O)N1CCN(Cc2ccc(CCNC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2)CC1 10.1016/j.bmcl.2015.05.077
9824856 121896 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 446 5 0 3 5.4 Brc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600829 121896 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 446 5 0 3 5.4 Brc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
11504274 121939 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 500 5 1 4 5.6 OC1(C(F)(F)F)CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3601009 121939 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 500 5 1 4 5.6 OC1(C(F)(F)F)CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
10024145 121943 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)nc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601013 121943 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 403 5 0 4 4.7 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)nc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
11328029 76162 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm0512286
CHEMBL206081 76162 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 436 5 1 7 2.9 COc1ccc2c(=O)cc(C(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)oc2c1 10.1021/jm0512286
45273642 194771 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 398 5 1 5 4.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
CHEMBL563096 194771 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 398 5 1 5 4.8 COc1ccc(-c2ccc(C(=O)Nc3ccc4nc(C5CC5)c(C)n4c3)cc2)nc1 10.1016/j.bmcl.2009.06.101
11599973 193218 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 600 8 2 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.067
CHEMBL540930 193218 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 600 8 2 4 6.5 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1 10.1016/j.bmcl.2009.05.067
11599186 73137 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016775 73137 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCC(N3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
56597407 138512 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 434 7 0 7 3.2 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786169 138512 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 434 7 0 7 3.2 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCCC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
127030069 138565 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 434 6 1 7 2.6 CC1(O)CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3786685 138565 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 434 6 1 7 2.6 CC1(O)CCN(Cc2ccc(OC3CN(C(=O)c4nnc(-c5ccccc5)o4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
11648912 79926 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 494 8 3 4 5.5 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)ccc1F 10.1016/j.bmcl.2006.07.040
CHEMBL214322 79926 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 494 8 3 4 5.5 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)ccc1F 10.1016/j.bmcl.2006.07.040
44403467 70183 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 490 7 2 5 6.0 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL194726 70183 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 490 7 2 5 6.0 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(Cl)ccc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
44403518 71405 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL196681 71405 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
11560917 123521 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 424 4 1 5 5.7 O=c1cc(NC2CCN(Cc3ccc4sccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL363139 123521 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 424 4 1 5 5.7 O=c1cc(NC2CCN(Cc3ccc4sccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
10389978 69256 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL193473 69256 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 470 5 2 5 4.9 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
44403765 135324 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL373084 135324 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
23593464 64356 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64356 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
56666755 64376 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 6 1 2 6.5 CCC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818806 64376 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 6 1 2 6.5 CCC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
44408109 75177 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204428 75177 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
127029624 137649 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 6 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769702 137649 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 6 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn12 10.1021/acs.jmedchem.5b01704
45487673 195594 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 440 4 1 4 4.6 OC(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
CHEMBL568572 195594 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 440 4 1 4 4.6 OC(c1ccc(CN2CCC3(CC2)OCc2cc(F)ncc23)cc1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.07.132
10344176 66834 4 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL187756 66834 4 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 458 5 1 5 4.6 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
21940008 64379 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818809 64379 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 408 5 1 2 6.0 O=C(Nc1ccc2c(c1)CCC(CN1CCCC1)=C2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2011.07.038
57396294 67731 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914637 67731 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 502 8 0 4 4.9 CCS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44418003 82042 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL217614 82042 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)ccc2n1 10.1016/j.bmcl.2006.08.008
21108056 67723 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914629 67723 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.1 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
18435980 74520 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 448 4 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm201596h
CHEMBL2031726 74520 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 448 4 1 3 5.9 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)N1CCC(c2ccc(Cl)cc2)CC1 10.1021/jm201596h
11596311 56407 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 392 10 0 5 4.1 CCN(CC)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642485 56407 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 392 10 0 5 4.1 CCN(CC)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
57401509 67730 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914636 67730 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44143496 191479 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 444 6 2 3 5.9 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
CHEMBL520296 191479 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 444 6 2 3 5.9 CN(c1nc2ccc(NC(=O)CCc3ccc(C(F)(F)F)cc3)cc2[nH]1)C1CCCCC1 10.1016/j.bmcl.2009.04.147
53318593 56401 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 458 8 0 5 4.9 O=c1cc(OCc2ccc(C(F)(F)F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642477 56401 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 458 8 0 5 4.9 O=c1cc(OCc2ccc(C(F)(F)F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
57522704 76009 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 7 1 4 5.4 Cc1c(NC(=O)c2ccc(OCC(C)C)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059411 76009 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 417 7 1 4 5.4 Cc1c(NC(=O)c2ccc(OCC(C)C)cc2)ccc2cc(CN3CCCC3)cnc12 10.1021/jm300167z
57522816 76015 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.6 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3C)cnc12 10.1021/jm300167z
CHEMBL2059417 76015 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.6 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3C)cnc12 10.1021/jm300167z
155516949 169574 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 540 6 1 6 3.6 CS(=O)(=O)N1CCN(CN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL4444299 169574 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 540 6 1 6 3.6 CS(=O)(=O)N1CCN(CN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
71816518 137743 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770706 137743 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 415 3 0 5 5.7 Cc1c(C2CC2)nc2ccc(-n3ccc4oc(-c5ccc(Cl)cc5)cc4c3=O)cn12 10.1021/acs.jmedchem.5b01704
56680348 64375 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 5 1 2 6.1 CC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818805 64375 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 5 1 2 6.1 CC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
23120575 194190 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL558826 194190 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ncc(-c4ccc(F)cc4)cn3)cn12 10.1016/j.bmcl.2009.06.101
45487653 197319 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585664 197319 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1R expressed in CHO cellsDisplacement of [125I]MCH from human MCH1R expressed in CHO cells
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
53318594 56414 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 391 10 1 5 4.2 CCN(CC)CCNc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642492 56414 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 391 10 1 5 4.2 CCN(CC)CCNc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
44390768 64128 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 434 6 2 7 3.8 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc([N+](=O)[O-])c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181383 64128 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 434 6 2 7 3.8 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc([N+](=O)[O-])c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44403765 135324 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
CHEMBL373084 135324 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 446 8 2 5 4.5 CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1 10.1021/jm050103y
9824428 65910 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 438 9 3 4 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
CHEMBL184634 65910 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 438 9 3 4 4.3 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.077
44394764 122640 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 7 2 4 4.1 CC(C)c1ccc(C(=O)NCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
CHEMBL361262 122640 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 7 2 4 4.1 CC(C)c1ccc(C(=O)NCCCOc2cccc3ccc(N)nc23)cc1 10.1016/j.bmcl.2004.07.034
22254581 65878 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 448 7 1 4 8.0 CC(CC(C)(C)C)Oc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL184520 65878 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 448 7 1 4 8.0 CC(CC(C)(C)C)Oc1cccc2ccc(NCc3ccc(-c4ccccc4Cl)o3)nc12 10.1016/j.bmcl.2004.07.032
44417856 80413 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)c(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215241 80413 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 399 5 2 3 5.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(Cl)c(Cl)c3)ccc2n1 10.1016/j.bmcl.2006.08.008
60169098 87320 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 475 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337727 87320 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 475 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
60169182 87322 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4F)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337729 87322 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 497 8 0 6 5.2 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4F)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
25116309 60444 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 494 8 1 4 7.1 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C(C)C)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761113 60444 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 494 8 1 4 7.1 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(C(C)C)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
11975438 79807 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 380 4 1 4 3.3 O=C(NC1CCN(Cc2ccccc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL213761 79807 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 380 4 1 4 3.3 O=C(NC1CCN(Cc2ccccc2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
44397128 123570 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 428 6 1 4 4.4 O=C(Cc1ccc(-c2ccccc2)cc1)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
CHEMBL363336 123570 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 428 6 1 4 4.4 O=C(Cc1ccc(-c2ccccc2)cc1)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.05.023
44403501 69292 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 458 7 2 5 5.0 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCc1ccco1 10.1016/j.bmcl.2005.06.089
CHEMBL193489 69292 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 458 7 2 5 5.0 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cc(Cl)cnc1NCc1ccco1 10.1016/j.bmcl.2005.06.089
44403524 71106 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 488 10 2 7 4.1 CC(C)OCCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196223 71106 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 488 10 2 7 4.1 CC(C)OCCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
11611530 134269 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 421 3 1 5 4.8 Cn1ccc2ccc(CN3CCC(/N=c4\cc(O)oc5ccc(Cl)cc45)CC3)cc21 10.1021/jm050598r
CHEMBL371877 134269 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 421 3 1 5 4.8 Cn1ccc2ccc(CN3CCC(/N=c4\cc(O)oc5ccc(Cl)cc45)CC3)cc21 10.1021/jm050598r
89691216 138858 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 417 5 0 5 5.1 Cn1c(C2CCCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793395 138858 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 417 5 0 5 5.1 Cn1c(C2CCCC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44401671 69908 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 7 1 7 4.9 CN(C)c1nc(NCC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL194173 69908 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 587 7 1 7 4.9 CN(C)c1nc(NCC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
10466478 123497 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 232 4 1 4 2.2 COCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL363011 123497 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 232 4 1 4 2.2 COCC(C)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
70695918 73213 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 499 9 3 6 4.4 Cc1nc(NCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017616 73213 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 499 9 3 6 4.4 Cc1nc(NCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
57390252 67796 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 409 6 0 2 6.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCCCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914856 67796 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 409 6 0 2 6.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCCCC2 10.1016/j.bmc.2011.09.007
45273659 194149 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
CHEMBL558326 194149 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 387 4 1 5 4.4 Cc1c(C2CC2)nc2ccc(NC(=O)c3ccc(-c4ccc(F)nc4)nc3)cn12 10.1016/j.bmcl.2009.06.101
44442124 154342 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 6 2 5 6.3 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C)c5ccc(Br)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL400799 154342 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 506 6 2 5 6.3 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cn(C)c5ccc(Br)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
11583925 165207 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL424720 165207 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 485 10 2 4 5.5 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)CCc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11563153 136030 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL373887 136030 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 564 10 3 5 7.4 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmcl.2006.07.040
44402414 71047 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 471 7 3 6 4.9 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCC(O)CC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL195896 71047 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 471 7 3 6 4.9 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCC(O)CC2)c1 10.1016/j.bmcl.2005.03.114
10443853 65869 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.2 CC(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL184476 65869 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 230 4 1 3 3.2 CC(C)CCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
45270273 193904 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 524 6 2 5 4.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.066
CHEMBL555349 193904 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 524 6 2 5 4.3 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NS(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2009.05.066
70689594 73185 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 472 5 2 6 4.5 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017588 73185 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 472 5 2 6 4.5 Cc1nc(N2CCC(O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
127025395 137740 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 431 3 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc4c(c3=O)CCC(c3ccc(Cl)cc3)O4)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770680 137740 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 431 3 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc4c(c3=O)CCC(c3ccc(Cl)cc3)O4)cn12 10.1021/acs.jmedchem.5b01704
57399742 67736 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 468 6 1 4 4.2 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914651 67736 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 468 6 1 4 4.2 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
9999058 93857 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.7 COc1ccc2nc(N[C@H]3CC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250526 93857 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.7 COc1ccc2nc(N[C@H]3CC[C@H](NCc4ccsc4)C3)cc(C)c2c1 10.1016/j.bmcl.2007.05.034
70693794 73196 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 496 5 2 5 5.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017599 73196 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 496 5 2 5 5.6 Cc1nc(N2CCC(O)(C3CC3)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3Cl)cc12 10.1016/j.bmcl.2012.03.049
70685398 73214 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 10 3 6 4.8 Cc1nc(NCCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017617 73214 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 513 10 3 6 4.8 Cc1nc(NCCCNC(=O)C2CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
45273783 194183 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 540 6 2 4 5.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCC(O)(Cc2ccccc2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL558726 194183 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 540 6 2 4 5.2 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCC(O)(Cc2ccccc2)CC1 10.1016/j.bmcl.2009.05.066
45273790 194238 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.3 O=C(NC[C@H]1CCCC[C@H]1O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL559329 194238 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 478 6 3 4 4.3 O=C(NC[C@H]1CCCC[C@H]1O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
59135479 91066 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 393 3 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403850 91066 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 393 3 1 3 5.5 Cc1ccc2c(c1)nc(C)n2[C@H]1CC[C@@H](NC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44407967 74128 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL202854 74128 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 506 7 1 4 6.5 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)cc12 10.1016/j.bmcl.2005.10.066
10389430 125417 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 458 5 1 5 4.3 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL364863 125417 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 458 5 1 5 4.3 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc12 10.1016/j.bmcl.2004.05.051
59691584 121916 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 444 6 0 2 6.7 CN(C(=O)/C=C/c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600976 121916 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 444 6 0 2 6.7 CN(C(=O)/C=C/c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
70687479 73148 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3cccc(F)c3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016785 73148 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 570 7 2 7 5.5 Cc1nc(N2CCC(O)(c3cccc(F)c3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44562481 185419 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 477 8 1 4 5.8 FC(F)(F)c1ccc(-n2ccc(CN3CCC(NCCOc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL487041 185419 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 477 8 1 4 5.8 FC(F)(F)c1ccc(-n2ccc(CN3CCC(NCCOc4cccc(Cl)c4)CC3)c2)cc1 10.1016/j.bmcl.2008.07.079
70695860 73054 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 519 7 3 8 2.7 Cc1nc(N2CCC(O)(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016580 73054 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 519 7 3 8 2.7 Cc1nc(N2CCC(O)(C(N)=O)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
56683679 64377 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 474 6 1 3 6.7 CCOC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818807 64377 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 474 6 1 3 6.7 CCOC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
44438742 93379 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 496 6 1 5 4.4 O=C(NC1CCN(Cc2ccc(OCC(F)(F)F)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
CHEMBL247689 93379 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 496 6 1 5 4.4 O=C(NC1CCN(Cc2ccc(OCC(F)(F)F)c(F)c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.068
11374857 79794 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 472 6 1 7 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(OC(F)F)cc2o1 10.1021/jm060683e
CHEMBL213715 79794 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 472 6 1 7 3.5 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccc(OC(F)F)cc2o1 10.1021/jm060683e
44394921 65893 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 431 9 2 4 4.3 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL184579 65893 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 431 9 2 4 4.3 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
44394961 66884 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 548 10 2 5 5.2 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2004.07.077
CHEMBL187953 66884 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 548 10 2 5 5.2 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCN1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2004.07.077
10038053 65762 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.032
CHEMBL183932 65762 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 2 1 3 3.8 CC1CCCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.032
53321222 56402 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 466 9 0 5 5.6 O=c1cc(OCc2ccc(-c3ccccc3)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642478 56402 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 466 9 0 5 5.6 O=c1cc(OCc2ccc(-c3ccccc3)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
49865975 16024 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 486 8 2 6 4.7 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224228 16024 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 486 8 2 6 4.7 CC(=O)Nc1cccc(N2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
10456755 70739 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195351 70739 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 456 5 2 5 4.5 Cc1cc(N2CCNCC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
117798675 138817 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 393 5 0 5 4.7 CCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
CHEMBL3793016 138817 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 393 5 0 5 4.7 CCn1nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc2c1C 10.1016/j.bmc.2016.04.013
71660917 138831 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3793118 138831 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
11464405 80070 18 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1021/jm060683e
CHEMBL214731 80070 18 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 424 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1021/jm060683e
44250211 194538 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 549 9 1 5 6.2 Cc1nccn1CC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.067
CHEMBL561584 194538 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 549 9 1 5 6.2 Cc1nccn1CC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.067
127029632 137781 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3cccc(OCc4ccc(Cl)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771133 137781 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3cccc(OCc4ccc(Cl)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
53317524 56405 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 422 9 0 5 4.1 O=c1cc(OCCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642483 56405 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 422 9 0 5 4.1 O=c1cc(OCCc2ccc(F)cc2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
17484866 66491 2 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 320 5 1 2 3.6 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2005.05.023
CHEMBL186159 66491 2 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 320 5 1 2 3.6 O=C(NC1CCN(C/C=C/c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2005.05.023
90666261 108871 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 571 7 1 6 6.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
CHEMBL3219270 108871 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 571 7 1 6 6.6 CC(=O)Nc1cccc(C2CCN(Cc3ccc(C(=O)c4nc5ccccc5n4-c4ccc(F)cc4)cc3C#N)CC2)c1 10.1039/C1MD00015B
70681215 73250 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 540 6 2 6 4.5 Cc1nc(N2CCC(N3CCNC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017752 73250 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 540 6 2 6 4.5 Cc1nc(N2CCC(N3CCNC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11975326 80082 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 406 4 1 6 2.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccccc2o1 10.1021/jm060683e
CHEMBL214767 80082 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 406 4 1 6 2.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2ccccc2o1 10.1021/jm060683e
45270319 193541 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 555 8 2 5 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(CN1CCOCC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL550816 193541 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 555 8 2 5 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(CN1CCOCC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
44562565 173489 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)on2)cc1 10.1016/j.bmcl.2008.07.079
CHEMBL454424 173489 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 469 5 0 4 6.7 Fc1ccc(-c2cc(C3CCN(Cc4ccn(-c5ccc(C(F)(F)F)cc5)c4)CC3)on2)cc1 10.1016/j.bmcl.2008.07.079
45272539 194227 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 4 5.1 O=C(C1CCCCN1C(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1 10.1016/j.bmcl.2009.05.067
CHEMBL559237 194227 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 4 5.1 O=C(C1CCCCN1C(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC1 10.1016/j.bmcl.2009.05.067
44394587 123534 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 283 6 2 5 2.6 Nc1ccc2cccc(OCCNCc3ccoc3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL363220 123534 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 283 6 2 5 2.6 Nc1ccc2cccc(OCCNCc3ccoc3)c2n1 10.1016/j.bmcl.2004.07.034
22421739 66765 6 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 418 6 1 5 4.0 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4cccc(C)c4)ccc3n2)CC1 10.1021/jm040762v
CHEMBL187430 66765 6 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 418 6 1 5 4.0 CCN1CCN(c2cc(C)c3cc(NC(=O)COc4cccc(C)c4)ccc3n2)CC1 10.1021/jm040762v
86695565 130694 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 435 8 0 6 3.7 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686757 130694 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 435 8 0 6 3.7 Cc1cc(CN2CCCC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
91759584 130773 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686836 130773 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 468 8 1 8 2.6 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
91759578 130799 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 0 8 2.8 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686861 130799 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 481 8 0 8 2.8 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
45270850 194969 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 486 7 2 4 4.7 CC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
CHEMBL564413 194969 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 486 7 2 4 4.7 CC(NC(=O)CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccc(=O)[nH]c1 10.1016/j.bmcl.2009.05.067
59135474 91079 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403863 91079 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 435 5 2 4 5.2 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NCC2Cc3ccc(F)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
70695913 73187 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 436 4 2 5 4.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017590 73187 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 436 4 2 5 4.6 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
44401368 69901 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 489 14 2 6 5.2 CCCCCCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
CHEMBL194122 69901 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 489 14 2 6 5.2 CCCCCCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
49866086 16051 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 499 7 2 5 4.7 CC(=O)Nc1cccc(C2CCN(CCNC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224386 16051 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 499 7 2 5 4.7 CC(=O)Nc1cccc(C2CCN(CCNC(=O)c3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
70685410 73249 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 569 6 1 7 5.7 Cc1nc(N2CCC(N3CC(C)(C)OC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017751 73249 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 569 6 1 7 5.7 Cc1nc(N2CCC(N3CC(C)(C)OC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
60130349 121868 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 364 6 2 2 4.4 NCc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600802 121868 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 364 6 2 2 4.4 NCc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
44410904 171880 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL448110 171880 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44442063 93946 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 337 5 2 4 4.8 c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250927 93946 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 337 5 2 4 4.8 c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
49865678 15869 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 497 9 2 6 5.7 COc1ccc(-n2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2010.07.086
CHEMBL1223767 15869 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 497 9 2 6 5.7 COc1ccc(-n2c(NCCCN3CCC(c4cccc(NC(C)=O)c4)CC3)nc3ccccc32)cc1 10.1016/j.bmcl.2010.07.086
44403478 165749 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 401 5 2 5 3.5 CNc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL427187 165749 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 401 5 2 5 3.5 CNc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44388096 63165 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 516 8 2 3 6.5 Cc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2019.126741
CHEMBL180009 63165 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 516 8 2 3 6.5 Cc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2019.126741
70685408 73243 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 6 5.5 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017745 73243 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 6 5.5 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2012.03.049
127028868 138799 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nn2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc12 10.1016/j.bmc.2016.04.013
CHEMBL3792826 138799 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nn2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc12 10.1016/j.bmc.2016.04.013
70691648 73089 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 439 6 1 6 3.8 CCN1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
CHEMBL2016699 73089 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 439 6 1 6 3.8 CCN1CCN(c2nc(C)c3cc(NC(=O)COc4ccc(Cl)cc4)ccc3n2)CC1 10.1016/j.bmcl.2012.03.050
44407989 75015 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 388 7 1 4 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccccc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203858 75015 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 388 7 1 4 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccccc3)cc12 10.1016/j.bmcl.2005.10.066
44405619 72144 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccncc1 10.1016/j.bmcl.2005.08.049
CHEMBL199025 72144 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccncc1 10.1016/j.bmcl.2005.08.049
44394725 65805 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 365 6 2 6 2.7 Nc1ccc2cccc(OCCCNC(=O)c3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL184191 65805 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 365 6 2 6 2.7 Nc1ccc2cccc(OCCCNC(=O)c3ccc4c(c3)OCO4)c2n1 10.1016/j.bmcl.2004.07.034
11719291 81472 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 447 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3ccc(=O)[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216482 81472 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 447 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3ccc(=O)[nH]c3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
11711452 81610 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 420 4 1 5 4.1 O=C(NC1CCN(Cc2ccc3occc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL216554 81610 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 420 4 1 5 4.1 O=C(NC1CCN(Cc2ccc3occc3c2)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1016/j.bmcl.2006.11.065
57394274 69284 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(F)cc4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934834 69284 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 516 7 1 5 5.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(F)cc4F)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
25116307 60439 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1cccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761108 60439 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1cccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)c1 10.1016/j.bmcl.2011.02.099
16742746 121920 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 416 9 1 5 5.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600980 121920 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 416 9 1 5 5.2 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
10274635 68502 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 435 3 1 3 3.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3=O)C[C@@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922268 68502 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 435 3 1 3 3.6 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCN3CCOCC3=O)C[C@@H]21 10.1016/j.bmcl.2011.09.110
122184832 121997 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 362 8 0 4 3.7 CN(C)Cc1ccc(CCn2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601294 121997 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 362 8 0 4 3.7 CN(C)Cc1ccc(CCn2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmcl.2015.05.065
9978490 121895 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600828 121895 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
44410838 76693 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 432 4 1 5 4.8 Cn1c(=O)nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL207296 76693 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 432 4 1 5 4.8 Cn1c(=O)nc(NC2CCN(Cc3ccc4ccccc4c3)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
53324076 56400 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 420 9 0 6 3.9 COc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642476 56400 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 420 9 0 6 3.9 COc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1 10.1016/j.bmc.2010.12.002
44442064 154258 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 351 5 2 4 5.1 Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL400298 154258 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 351 5 2 4 5.1 Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
45487384 195156 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)nc1 10.1016/j.bmcl.2009.07.023
CHEMBL565833 195156 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membraneDisplacement of [125I]MCH from human recombinant MCH1R expressed on CHOK1 cell membrane
ChEMBL 395 10 1 5 3.7 CCCNCc1ccc(CCn2ccc(OCc3ccc(F)cc3)cc2=O)nc1 10.1016/j.bmcl.2009.07.023
70681113 73094 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016704 73094 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 545 7 1 8 4.2 Cc1nc(N2CCN(C3CCOCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
70691653 73119 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 510 7 3 6 4.3 Cc1nc(N2CCC(NC(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016730 73119 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 510 7 3 6 4.3 Cc1nc(N2CCC(NC(=O)NC(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
71226400 128648 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3670640 128648 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 446 6 0 7 2.9 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCOC4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
71227163 138525 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCCO4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3786346 138525 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CC4(CCCO4)C3)cc2)C1 10.1021/acs.jmedchem.5b01654
71226277 138576 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCOC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786841 138576 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 0 8 2.9 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CC6(CCOC6)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
11236807 81140 0 None -1 3 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81140 0 None -1 3 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
11641948 79916 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL214280 79916 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 506 8 3 4 6.2 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2Cl)cc1C 10.1016/j.bmcl.2006.07.040
11583747 81069 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1cccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)c1 10.1016/j.bmcl.2006.07.040
CHEMBL216010 81069 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 476 8 3 4 5.4 Cc1cccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2cccc(F)c2)c1 10.1016/j.bmcl.2006.07.040
44403524 71106 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 488 10 2 7 4.1 CC(C)OCCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196223 71106 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 488 10 2 7 4.1 CC(C)OCCCNc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
11603897 123796 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4[nH]ccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL363583 123796 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 407 4 2 4 5.0 O=c1cc(NC2CCN(Cc3ccc4[nH]ccc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
11548234 70837 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL195635 70837 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 528 7 1 6 5.5 Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
45271907 193376 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 437 3 1 3 6.6 CC(C)(C)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL549512 193376 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 437 3 1 3 6.6 CC(C)(C)c1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
44408028 140360 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 518 11 2 6 6.0 Cc1cc(NCCN(C(C)C)C(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL382161 140360 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assayDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO cell by WC assay
ChEMBL 518 11 2 6 6.0 Cc1cc(NCCN(C(C)C)C(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
57391028 67728 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914634 67728 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 494 9 0 3 6.3 CCCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57399740 67727 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914633 67727 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 478 7 0 3 5.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)C1CC1)CC2 10.1016/j.bmc.2011.09.007
21062998 64369 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818798 64369 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 506 8 1 2 7.8 CN(CCc1ccccc1)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
89690574 137784 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771182 137784 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
57392824 67726 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914632 67726 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 480 8 0 3 5.9 CCCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11532924 137841 0 None 47 3 Rat 8.1 pIC50 = 8.1 Binding
Activity at chimeric rat/human MCH1R by accumulation of GTPgammaSActivity at chimeric rat/human MCH1R by accumulation of GTPgammaS
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL377241 137841 0 None 47 3 Rat 8.1 pIC50 = 8.1 Binding
Activity at chimeric rat/human MCH1R by accumulation of GTPgammaSActivity at chimeric rat/human MCH1R by accumulation of GTPgammaS
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
89690574 137784 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771182 137784 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 411 5 0 6 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
53317307 56403 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 440 8 0 5 5.0 O=c1cc(OCc2ccc3ccccc3c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642479 56403 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 440 8 0 5 5.0 O=c1cc(OCc2ccc3ccccc3c2)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
127029623 137794 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 379 5 1 5 3.9 Cc1nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3771335 137794 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 379 5 1 5 3.9 Cc1nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn2c1C 10.1021/acs.jmedchem.5b01704
57522701 76028 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 5.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059514 76028 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 5.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)(C)N3CCCC3)cnc12 10.1021/jm300167z
71226895 128653 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCCC34COC4)cc2)C1 nan
CHEMBL3670645 128653 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.Activation Assay: Melanin Concentrating Hormone Receptor 1 (MCHR1) is a G-protein coupled receptor that interacts with heterotrimeric G proteins containing a Gαi/o subunit. Binding of MCH to MCHR1 results in the exchange of GDP for GTP on the Gαi/o proteins associated with the activated receptor. This activation can be quantified by measuring the amount of a GTP analog, GTPγ35S, bound to the membrane-associated receptor. GTPγ35S is not hydrolyzed by the intrinsic GTPase activity of a G-protein but instead forms a stable complex. Inhibition of MCH binding by a competing ligand may thus be assessed by a decrease in the amount of GTPγ35S bound to membranes in the presence of such a competing ligand.
ChEMBL 446 6 0 7 3.0 O=C(c1nnc(-c2ccccc2)o1)N1CC(Oc2ccc(CN3CCCC34COC4)cc2)C1 nan
91759552 122004 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 409 8 0 6 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3601301 122004 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 409 8 0 6 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
91759551 130720 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 451 8 1 7 2.7 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686783 130720 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 451 8 1 7 2.7 Cc1cc(CN2CC[C@H](O)C2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
44394909 66684 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 504 10 3 6 4.6 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCOCC1 10.1016/j.bmcl.2004.07.077
CHEMBL187093 66684 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 504 10 3 6 4.6 COc1cc(NC(=O)Nc2cccc(Oc3ccccc3)c2)ccc1C(=O)NCCCN1CCOCC1 10.1016/j.bmcl.2004.07.077
44405519 72011 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 5 4.1 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL198588 72011 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 398 4 2 5 4.1 Clc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
44394605 66668 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 271 4 1 4 2.7 CC(CN1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL187003 66668 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 271 4 1 4 2.7 CC(CN1CCCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394639 66358 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL185558 66358 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
10361342 122396 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL360620 122396 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 363 4 1 6 3.2 Nc1ccc2cccc(O[C@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
11188955 80042 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 406 6 2 5 4.4 CC(C)Nc1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
CHEMBL214678 80042 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 406 6 2 5 4.4 CC(C)Nc1nc2ccc(NC(=O)COc3ccc(C(F)(F)F)cc3)cc2n1C 10.1016/j.bmcl.2006.11.092
60168816 87330 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 8 0 5 4.3 COc1cc(N2Cc3ccc(Cc4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337737 87330 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 8 0 5 4.3 COc1cc(N2Cc3ccc(Cc4ccccc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
91759552 122004 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 409 8 0 6 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601301 122004 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 409 8 0 6 3.2 Cc1cc(CN(C)C)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O 10.1016/j.bmcl.2015.05.065
56666756 64378 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 473 6 2 2 6.3 CCNC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818808 64378 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 473 6 2 2 6.3 CCNC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
117798671 138813 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793001 138813 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
57401508 67729 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 514 7 0 3 6.4 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)c1ccccc1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914635 67729 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 514 7 0 3 6.4 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)c1ccccc1)CC2 10.1016/j.bmc.2011.09.007
44403516 69936 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2ncc[nH]2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL194342 69936 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 463 8 3 7 3.2 COc1ccc(NCc2ncc[nH]2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403480 70191 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 442 6 2 6 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
CHEMBL194759 70191 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 442 6 2 6 3.8 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NC1CCC1 10.1016/j.bmcl.2005.06.089
44403479 97743 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 428 6 2 5 3.9 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL274254 97743 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 428 6 2 5 3.9 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2005.06.089
44403538 135575 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 470 8 3 6 4.0 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ncccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL373235 135575 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 470 8 3 6 4.0 COc1ccc(NCc2c[nH]cn2)c(C(=O)NC2CCN(Cc3ccc4ncccc4c3)CC2)c1 10.1016/j.bmcl.2005.06.089
44403479 97743 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 428 6 2 5 3.9 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL274254 97743 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 428 6 2 5 3.9 CC(C)Nc1ncc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)CCO3)CC1 10.1016/j.bmcl.2005.06.089
44403507 126240 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1ncc[nH]1 10.1016/j.bmcl.2005.06.089
CHEMBL365360 126240 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1ncc[nH]1 10.1016/j.bmcl.2005.06.089
44403511 135637 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 475 8 2 8 3.2 COc1ccc(NCc2cncnc2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL373266 135637 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 475 8 2 8 3.2 COc1ccc(NCc2cncnc2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
122184567 121888 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 10 0 4 5.6 CCN(CC)CCOc1ccc(/C=C\c2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600821 121888 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 10 0 4 5.6 CCN(CC)CCOc1ccc(/C=C\c2ccc(-c3ccc(OC)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
11409615 141221 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 509 8 2 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
CHEMBL386039 141221 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 509 8 2 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2019.126741
91759576 130771 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 0 8 3.2 CCN1CCN(Cc2ccc(C(=O)Cn3ncc(OCc4ccc(Cl)cn4)cc3=O)c(C)c2)CC1 nan
CHEMBL3686834 130771 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 495 9 0 8 3.2 CCN1CCN(Cc2ccc(C(=O)Cn3ncc(OCc4ccc(Cl)cn4)cc3=O)c(C)c2)CC1 nan
11178792 94076 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 465 6 2 6 5.7 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c4ccc4cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251702 94076 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 465 6 2 6 5.7 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5c4ccc4cccnc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
45268247 194910 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 4 5.0 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.067
CHEMBL564032 194910 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 4 5.0 O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CCCC(C(=O)N2CCCC2)C1 10.1016/j.bmcl.2009.05.067
44407629 168078 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL436320 168078 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 6 2 6 4.3 Cc1cc(N2CCCNCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
11304816 65932 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2004.05.051
CHEMBL184717 65932 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Tested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1RTested for MCH-1 induced [Ca2+] release from CHO cells transfected with human MCH-1R
ChEMBL 424 5 1 5 4.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2004.05.051
44394998 64827 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Cl)c(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL182466 64827 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.7 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Cl)c(Cl)c2)cc1OC 10.1016/j.bmcl.2004.07.077
11676200 178626 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 423 7 1 4 4.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472554 178626 1 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 423 7 1 4 4.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2008.07.079
71718911 87355 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1cc(N2Cc3ccc(-c4ccccc4OC)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337762 87355 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 459 8 0 6 4.4 COc1cc(N2Cc3ccc(-c4ccccc4OC)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
91759565 130746 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 524 8 0 7 3.5 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
CHEMBL3686810 130746 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 524 8 0 7 3.5 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Br)cn2)cc1=O nan
89690124 137758 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 439 5 0 5 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770865 137758 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 439 5 0 5 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89691143 138772 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792529 138772 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 405 5 0 5 4.8 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44395019 65890 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL184560 65890 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 476 11 3 5 5.2 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
60168914 87331 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 4.6 COc1cc(N2Cc3ccc(Cc4ccccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337738 87331 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 457 8 0 5 4.6 COc1cc(N2Cc3ccc(Cc4ccccc4C)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
22254540 66703 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.1 Nc1ccc2cccc(OCCC(F)(F)F)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL187165 66703 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.1 Nc1ccc2cccc(OCCC(F)(F)F)c2n1 10.1016/j.bmcl.2004.07.032
44407870 75546 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204968 75546 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 474 9 1 5 5.0 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)CCc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
89691144 138902 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793989 138902 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 406 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11974230 165448 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 438 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
CHEMBL425448 165448 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 438 4 1 6 3.1 O=C(NC1CCN(Cc2ccc3c(c2)OCCO3)CC1)c1cc(=O)c2ccc(F)cc2o1 10.1021/jm060683e
18436129 74512 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 408 5 1 4 5.1 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccccc2)nc1 10.1021/jm201596h
CHEMBL2031718 74512 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation countingDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 408 5 1 4 5.1 O=C(Nc1ccc2cc(CN3CCCC3)cnc2c1)c1ccc(-c2ccccc2)nc1 10.1021/jm201596h
44394596 65858 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 377 3 1 6 2.8 Nc1ccc2cccc(O[C@H]3CCN(C(=O)c4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL184437 65858 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 377 3 1 6 2.8 Nc1ccc2cccc(O[C@H]3CCN(C(=O)c4ccc5c(c4)OCO5)C3)c2n1 10.1016/j.bmcl.2004.07.035
22421743 66474 4 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 432 7 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)CCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm040762v
CHEMBL186077 66474 4 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 432 7 1 5 4.3 CCN1CCN(c2cc(C)c3cc(NC(=O)CCc4ccc(OC)cc4)ccc3n2)CC1 10.1021/jm040762v
70695852 73105 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 515 6 1 6 4.6 Cc1nc(N2CCN(C(=O)c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016716 73105 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 515 6 1 6 4.6 Cc1nc(N2CCN(C(=O)c3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
11546687 81129 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)ccc2o1 10.1021/jm060683e
CHEMBL216133 81129 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 440 4 1 6 3.6 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(Cl)ccc2o1 10.1021/jm060683e
25115852 60431 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 480 9 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761100 60431 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 480 9 1 4 6.7 CC(=O)Nc1cccc(C2CCN(CCCCCn3c(-c4ccccc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
70681214 73244 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 489 5 1 5 4.8 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017746 73244 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 489 5 1 5 4.8 Cc1nc(N2CCC(N3CCCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
117816748 138880 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793841 138880 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4cc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
11635332 193393 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 550 8 2 5 5.7 Cc1nccn1CC(NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
CHEMBL549595 193393 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 550 8 2 5 5.7 Cc1nccn1CC(NC(=O)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)c1ccccc1 10.1016/j.bmcl.2009.05.066
25116306 60438 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1ccccc1-c1nc2ccccc2n1CCCN1CCC(c2cccc(NC(C)=O)c2)CC1 10.1016/j.bmcl.2011.02.099
CHEMBL1761107 60438 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1ccccc1-c1nc2ccccc2n1CCCN1CCC(c2cccc(NC(C)=O)c2)CC1 10.1016/j.bmcl.2011.02.099
11975436 78668 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)c(Cl)ccc2o1 10.1021/jm060683e
CHEMBL2113245 78668 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 474 4 1 6 4.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2c(Cl)c(Cl)ccc2o1 10.1021/jm060683e
11632909 132907 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ncoc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL370608 132907 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 409 4 1 6 4.7 O=c1cc(NC2CCN(Cc3ccc4ncoc4c3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
44417898 82149 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 506 5 0 4 4.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2019.126741
CHEMBL217860 82149 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 506 5 0 4 4.4 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCc2cc(CN3CCS(=O)(=O)CC3)ccc2C1 10.1016/j.bmcl.2019.126741
10202381 68501 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 421 3 1 3 4.1 C[C@@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@@H]2CCN(CCN3CCOCC3)C[C@H]21 10.1016/j.bmcl.2011.09.110
CHEMBL1922267 68501 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
ChEMBL 421 3 1 3 4.1 C[C@@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@@H]2CCN(CCN3CCOCC3)C[C@H]21 10.1016/j.bmcl.2011.09.110
44417890 165412 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3c2ccc2c3OCO2)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL425257 165412 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3c2ccc2c3OCO2)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
21939767 64352 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818777 64352 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
89691019 138850 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793343 138850 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 377 5 0 6 4.2 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
117816753 138794 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3792764 138794 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1c2cc(-n3ccc(OCc4ccc(F)cc4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117798780 138848 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4nc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793312 138848 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 420 4 0 7 4.1 Cc1c2cc(-n3ccc(OCc4nc(C(F)(F)F)cs4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
59135492 91081 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 418 4 1 4 5.4 Cc1nc2cc(C#N)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403865 91081 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 418 4 1 4 5.4 Cc1nc2cc(C#N)ccc2n1[C@H]1CC[C@@H](NCC2Cc3ccc(Cl)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
16721015 79996 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
CHEMBL214585 79996 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 450 3 1 6 3.5 O=C(NC1CCN(C2CCc3cc4c(cc32)OCO4)CC1)c1cc(=O)c2cc(F)ccc2o1 10.1016/j.bmcl.2006.11.061
54583954 60296 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
CHEMBL1760237 60296 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 522 11 1 5 5.4 COc1ccc([C@H]2CN(CCc3ccc(OC)c(OC)c3)C[C@@H]2CCNC(=O)c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.02.046
10386529 121945 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 404 5 0 5 4.1 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)nn3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601015 121945 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 404 5 0 5 4.1 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)nn3)nc2)cc1 10.1016/j.bmcl.2015.05.077
71660917 138831 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
CHEMBL3793118 138831 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 363 4 0 5 3.8 Cc1nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc2n1C 10.1016/j.bmc.2016.04.011
57396310 67793 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 7 1 3 4.8 CC(=O)NC1Cc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914853 67793 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 438 7 1 3 4.8 CC(=O)NC1Cc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
89690600 137638 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 345 4 0 5 3.7 Cc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3769585 137638 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 345 4 0 5 3.7 Cc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
59835909 121948 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601018 121948 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
11351174 139583 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 440 8 1 5 5.1 O=C(Cc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
CHEMBL380144 139583 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
ChEMBL 440 8 1 5 5.1 O=C(Cc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCN2CCCC2)c1 10.1021/jm0512286
11526309 188619 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 508 8 1 5 5.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(OC(F)(F)F)cc3)o2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL511480 188619 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 508 8 1 5 5.7 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(OC(F)(F)F)cc3)o2)CC1 10.1016/j.bmcl.2008.07.079
11396908 71453 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.2 O=C(NCc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
CHEMBL196839 71453 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 455 8 2 5 5.2 O=C(NCc1ccc(Oc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1 10.1016/j.bmcl.2005.03.114
70695851 73090 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 481 6 1 6 4.8 Cc1nc(N2CCN(CC(C)(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016700 73090 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 481 6 1 6 4.8 Cc1nc(N2CCN(CC(C)(C)C)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
10443307 66597 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 216 4 1 3 3.0 CCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL186659 66597 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 216 4 1 3 3.0 CCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
86695566 130695 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 494 9 0 7 3.8 CCN1CCN(Cc2ccc(C(=O)Cn3ccc(OCc4ccc(Cl)cn4)cc3=O)c(C)c2)CC1 nan
CHEMBL3686758 130695 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 494 9 0 7 3.8 CCN1CCN(Cc2ccc(C(=O)Cn3ccc(OCc4ccc(Cl)cn4)cc3=O)c(C)c2)CC1 nan
57401508 67729 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 514 7 0 3 6.4 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)c1ccccc1)CC2 10.1016/j.bmc.2011.09.007
CHEMBL1914635 67729 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 514 7 0 3 6.4 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCN(C(=O)c1ccccc1)CC2 10.1016/j.bmc.2011.09.007
70689525 73144 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 530 7 2 7 5.0 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016781 73144 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 530 7 2 7 5.0 Cc1nc(N2CCC(O)(C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
10303307 64130 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 565 7 2 6 5.8 CN(C)c1nc(NC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181393 64130 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 565 7 2 6 5.8 CN(C)c1nc(NC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
10073563 67180 5 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 472 5 1 5 5.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3Cl)cc12 10.1021/jm040762v
CHEMBL189653 67180 5 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 472 5 1 5 5.0 Cc1cc(N2CCN(C)CC2)nc2ccc(NC(=O)C(C)Oc3ccc(Cl)cc3Cl)cc12 10.1021/jm040762v
44394931 123506 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(C(F)(F)F)c2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL363047 123506 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 452 9 3 4 4.4 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2cccc(C(F)(F)F)c2)cc1OC 10.1016/j.bmcl.2004.07.077
11531010 133052 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL371222 133052 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 380 5 2 6 3.4 COc1ccc2[nH]nc(NC3CCN(Cc4ccc5c(c4)OCO5)CC3)c2c1 10.1016/j.bmcl.2005.08.049
15133403 204617 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 371 3 2 3 4.8 Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL87370 204617 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 371 3 2 3 4.8 Cc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
25113838 60445 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 528 8 1 4 7.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(-c5ccccc5)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
CHEMBL1761114 60445 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 528 8 1 4 7.6 CC(=O)Nc1cccc(C2CCN(CCCn3c(-c4ccc(-c5ccccc5)cc4)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2011.02.099
122184558 121871 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 477 10 1 3 4.9 CCN(CC(=O)N(C)C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600805 121871 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 477 10 1 3 4.9 CCN(CC(=O)N(C)C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmcl.2015.05.077
122184560 121875 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 7 0 2 5.9 CN(CCc1ccc(CN2CCCC2)cc1)C(=O)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600809 121875 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 7 0 2 5.9 CN(CCc1ccc(CN2CCCC2)cc1)C(=O)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.05.077
59835725 121898 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 459 6 1 4 4.4 NC(=O)C1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
CHEMBL3600831 121898 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 459 6 1 4 4.4 NC(=O)C1CCN(CCOc2ccc(C#Cc3ccc(-c4ccc(Cl)cc4)cn3)cc2)CC1 10.1016/j.bmcl.2015.05.077
59835758 121953 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 6 1 4 4.6 OC[C@H]1CCCN1CCOc1ccc(C#Cc2ccc(-c3ccc(Cl)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3601022 121953 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting methodDisplacement of [125I]-MCH from human MCHR1 expressed in CHO/Galpha16 cell membranes by scintillation counting method
ChEMBL 432 6 1 4 4.6 OC[C@H]1CCCN1CCOc1ccc(C#Cc2ccc(-c3ccc(Cl)cc3)cn2)cc1 10.1016/j.bmcl.2015.05.077
23593464 64356 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818783 64356 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 5 1 2 5.9 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
45271633 193863 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 510 5 1 3 5.8 O=C(NCc1ccc(Cl)cc1Cl)N1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
CHEMBL554511 193863 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 510 5 1 3 5.8 O=C(NCc1ccc(Cl)cc1Cl)N1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.067
90666097 108829 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 534 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
CHEMBL3219000 108829 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed CHO-K1 cell membrane by SPA-YSI assay
ChEMBL 534 7 1 5 7.3 CC(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4nc5ccccc5n4-c4ccc(F)cc4)cc3)CC2)c1 10.1039/C1MD00015B
11591644 15899 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1223829 15899 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 515 9 2 5 6.4 CC(=O)Nc1cccc(C2CCN(CCCNc3nc4ccccc4n3Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
57522945 76017 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059419 76017 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 429 7 1 4 5.7 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc([C@H](C)N3CCCC3)cnc12 10.1021/jm300167z
44403517 71158 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1cscn1 10.1016/j.bmcl.2005.06.089
CHEMBL196277 71158 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1cscn1 10.1016/j.bmcl.2005.06.089
10436090 65859 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL184438 65859 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
57401510 67733 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 481 7 1 3 5.3 CCNC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914639 67733 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 481 7 1 3 5.3 CCNC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
45272701 193968 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 422 4 1 4 5.5 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cn2)cc1 10.1016/j.bmcl.2009.06.101
CHEMBL556432 193968 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 422 4 1 4 5.5 O=C(Nc1ccc2nc(C3CC3)cn2c1)c1ccc(-c2ccc(C(F)(F)F)cn2)cc1 10.1016/j.bmcl.2009.06.101
1305 508 10 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2019.126741
9934033 508 10 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2019.126741
CHEMBL182150 508 10 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2019.126741
57522946 76018 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
CHEMBL2059421 76018 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 6.1 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)N3CCCCC3)cnc12 10.1021/jm300167z
57522701 76028 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 5.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)(C)N3CCCC3)cnc12 10.1021/jm300167z
CHEMBL2059514 76028 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 443 7 1 4 5.9 Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(C(C)(C)N3CCCC3)cnc12 10.1021/jm300167z
23593474 64357 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818784 64357 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 5 1 2 5.6 Cc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
21939915 64370 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818799 64370 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 1 3 5.9 O=C(Nc1ccc2c(c1)CCC(CN1CCOCC1)=C2)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmc.2011.07.038
57398088 67725 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914631 67725 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 466 7 0 3 5.5 CCC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
11582824 77724 0 None - 1 Rat 8.1 pIC50 = 8.1 Binding
Activity at chimeric rat/human MCH1R by accumulation of GTPgammaSActivity at chimeric rat/human MCH1R by accumulation of GTPgammaS
ChEMBL 431 4 1 6 3.9 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL210191 77724 0 None - 1 Rat 8.1 pIC50 = 8.1 Binding
Activity at chimeric rat/human MCH1R by accumulation of GTPgammaSActivity at chimeric rat/human MCH1R by accumulation of GTPgammaS
ChEMBL 431 4 1 6 3.9 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
56673713 66107 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818803 66107 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1852093 66107 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 402 5 2 2 5.8 CNCC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
57401509 67730 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914636 67730 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 488 7 0 4 4.5 CS(=O)(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
44402329 71563 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 3 5 6.4 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCCNC2CCCC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL197210 71563 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 469 9 3 5 6.4 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCCNC2CCCC2)c1 10.1016/j.bmcl.2005.03.114
11563383 70156 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
CHEMBL194691 70156 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 502 9 2 6 5.4 CCN1CCCC1CNc1cc(C)c2cc(NC(=O)COc3ccc(OC(F)(F)F)cc3)ccc2n1 10.1021/jm050103y
71730269 122007 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 391 8 0 6 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O 10.1016/j.bmcl.2015.05.065
CHEMBL3601304 122007 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCH-R1 expressed in CHO/Galpha16 cells after 60 mins by scintillation counting
ChEMBL 391 8 0 6 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O 10.1016/j.bmcl.2015.05.065
53317305 56395 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccccc2F)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642471 56395 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 408 8 0 5 4.0 O=c1cc(OCc2ccccc2F)ccn1-c1ccc(OCCN2CCCC2)cc1 10.1016/j.bmc.2010.12.002
24952419 91080 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
CHEMBL2403864 91080 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cellsDisplacement of [125I]MCH peptide from human MCHR1 expressed in CHOK1 cells
ChEMBL 442 5 2 5 4.9 Cc1ccc2c(c1)nc(C(C)(C)O)n2[C@H]1CC[C@@H](NC[C@H]2Cc3ccc(C#N)cc3C2)CC1 10.1016/j.bmcl.2013.05.017
44143504 187477 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 385 5 2 4 4.7 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccccc4)nc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497831 187477 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 385 5 2 4 4.7 CC(C)N(C)c1nc2ccc(NC(=O)c3ccc(-c4ccccc4)nc3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
45487653 197319 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of rat MCH1R receptorInhibition of rat MCH1R receptor
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
CHEMBL585664 197319 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of rat MCH1R receptorInhibition of rat MCH1R receptor
ChEMBL 494 6 0 7 3.9 CCO/N=C(/c1ccc(F)c(F)c1)c1ccc(CN2CCC3(CC2)OCc2cn(C)c(=O)cc23)cn1 10.1016/j.bmcl.2009.07.132
44394572 66166 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 287 4 1 5 1.9 CC(CN1CCOCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL185236 66166 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 287 4 1 5 1.9 CC(CN1CCOCC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
44394883 125830 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 271 6 2 4 2.6 CC(CNCC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
CHEMBL365041 125830 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 271 6 2 4 2.6 CC(CNCC1CC1)Oc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.034
60169185 87324 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 513 8 0 6 5.7 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4Cl)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337731 87324 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 513 8 0 6 5.7 COc1cc(N2Cc3ccc(Sc4ccc(F)cc4Cl)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
60168818 87333 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 5 4.5 COc1cc(N2Cc3ccc(Cc4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337740 87333 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 461 8 0 5 4.5 COc1cc(N2Cc3ccc(Cc4ccc(F)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
71720120 87342 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 7 0 5 4.7 COc1cc(N2Cc3ccc(-c4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337749 87342 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 443 7 0 5 4.7 COc1cc(N2Cc3ccc(-c4ccc(C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89690600 137638 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 345 4 0 5 3.7 Cc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
CHEMBL3769585 137638 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 345 4 0 5 3.7 Cc1nc2ccc(-n3ccc(OCc4ccccc4)cc3=O)cn2c1C 10.1021/acs.jmedchem.5b01704
57390252 67796 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 409 6 0 2 6.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCCCC2 10.1016/j.bmc.2011.09.007
CHEMBL1914856 67796 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 409 6 0 2 6.5 O=C(CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc2c(c1)CCCCC2 10.1016/j.bmc.2011.09.007
44442148 154146 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 520 9 2 6 6.7 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OCc6ccccc6)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL399734 154146 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 520 9 2 6 6.7 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccc(OCc6ccccc6)cc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
44403472 71370 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 388 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1O 10.1016/j.bmcl.2005.06.089
CHEMBL196591 71370 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 388 4 2 5 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)ccc1O 10.1016/j.bmcl.2005.06.089
44417915 140845 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 471 6 1 5 5.0 COC(=O)C1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL383884 140845 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 471 6 1 5 5.0 COC(=O)C1CCCN1c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
11632484 69976 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 388 7 1 4 4.2 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)ccc3c2)cc1 10.1021/jm050103y
CHEMBL194477 69976 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 388 7 1 4 4.2 Cc1ccc(/C=C/C(=O)Nc2ccc3nc(N(C)CCN(C)C)ccc3c2)cc1 10.1021/jm050103y
44407711 75564 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205115 75564 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
22254570 65794 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 270 4 1 3 4.2 Nc1ccc2cccc(OCCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL184102 65794 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 270 4 1 3 4.2 Nc1ccc2cccc(OCCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
70683299 73245 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 503 5 1 5 5.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
CHEMBL2017747 73245 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 503 5 1 5 5.2 C/C(=C\C(=O)Nc1ccc2nc(N3CCC(N4CCCC4=O)CC3)nc(C)c2c1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.03.049
45271994 193507 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 557 5 1 4 5.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCC(C(F)(F)F)CC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL550535 193507 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 557 5 1 4 5.1 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCC(C(F)(F)F)CC2)C1 10.1016/j.bmcl.2009.05.066
44401616 69675 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NCC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193970 69675 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NCC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
45273392 194057 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 444 7 2 4 4.2 O=C(CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1)NCC(O)C(F)(F)F 10.1016/j.bmcl.2009.05.067
CHEMBL557306 194057 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 444 7 2 4 4.2 O=C(CC1CCN(Cc2ccc(-c3ccc(Cl)cc3)o2)CC1)NCC(O)C(F)(F)F 10.1016/j.bmcl.2009.05.067
10421932 66732 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 6 1 3 3.8 CCCCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
CHEMBL187295 66732 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 244 6 1 3 3.8 CCCCCCOc1cccc2ccc(N)nc12 10.1016/j.bmcl.2004.07.032
44417934 82039 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 435 7 1 5 3.0 CN(C)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
CHEMBL217605 82039 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 435 7 1 5 3.0 CN(C)Cc1ccc(CCN2CCn3nc(C(=O)Nc4ccc(F)cc4)cc3C2=O)cc1 10.1016/j.bmcl.2019.126741
11496313 71953 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL198361 71953 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 461 6 1 6 4.3 Cc1cc(N2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
3611477 126979 7 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 443 5 1 4 5.9 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL366180 126979 7 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 443 5 1 4 5.9 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
89690124 137758 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 439 5 0 5 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770865 137758 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 439 5 0 5 5.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(C(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
45272024 193731 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 516 5 3 4 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC12CC3CC(CC(O)(C3)C1)C2 10.1016/j.bmcl.2009.05.066
CHEMBL552144 193731 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 516 5 3 4 4.8 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC12CC3CC(CC(O)(C3)C1)C2 10.1016/j.bmcl.2009.05.066
44562415 176381 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 436 6 1 5 3.9 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL462351 176381 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 436 6 1 5 3.9 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1016/j.bmcl.2008.07.079
44408109 75177 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204428 75177 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 488 7 1 6 4.6 Cc1cc(N2CCC(N(C)C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44402505 71084 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 499 10 2 6 6.0 COC[C@@H]1CCCN1CCCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
CHEMBL196115 71084 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 499 10 2 6 6.0 COC[C@@H]1CCCN1CCCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc21 10.1016/j.bmcl.2005.03.114
44396196 66636 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 421 6 1 6 3.8 CCN1CCN(c2cc(C)c3cc(NC(=O)CSc4ccncc4)ccc3n2)CC1 10.1021/jm040762v
CHEMBL186842 66636 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cellsInhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
ChEMBL 421 6 1 6 3.8 CCN1CCN(c2cc(C)c3cc(NC(=O)CSc4ccncc4)ccc3n2)CC1 10.1021/jm040762v
10083101 65724 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 2 1 3 3.4 CC1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.032
CHEMBL183739 65724 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 242 2 1 3 3.4 CC1CCC(Oc2cccc3ccc(N)nc23)C1 10.1016/j.bmcl.2004.07.032
89789910 130700 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 8 2.5 Cc1cc(CN2CCNCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686763 130700 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 467 8 1 8 2.5 Cc1cc(CN2CCNCC2)ccc1C(=O)Cn1ncc(OCc2ccc(Cl)cn2)cc1=O nan
45267561 194900 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 438 5 1 4 5.3 CN(C)Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
CHEMBL563984 194900 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptorDisplacement of [125I]MCH from human MCH1 receptor
ChEMBL 438 5 1 4 5.3 CN(C)Cc1cn2cc(NC(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)ccc2n1 10.1016/j.bmcl.2009.06.101
44407711 75564 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL205115 75564 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 426 8 1 5 4.2 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2005.10.066
11204090 63162 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(N[C@H]2CC[C@@H](NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL180003 63162 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(N[C@H]2CC[C@@H](NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44401449 70735 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 544 6 2 6 5.0 O=S(=O)(NC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL195346 70735 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCHInhibitory activity against mutated constitutively activated human Melanin concentrating hormone receptor 1 (CA-MCH-R1) stably expressed in HEK293 cells using [125I](Phe13, Tyr19) MCH
ChEMBL 544 6 2 6 5.0 O=S(=O)(NC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
10149893 81027 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 333 6 2 3 4.3 CCCc1cc(N)c2cc(NC(=O)CCc3ccccc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL215955 81027 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 333 6 2 3 4.3 CCCc1cc(N)c2cc(NC(=O)CCc3ccccc3)ccc2n1 10.1016/j.bmcl.2006.08.008
91759555 130725 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 480 8 0 7 3.4 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
CHEMBL3686788 130725 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 480 8 0 7 3.4 Cc1cc(CN2CCN(C)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(Cl)cn2)cc1=O nan
23593472 64359 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
CHEMBL1818786 64359 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 7 1 2 6.2 CCCc1ccc(-c2ccc(C(=O)Nc3ccc4c(c3)CCC(CN(C)C)C4)cc2)cc1 10.1016/j.bmc.2011.07.038
70691651 73102 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 7 1 7 4.3 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016713 73102 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 7 1 7 4.3 Cc1nc(N2CCN(C(=O)C3CCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
44442067 93864 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 380 6 2 5 4.9 CN(C)c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250544 93864 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 380 6 2 5 4.9 CN(C)c1ccc2nc(N[C@H]3CCC[C@H](NCc4ccsc4)C3)ccc2c1 10.1016/j.bmcl.2007.05.034
1314 3657 18 None - 1 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
9865843 3657 18 None - 1 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
CHEMBL178707 3657 18 None - 1 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.07.034
11539632 70202 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 70202 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assayDisplacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
89691057 138928 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 433 7 0 5 5.7 CCCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794238 138928 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 433 7 0 5 5.7 CCCn1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
10255474 123141 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2ccc(Nc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
CHEMBL362094 123141 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligandBinding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using [125I]MCH as radioligand
ChEMBL 501 10 4 5 5.7 COc1cc(NC(=O)Nc2ccc(Nc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1 10.1016/j.bmcl.2004.07.077
44405477 71654 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 340 4 2 3 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccccc4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
CHEMBL197485 71654 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 340 4 2 3 4.3 Clc1ccc2[nH]nc(NC3CCN(Cc4ccccc4)CC3)c2c1 10.1016/j.bmcl.2005.08.049
70691724 73207 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 450 7 2 5 5.0 Cc1nc(N(CCO)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017610 73207 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 450 7 2 5 5.0 Cc1nc(N(CCO)C2CCCC2)nc2ccc(NC(=O)/C=C/c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.049
44207909 16505 1 None - 9 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL1242923 16505 1 None - 9 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
44207909 16505 1 None - 9 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
CHEMBL1242923 16505 1 None - 9 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]NMS from human mAChR1 receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
ChEMBL 407 7 1 4 2.6 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm5013243
57391027 67722 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 436 6 0 3 4.6 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(F)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914628 67722 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 436 6 0 3 4.6 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccc(F)cc4)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
57391045 67791 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.5 CC(=O)N1CCCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
CHEMBL1914851 67791 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells
ChEMBL 452 6 0 3 5.5 CC(=O)N1CCCc2ccc(C(=O)CCCN3CCC(c4ccc(Cl)cc4)CC3)cc2C1 10.1016/j.bmc.2011.09.007
44438753 93014 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 570 8 2 6 3.8 O=C(NCCN1CCC(F)(F)CC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
CHEMBL246051 93014 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHR1 expressed in IMR32 cells
ChEMBL 570 8 2 6 3.8 O=C(NCCN1CCC(F)(F)CC1)c1ccc(CN2CCC(NC(=O)c3cc(=O)c4ccc(F)cc4o3)CC2)cc1 10.1016/j.bmcl.2006.11.068
49865871 15988 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 471 9 2 5 6.3 CCNc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224082 15988 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 471 9 2 5 6.3 CCNc1cccc(C2CCN(CCCNc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44407956 74497 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL203161 74497 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 488 6 2 6 4.6 Cc1cc(N2C[C@H](C)N[C@H](C)C2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44417976 165378 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 7 1 3 5.7 CCN(CC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
CHEMBL425098 165378 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 415 7 1 3 5.7 CCN(CC)c1ccc2cc(NC(=O)CCc3ccc(C(F)(F)F)cc3)ccc2n1 10.1016/j.bmcl.2006.08.006
49865976 16026 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 470 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
CHEMBL1224230 16026 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 470 7 1 4 5.9 CC(=O)Nc1cccc(C2CCN(CCCc3nc4ccccc4n3-c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2010.07.086
44395082 65740 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 546 10 3 5 5.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2Br)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL183839 65740 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 546 10 3 5 5.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(OC(F)(F)F)cc2Br)cc1OC 10.1016/j.bmcl.2004.07.077
44442119 93801 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 377 6 2 6 3.9 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cnccn4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL250122 93801 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 377 6 2 6 3.9 COc1ccc2c(C)cc(N[C@H]3CCC[C@H](NCc4cnccn4)C3)nc2c1 10.1016/j.bmcl.2007.05.034
155520135 172662 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 400 5 0 4 3.8 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3cccnc3)cn1)C2 10.1016/j.bmcl.2019.126741
CHEMBL4524539 172662 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 400 5 0 4 3.8 CN(C)Cc1ccc2c(c1)CC[C@H](N(C)C(=O)c1ccc(-c3cccnc3)cn1)C2 10.1016/j.bmcl.2019.126741
59691661 121917 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 433 6 2 2 6.3 O=C(NCc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600977 121917 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 433 6 2 2 6.3 O=C(NCc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
71730269 122007 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 391 8 0 6 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
CHEMBL3601304 122007 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 391 8 0 6 3.1 Cc1cc(CN(C)C)ccc1C(=O)Cn1ncc(OCc2ccccc2)cc1=O nan
44405651 71571 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
CHEMBL197232 71571 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human MCHr1 from neuronal IMR32 cellsBinding affinity to human MCHr1 from neuronal IMR32 cells
ChEMBL 475 6 1 7 4.9 Clc1ccc2c(c1)c(NC1CCN(Cc3ccc4c(c3)OCO4)CC1)nn2Cc1ccccn1 10.1016/j.bmcl.2005.08.049
44417844 141043 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 345 5 2 3 4.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL384994 141043 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 345 5 2 3 4.7 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(C)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44417874 141117 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 377 6 2 4 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(SC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL385398 141117 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 377 6 2 4 5.1 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(SC)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
25116308 60440 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1ccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)cc1 10.1016/j.bmcl.2011.02.099
CHEMBL1761109 60440 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assayDisplacement of Eu-labeled MCH from human MCH-R1 expressed in CHO by time-resolved fluorometric assay
ChEMBL 482 8 1 5 5.9 COc1ccc(-c2nc3ccccc3n2CCCN2CCC(c3cccc(NC(C)=O)c3)CC2)cc1 10.1016/j.bmcl.2011.02.099
122184697 121964 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 459 10 2 6 4.4 CC(=O)NC1CCN(Cc2ccc(NCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
CHEMBL3601038 121964 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 459 10 2 6 4.4 CC(=O)NC1CCN(Cc2ccc(NCCCc3ccc(Oc4ccccc4)nn3)cc2)CC1 10.1016/j.bmcl.2015.05.074
9934161 74587 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 464 4 2 3 5.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032048 74587 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation countingDisplacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting
ChEMBL 464 4 2 3 5.1 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCOCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
44410904 171880 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
CHEMBL448110 171880 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 452 4 1 7 3.9 Cn1c(=O)nc(NC2CC3CCC(C2)N3Cc2ccc3c(c2)OCO3)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.02.044
44442090 93713 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL249489 93713 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 367 6 2 5 4.8 COc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
44442139 94009 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 414 6 2 5 5.2 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
CHEMBL251290 94009 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 414 6 2 5 5.2 COc1ccc2c(C)cc(N[C@H]3CC[C@H](NCc4cn(C)c5ccccc45)C3)nc2c1 10.1016/j.bmcl.2007.05.034
70693733 73113 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 8 2 7 4.3 Cc1nc(N2CCC(C(=O)NC3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016724 73113 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 543 8 2 7 4.3 Cc1nc(N2CCC(C(=O)NC3CC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.050
49866088 16053 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 482 7 1 4 5.9 O=C1Cc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2N1 10.1016/j.bmcl.2010.07.086
CHEMBL1224388 16053 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHOK1 cells by scintillation proximity assay
ChEMBL 482 7 1 4 5.9 O=C1Cc2ccc(C3CCN(CCCCc4nc5ccccc5n4-c4ccc(F)cc4)CC3)cc2N1 10.1016/j.bmcl.2010.07.086
127030367 138521 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 9 0 8 3.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)CC5(C)COC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3786311 138521 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 478 9 0 8 3.1 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN(C)CC5(C)COC5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
127030070 138618 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 464 7 1 8 2.6 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC(C)(O)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
CHEMBL3787261 138618 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 464 7 1 8 2.6 COc1ccc(-c2nnc(C(=O)N3CC(Oc4ccc(CN5CCC(C)(O)C5)cc4)C3)o2)cc1 10.1021/acs.jmedchem.5b01654
56597689 138623 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 392 6 0 6 3.0 Cc1cc(CN(C)C)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 10.1021/acs.jmedchem.5b01654
CHEMBL3787333 138623 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis
ChEMBL 392 6 0 6 3.0 Cc1cc(CN(C)C)ccc1OC1CN(C(=O)c2nnc(-c3ccccc3)o2)C1 10.1021/acs.jmedchem.5b01654
11627122 141194 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 480 8 3 4 5.2 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2006.07.040
CHEMBL385831 141194 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 480 8 3 4 5.2 O=C(Nc1cccc(F)c1)Nc1cc(C(=O)NCCN2CCCC2)ccc1Oc1cccc(F)c1 10.1016/j.bmcl.2006.07.040
44403477 71469 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 387 4 2 5 3.0 Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
CHEMBL196898 71469 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 387 4 2 5 3.0 Nc1ccc(Cl)cc1C(=O)NC1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2005.06.089
44403513 133743 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
CHEMBL371700 133743 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 468 7 3 7 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1c[nH]cn1 10.1016/j.bmcl.2005.06.089
44403511 135637 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 475 8 2 8 3.2 COc1ccc(NCc2cncnc2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL373266 135637 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 475 8 2 8 3.2 COc1ccc(NCc2cncnc2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403518 71405 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
CHEMBL196681 71405 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 485 7 2 8 3.9 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(Cl)cnc1NCc1nccs1 10.1016/j.bmcl.2005.06.089
11545677 70019 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 394 5 1 4 5.0 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
CHEMBL194523 70019 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration aganist melanin concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 394 5 1 4 5.0 O=c1cc(NC2CCN(C/C=C/c3ccccc3)CC2)c2cc(Cl)ccc2o1 10.1021/jm050598r
89689924 137791 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 449 5 0 5 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Br)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771307 137791 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 449 5 0 5 5.0 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4ccc(Br)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
89702566 138785 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3792707 138785 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 411 5 0 6 4.9 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4csc(Cl)c4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
11512135 69950 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194408 69950 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 460 8 1 5 4.9 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
44390742 122761 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL361442 122761 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3ccc(F)cc3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
11559625 56406 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 364 8 0 5 3.4 CN(C)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
CHEMBL1642484 56406 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assayDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
ChEMBL 364 8 0 5 3.4 CN(C)CCOc1ccc(-n2ccc(OCc3ccccc3)cc2=O)cc1 10.1016/j.bmc.2010.12.002
44390713 123165 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL362193 123165 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 407 5 2 5 4.0 CN(C)c1nc(N[C@H]2CC[C@@H](NC(=O)c3cccc(F)c3)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44573820 192655 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 489 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
CHEMBL523882 192655 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 489 6 1 2 6.5 Cc1ccc(N(C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)c2ccc(F)c(F)c2)cc1 10.1016/j.bmcl.2009.04.016
11627530 75542 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204952 75542 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 504 9 2 7 4.2 Cc1cc(NCCN2CCOCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
10005009 165812 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL427540 165812 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 472 6 2 6 4.0 Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
56666754 64368 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 7 1 2 6.9 CCN(CC)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
CHEMBL1818797 64368 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 444 7 1 2 6.9 CCN(CC)CC1=Cc2ccc(NC(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmc.2011.07.038
44573932 186898 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 482 7 0 7 2.9 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cnnn1 10.1016/j.bmcl.2009.04.016
CHEMBL494156 186898 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from human MCHR1 expressed in CHO cells
ChEMBL 482 7 0 7 2.9 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)C(c1ccc(F)c(F)c1)n1cnnn1 10.1016/j.bmcl.2009.04.016
22254551 124511 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.034
CHEMBL364377 124511 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.034
44394592 65416 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 376 5 2 5 3.4 CC(=O)Nc1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
CHEMBL183468 65416 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 376 5 2 5 3.4 CC(=O)Nc1ccc(CN2CC[C@H](Oc3cccc4ccc(N)nc34)C2)cc1 10.1016/j.bmcl.2004.07.035
22254551 124511 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.035
CHEMBL364377 124511 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.035
22254551 124511 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
CHEMBL364377 124511 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranesConcentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
ChEMBL 256 3 1 3 3.8 Nc1ccc2cccc(OCC3CCCCC3)c2n1 10.1016/j.bmcl.2004.07.032
71719526 87347 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 471 8 0 5 5.5 COc1cc(N2Cc3ccc(-c4ccc(C(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
CHEMBL2337754 87347 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assayDisplacement of Eu-MCH from human MCHR1 expressed in CHO cell membranes by TRF assay
ChEMBL 471 8 0 5 5.5 COc1cc(N2Cc3ccc(-c4ccc(C(C)C)cc4)nc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2013.01.053
89691284 138879 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 6 0 5 4.4 Cn1c(CC2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3793827 138879 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 403 6 0 5 4.4 Cn1c(CC2CC2)nc2ccc(-n3ccc(OCc4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
117798671 138813 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3793001 138813 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4csc(C(F)(F)F)c4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
117798692 138803 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
CHEMBL3792893 138803 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 419 4 0 6 4.7 Cc1c2cc(-n3ccc(OCc4ccc(C(F)(F)F)s4)cc3=O)ccc2nn1C 10.1016/j.bmc.2016.04.013
45273778 194170 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 496 6 3 4 4.8 O=C(NCc1nc2ccccc2[nH]1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
CHEMBL558533 194170 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 496 6 3 4 4.8 O=C(NCc1nc2ccccc2[nH]1)NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1 10.1016/j.bmcl.2009.05.066
23022394 76012 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 444 8 2 4 5.5 CCCCC(=O)Nc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
CHEMBL2059414 76012 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 444 8 2 4 5.5 CCCCC(=O)Nc1ccc(C(=O)Nc2ccc3cc(CN4CCCC4)cnc3c2C)cc1 10.1021/jm300167z
44396952 66380 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1ccccc1-c1ccc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
CHEMBL185688 66380 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 458 7 1 5 4.4 COc1ccccc1-c1ccc(CC(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.bmcl.2005.05.023
44397425 66528 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 422 5 1 5 3.7 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2005.05.023
CHEMBL186333 66528 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 422 5 1 5 3.7 O=C(NC1CCCN(Cc2ccc3c(c2)OCO3)C1)c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2005.05.023
44397221 66781 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 453 6 1 5 4.3 N#Cc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
CHEMBL187503 66781 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)Inhibition of binding to MCHR1 of human neuronal IMR32-derived cell-line I3.4.2 (Galpha-16 transfected)
ChEMBL 453 6 1 5 4.3 N#Cc1cccc(-c2ccc(CC(=O)NC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.bmcl.2005.05.023
44403527 126641 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 477 8 2 8 3.2 COc1ccc(NCc2cncn2C)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL365734 126641 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cellsInhibitory activity towards melanin-concentrating hormone receptor 1 in IMR32 cells
ChEMBL 477 8 2 8 3.2 COc1ccc(NCc2cncn2C)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
44403498 70719 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 437 8 2 6 3.6 COc1ccc(NCC2CC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
CHEMBL195255 70719 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against MCH1R IMR32 cells in FLIPR-based assayInhibitory concentration against MCH1R IMR32 cells in FLIPR-based assay
ChEMBL 437 8 2 6 3.6 COc1ccc(NCC2CC2)c(C(=O)NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c1 10.1016/j.bmcl.2005.06.089
57403264 67719 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccccc4C)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
CHEMBL1914625 67719 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cellsDisplacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
ChEMBL 432 6 0 3 4.8 CC(=O)N1CCc2ccc(C(=O)CCCN3CCC(c4ccccc4C)CC3)cc2CC1 10.1016/j.bmc.2011.09.007
89691264 138944 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 407 5 0 7 3.6 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ncc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
CHEMBL3794445 138944 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting
ChEMBL 407 5 0 7 3.6 Cn1c(C2CC2)nc2ccc(-n3ccc(OCc4ncc(Cl)cn4)cc3=O)cc21 10.1016/j.bmc.2016.04.011
44143505 187448 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 403 5 2 4 4.9 CC(C)N(C)c1nc2ccc(NC(=O)c3cncc(-c4ccc(F)cc4)c3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
CHEMBL497638 187448 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation countingDisplacement of [125I]MCH from human MCH1 receptor expressed in CHO-K1 cells by scintillation counting
ChEMBL 403 5 2 4 4.9 CC(C)N(C)c1nc2ccc(NC(=O)c3cncc(-c4ccc(F)cc4)c3)cc2[nH]1 10.1016/j.bmcl.2009.04.147
44562405 190303 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 6 1 5 3.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3c(c2)OCCO3)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL518514 190303 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 6 1 5 3.3 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc3c(c2)OCCO3)CC1 10.1016/j.bmcl.2008.07.079
57390739 69282 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 494 7 1 5 5.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934832 69282 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 494 7 1 5 5.6 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccc(C)cc4)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
70691739 73262 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 543 7 2 7 3.9 Cc1nc(N2CCC(N(C)C(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017764 73262 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 543 7 2 7 3.9 Cc1nc(N2CCC(N(C)C(=O)CO)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
11974228 79947 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 460 4 1 6 3.3 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)c(F)c2o1 10.1021/jm060683e
CHEMBL214413 79947 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 460 4 1 6 3.3 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)c(F)c(F)c2o1 10.1021/jm060683e
44407860 75055 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
CHEMBL204082 75055 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assayDisplacement of [3H]myo-inositol from human MCH1 receptor expressed in CHO cell by IP3 assay
ChEMBL 564 9 2 6 6.5 Cc1cc(NC2CCN(Cc3ccccc3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2005.10.066
44402567 165248 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 485 8 3 6 5.3 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCCN2CCC(O)CC2)c1 10.1016/j.bmcl.2005.03.114
CHEMBL424836 165248 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 485 8 3 6 5.3 O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2c(cnn2CCCN2CCC(O)CC2)c1 10.1016/j.bmcl.2005.03.114
44394983 65933 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 446 9 3 4 4.7 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
CHEMBL184720 65933 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 446 9 3 4 4.7 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1C(=O)NCCCN(C)C 10.1016/j.bmcl.2004.07.077
122184700 121968 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 419 9 1 6 4.2 O[C@@H]1CCCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)C1 10.1016/j.bmcl.2015.05.074
CHEMBL3601041 121968 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 419 9 1 6 4.2 O[C@@H]1CCCN(Cc2ccc(OCCCc3ccc(Oc4ccccc4)nn3)cc2)C1 10.1016/j.bmcl.2015.05.074
89690237 137683 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ncc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770135 137683 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 406 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ncc(OCc4ccc(Cl)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
44562403 189226 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 413 5 1 5 4.4 O=C(NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)c1csc([N+](=O)[O-])c1 10.1016/j.bmcl.2008.07.079
CHEMBL516489 189226 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 413 5 1 5 4.4 O=C(NC1CCN(Cc2ccc(Cl)c(Cl)c2)CC1)c1csc([N+](=O)[O-])c1 10.1016/j.bmcl.2008.07.079
46902026 16775 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253789 16775 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44562462 178579 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 493 7 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(C(F)(F)F)cn3)o2)CC1 10.1016/j.bmcl.2008.07.079
CHEMBL472196 178579 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 493 7 1 5 5.2 O=C(COc1cccc(Cl)c1)NC1CCN(Cc2ccc(-c3ccc(C(F)(F)F)cn3)o2)CC1 10.1016/j.bmcl.2008.07.079
91759550 130719 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 465 8 1 7 3.1 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
CHEMBL3686782 130719 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).Binding Assay: Membranes from CHO/Galpha16 cells stably transfected with human hMCH-1R are resuspended using a syringe (needle 0.6x25 mm) and diluted in test buffer (50 mM HEPES, 10 mM MgCl2, 2 mM EGTA, pH 7.00; 0.1% bovine serum albumin (protease-free), 0.021% bacitracin, 1 ug/ml aprotinin, 1 ug/ml leupeptin and 1 uM phosphoramidone) to a concentration of 5 to 15 ug/ml. 200 microliters of this membrane fraction (contains 1 to 3 ug of protein) are incubated for 60 minutes at ambient temperature with 100 pM of 125I-tyrosyl melanin concentrating hormone (125I-MCH commercially obtainable from NEN) and increasing concentrations of the test compound in a final volume of 250 microliters. After the incubation the reaction is filtered using a cell harvester through 0.5% PEI treated fibreglass filters (GF/B, Unifilter Packard). The membrane-bound radioactivity retained on the filter is then determined after the addition of scintillator substance (Packard Microscint 20).
ChEMBL 465 8 1 7 3.1 Cc1cc(CN2CCC(O)CC2)ccc1C(=O)Cn1ccc(OCc2ccc(F)cn2)cc1=O nan
70683300 73247 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 7 4.6 Cc1nc(N2CCC(N3C(=O)CCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
CHEMBL2017749 73247 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125-I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 553 6 1 7 4.6 Cc1nc(N2CCC(N3C(=O)CCC3=O)CC2)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1016/j.bmcl.2012.03.049
59691704 121915 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 434 7 1 3 6.0 O=C(COc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3600975 121915 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 434 7 1 3 6.0 O=C(COc1ccc(-c2ccc(Cl)cc2)cc1)Nc1ccc(CN2CCCCC2)cc1 10.1016/j.bmcl.2015.05.074
127025395 137740 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 431 3 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc4c(c3=O)CCC(c3ccc(Cl)cc3)O4)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3770680 137740 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 431 3 0 5 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc4c(c3=O)CCC(c3ccc(Cl)cc3)O4)cn12 10.1021/acs.jmedchem.5b01704
44407997 75023 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 402 7 1 4 4.6 C/C(=C\c1ccccc1)C(=O)Nc1ccc2nc(N(C)CCN(C)C)cc(C)c2c1 10.1016/j.bmcl.2005.10.066
CHEMBL203917 75023 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human MCH1 receptor by SPA assayInhibition of human MCH1 receptor by SPA assay
ChEMBL 402 7 1 4 4.6 C/C(=C\c1ccccc1)C(=O)Nc1ccc2nc(N(C)CCN(C)C)cc(C)c2c1 10.1016/j.bmcl.2005.10.066
44413259 139147 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 507 5 1 4 6.5 Fc1cc2[nH]c(C(=C3CCN(CC4CC4)CC3)c3ccc(-c4cncnc4)cc3)nc2cc1C(F)(F)F 10.1016/j.bmcl.2019.126741
CHEMBL379802 139147 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assayAntagonist activity at MCHR1 (unknown origin) expressed in CHO cells co-expressing aequorin incubated for 10 mins by luminescence assay
ChEMBL 507 5 1 4 6.5 Fc1cc2[nH]c(C(=C3CCN(CC4CC4)CC3)c3ccc(-c4cncnc4)cc3)nc2cc1C(F)(F)F 10.1016/j.bmcl.2019.126741
44417906 140866 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 449 5 1 6 4.0 CCc1nc2cc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)ccc2o1 10.1016/j.bmcl.2006.11.065
CHEMBL384043 140866 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cellsDisplacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
ChEMBL 449 5 1 6 4.0 CCc1nc2cc(CN3CCC(NC(=O)c4cc(=O)c5ccc(F)cc5o4)CC3)ccc2o1 10.1016/j.bmcl.2006.11.065
44417864 79865 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 389 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(OC(C)=O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
CHEMBL214020 79865 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R1
ChEMBL 389 6 2 5 4.3 CCCc1cc(N)c2cc(NC(=O)/C=C/c3ccc(OC(C)=O)cc3)ccc2n1 10.1016/j.bmcl.2006.08.008
44403747 70227 5 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 7 1 5 5.1 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(C)C)cc4)ccc3n2)CC1 10.1021/jm050103y
CHEMBL194946 70227 5 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 458 7 1 5 5.1 CCN1CCN(c2cc(C)c3cc(NC(=O)/C=C/c4ccc(OC(C)C)cc4)ccc3n2)CC1 10.1021/jm050103y
122184691 121956 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 402 9 1 5 4.8 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
CHEMBL3601030 121956 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I-MCH] from human MCH receptor 1 expressed in CHO cell membranes by scintillation counting method
ChEMBL 402 9 1 5 4.8 COc1ccc(-c2ccc(CCCNc3ccc(CN4CCCC4)cc3)nn2)cc1 10.1016/j.bmcl.2015.05.074
89690622 137795 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771336 137795 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 377 5 0 6 4.3 Cc1c(C2CC2)nc2ccc(-n3ccc(OCc4cccs4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
21939767 64352 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
CHEMBL1818777 64352 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 384 5 1 2 5.3 CN(C)CC1CCc2cc(NC(=O)c3ccc(-c4ccccc4)cc3)ccc2C1 10.1016/j.bmc.2011.07.038
127029631 137671 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(Oc4ccc(OC(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3769964 137671 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 5 0 6 5.4 Cc1c(C2CC2)nc2ccc(-n3ccc(Oc4ccc(OC(F)(F)F)cc4)cc3=O)cn12 10.1021/acs.jmedchem.5b01704
57401251 69274 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccccc4Cl)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
CHEMBL1934824 69274 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assayDisplacement of Eu-MCH from human recombinant MCH-R1 expressed in CHO cell membrane after 90 mins by time-resolved fluorescence assay
ChEMBL 514 7 1 5 5.9 CC(=O)Nc1cccc(C2CCN(CCCn3nc(-c4ccccc4Cl)c4ccccc4c3=O)CC2)c1 10.1016/j.bmcl.2011.10.111
70685336 73092 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCN(C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
CHEMBL2016702 73092 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assayDisplacement of [125I]MCH from human recombinant MCHR1 expressed in CHO-K1 cell membranes after 2 hrs by SPA binding assay
ChEMBL 479 6 1 6 4.7 Cc1nc(N2CCN(C3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2012.03.050
44394926 125726 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 430 10 3 5 4.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(SC)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
CHEMBL365011 125726 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)Binding affinity against human Melanin-concentrating hormone receptor 1 stably transfected CHO cells was determined using scintillation proximity assay (SPA)
ChEMBL 430 10 3 5 4.1 CCN(CC)CCNC(=O)c1ccc(NC(=O)Nc2ccc(SC)cc2)cc1OC 10.1016/j.bmcl.2004.07.077
44390385 121988 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 565 9 2 6 6.4 CN(C)c1nc(NCC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360117 121988 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cellsInhibitory activity against human CA-MCH-R1 (Melanin-concentrating hormone receptor 1) by using [125I](Phe13,Tyr19)MCH as radioligand expressed in HEK293 cells
ChEMBL 565 9 2 6 6.4 CN(C)c1nc(NCC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44417955 82008 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 397 5 1 5 3.7 O=C(COc1ccc(Cl)cc1)Nc1ccc2nc(N3CCOCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
CHEMBL217460 82008 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranesDisplacement of 125I-[Phe13,Tyr19]-MCH from MCH-R1 expressing cell membranes
ChEMBL 397 5 1 5 3.7 O=C(COc1ccc(Cl)cc1)Nc1ccc2nc(N3CCOCC3)ccc2c1 10.1016/j.bmcl.2006.11.092
44562443 178601 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 451 7 1 4 4.9 Cc1cc(CN2CCC(NC(=O)COc3cccc(Cl)c3)CC2)c(C)n1-c1ccccc1 10.1016/j.bmcl.2008.07.079
CHEMBL472380 178601 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 451 7 1 4 4.9 Cc1cc(CN2CCC(NC(=O)COc3cccc(Cl)c3)CC2)c(C)n1-c1ccccc1 10.1016/j.bmcl.2008.07.079
11705240 132279 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL370120 132279 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cellsDisplacement of 150p M [125I]MCH from human MCH1R expressed in CHO-K1 cells
ChEMBL 459 6 1 5 5.5 Cc1cc(N2CCCCC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
20817864 75692 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 483 5 1 8 3.8 COC(=O)c1c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n(C)c1=O 10.1016/j.bmcl.2006.02.044
CHEMBL205741 75692 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 483 5 1 8 3.8 COC(=O)c1c(NC2CCN(Cc3ccc4c(c3)OCO4)CC2)c2cc(Cl)ccc2n(C)c1=O 10.1016/j.bmcl.2006.02.044
44402635 71495 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 446 7 2 5 3.9 O=C(Nc1ccc2c(cnn2CCN2CCCC2)c1)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.03.114
CHEMBL196991 71495 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCHInhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]MCH
ChEMBL 446 7 2 5 3.9 O=C(Nc1ccc2c(cnn2CCN2CCCC2)c1)NC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.03.114
127028869 138952 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1nn(C)c2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc12 10.1016/j.bmc.2016.04.013
CHEMBL3794501 138952 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation countingDisplacement of [125I]-MCH(4 to 19) from human MCHR1 expressed in CHO cell membranes after 1 hr liquid scintillation counting
ChEMBL 379 4 0 5 4.3 Cc1nn(C)c2ccc(-n3ccc(OCc4ccc(Cl)cc4)cc3=O)cc12 10.1016/j.bmc.2016.04.013
11974227 168728 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)cc(F)c2o1 10.1021/jm060683e
CHEMBL441542 168728 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 cellsDisplacement of [125I]MCH from MCHr1 expressed in IMR32 cells
ChEMBL 442 4 1 6 3.2 O=C(NC1CCN(Cc2ccc3c(c2)OCO3)CC1)c1cc(=O)c2cc(F)cc(F)c2o1 10.1021/jm060683e
11635230 193893 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 539 5 1 6 2.6 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCS(=O)(=O)CC2)C1 10.1016/j.bmcl.2009.05.066
CHEMBL555135 193893 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cellsDisplacement of [125I]MCH from human MCH1 receptor expressed in HEK293 cells
ChEMBL 539 5 1 6 2.6 O=C(NC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)N1CC(N2CCS(=O)(=O)CC2)C1 10.1016/j.bmcl.2009.05.066
127029632 137781 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3cccc(OCc4ccc(Cl)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
CHEMBL3771133 137781 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [125I]-MCH (4 to19 residues) from human MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 405 5 0 5 4.9 Cc1c(C2CC2)nc2ccc(-n3cccc(OCc4ccc(Cl)cc4)c3=O)cn12 10.1021/acs.jmedchem.5b01704
44442070 154076 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 362 5 2 5 4.7 N#Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
CHEMBL399312 154076 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 362 5 2 5 4.7 N#Cc1cc(N[C@H]2CCC[C@H](NCc3ccsc3)C2)nc2ccccc12 10.1016/j.bmcl.2007.05.034
11520239 3562 4 None 2 4 Human 9.7 pKd = 9.7 Binding
Binding affinity to human MCHR1 expressed in COS7 cellsBinding affinity to human MCHR1 expressed in COS7 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmc.2012.07.051
1313 3562 4 None 2 4 Human 9.7 pKd = 9.7 Binding
Binding affinity to human MCHR1 expressed in COS7 cellsBinding affinity to human MCHR1 expressed in COS7 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmc.2012.07.051
CHEMBL185271 3562 4 None 2 4 Human 9.7 pKd = 9.7 Binding
Binding affinity to human MCHR1 expressed in COS7 cellsBinding affinity to human MCHR1 expressed in COS7 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1016/j.bmc.2012.07.051
45273336 194079 0 None 1 3 Human 10.5 pKi = 10.5 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
91934329 194079 0 None 1 3 Human 10.5 pKi = 10.5 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL557629 194079 0 None 1 3 Human 10.5 pKi = 10.5 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
45273336 194079 0 None -1 3 Mouse 10.3 pKi = 10.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
91934329 194079 0 None -1 3 Mouse 10.3 pKi = 10.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL557629 194079 0 None -1 3 Mouse 10.3 pKi = 10.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 2419 58 33 31 -3.5 CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O 10.1016/j.bmcl.2009.03.102
9915039 60483 0 None - 1 Human 9.8 pKi = 9.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 7 2 3 7.1 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL176219 60483 0 None - 1 Human 9.8 pKi = 9.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 7 2 3 7.1 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(CC4CC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
10258364 193106 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of proteinBinding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of protein
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 193106 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of proteinBinding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of protein
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 193106 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of proteinBinding affinity to human MCH1R expressed in CHO cells by scintillation counting per mg of protein
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
11520239 3562 4 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060381c
1313 3562 4 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060381c
CHEMBL185271 3562 4 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060381c
11520239 3562 4 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060383x
1313 3562 4 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060383x
CHEMBL185271 3562 4 None -2 4 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm060383x
45279585 123053 0 None 1 2 Rat 9.5 pKi = 9.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 420 4 1 7 3.0 CNC1CCN(c2ccc(-n3cnn4cc(-c5ccc(Cl)cc5)cc4c3=O)cn2)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618330 123053 0 None 1 2 Rat 9.5 pKi = 9.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 420 4 1 7 3.0 CNC1CCN(c2ccc(-n3cnn4cc(-c5ccc(Cl)cc5)cc4c3=O)cn2)C1 10.1016/j.bmcl.2015.09.018
10118862 60463 0 None - 1 Human 9.5 pKi = 9.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 520 7 2 3 7.1 CCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL176159 60463 0 None - 1 Human 9.5 pKi = 9.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 520 7 2 3 7.1 CCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
4033 1860 42 None 8 3 Rat 9.5 pKi = 9.5 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
9826520 1860 42 None 8 3 Rat 9.5 pKi = 9.5 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
CHEMBL214957 1860 42 None 8 3 Rat 9.5 pKi = 9.5 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2015.05.008
45279585 123053 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 420 4 1 7 3.0 CNC1CCN(c2ccc(-n3cnn4cc(-c5ccc(Cl)cc5)cc4c3=O)cn2)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618330 123053 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 420 4 1 7 3.0 CNC1CCN(c2ccc(-n3cnn4cc(-c5ccc(Cl)cc5)cc4c3=O)cn2)C1 10.1016/j.bmcl.2015.09.018
45279490 123047 0 None 1 2 Rat 9.4 pKi = 9.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 464 7 0 7 4.3 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618324 123047 0 None 1 2 Rat 9.4 pKi = 9.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 464 7 0 7 4.3 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
10230490 62834 0 None - 1 Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 536 8 2 4 6.3 COCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL178997 62834 0 None - 1 Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 536 8 2 4 6.3 COCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10258364 193106 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 193106 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 193106 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
10118863 60479 0 None - 1 Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 520 6 2 3 7.1 CC(C)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL176208 60479 0 None - 1 Human 9.4 pKi = 9.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 520 6 2 3 7.1 CC(C)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44455336 95132 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 476 5 1 6 4.3 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)c(F)cc21 10.1016/j.bmcl.2008.01.010
CHEMBL257733 95132 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 476 5 1 6 4.3 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)c(F)cc21 10.1016/j.bmcl.2008.01.010
45279490 123047 0 None -1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 464 7 0 7 4.3 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618324 123047 0 None -1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 464 7 0 7 4.3 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
45278579 123048 0 None 1 2 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618325 123048 0 None 1 2 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
10258364 193106 0 None -1 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538424 193106 0 None -1 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
CHEMBL538425 193106 0 None -1 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1RDisplacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from mouse MCH1R
ChEMBL 622 9 0 6 3.0 CCN(CCCN1CCC2(CC1)OCc1ccc(F)cc12)C(=O)C(c1ccc(F)c(F)c1)N1CCN(S(C)(=O)=O)CC1=O 10.1016/j.bmcl.2009.03.102
16043291 79568 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 441 5 0 6 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL212758 79568 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 441 5 0 6 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
10004545 74588 4 None 1862 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
CHEMBL2032049 74588 4 None 1862 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 462 4 2 2 6.2 C[C@H]1c2c([nH]c3ccc(C(F)(F)F)cc23)C[C@H]2CCN(CCC3(C(=O)O)CCCCC3)C[C@@H]21 10.1016/j.bmcl.2012.04.006
10324628 141681 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 527 10 3 4 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL388440 141681 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 527 10 3 4 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(O)(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
16756072 166798 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 547 10 2 3 6.4 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL429464 166798 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 547 10 2 3 6.4 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm060381c
10209344 122725 0 None - 1 Human 9.2 pKi = 9.2 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 546 6 2 3 7.6 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL361392 122725 0 None - 1 Human 9.2 pKi = 9.2 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 546 6 2 3 7.6 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
44416651 79972 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 536 6 1 4 5.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214513 79972 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 536 6 1 4 5.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416651 79972 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 536 6 1 4 5.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214513 79972 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 536 6 1 4 5.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
45278579 123048 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618325 123048 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
46188603 121237 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 408 4 1 6 2.9 CN[C@H]1CCN(c2ccc(N3Cc4cn(-c5ccc(Cl)cc5)nc4C3=O)cn2)C1 10.1016/j.bmcl.2015.05.008
CHEMBL3589145 121237 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Antagonist activity at rat MCHR1Antagonist activity at rat MCHR1
ChEMBL 408 4 1 6 2.9 CN[C@H]1CCN(c2ccc(N3Cc4cn(-c5ccc(Cl)cc5)nc4C3=O)cn2)C1 10.1016/j.bmcl.2015.05.008
45279869 123057 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 462 4 1 8 2.5 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(N3CC(O)C3)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618334 123057 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 462 4 1 8 2.5 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(N3CC(O)C3)C2)nc1 10.1016/j.bmcl.2015.09.018
10204151 165324 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1ccc(F)c(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL424961 165324 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1ccc(F)c(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
10114686 60231 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1cc(F)cc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL175993 60231 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 448 8 2 3 5.4 CN(C)CCC(CNC(=O)Nc1cc(F)cc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44416671 141296 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 538 6 1 5 5.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL386454 141296 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 538 6 1 5 5.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
10186594 167985 0 None - 1 Human 9.0 pKi = 9.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 526 5 2 3 6.7 CN1CCC(CNC(=O)Nc2ccc(Cl)c(C(F)(F)F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL435708 167985 0 None - 1 Human 9.0 pKi = 9.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 526 5 2 3 6.7 CN1CCC(CNC(=O)Nc2ccc(Cl)c(C(F)(F)F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10226765 122607 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2006.12.080
CHEMBL361215 122607 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2006.12.080
10226765 122607 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL361215 122607 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 464 8 2 3 5.9 CN(C)CCC(CNC(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44416671 141296 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 538 6 1 5 5.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL386454 141296 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 538 6 1 5 5.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430458 142267 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 511 4 0 6 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL389295 142267 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 511 4 0 6 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC2)C1 10.1016/j.bmcl.2007.02.012
11719447 66633 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL186827 66633 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44397114 127015 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 474 4 0 4 4.3 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(Cl)c1 10.1016/j.bmcl.2005.05.015
CHEMBL366309 127015 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 474 4 0 4 4.3 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(Cl)c1 10.1016/j.bmcl.2005.05.015
11640865 77402 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 4 0 6 4.2 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL209110 77402 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 4 0 6 4.2 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
11532402 138753 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 4 0 6 4.2 CN(C)[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL379189 138753 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 4 0 6 4.2 CN(C)[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
10204047 60180 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 446 8 2 3 5.7 CN(C)CCC(CNC(=O)Nc1cccc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL175709 60180 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 446 8 2 3 5.7 CN(C)CCC(CNC(=O)Nc1cccc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
10231341 63001 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 560 6 2 3 8.0 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL179437 63001 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 560 6 2 3 8.0 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCCCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
11582824 77724 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 4 1 6 3.9 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL210191 77724 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 4 1 6 3.9 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
44424218 165481 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 541 7 2 5 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL425654 165481 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 541 7 2 5 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
52948857 18960 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CCC3(c4ccc(C#N)cc4)CC23)CC1 10.1016/j.bmcl.2010.09.037
CHEMBL1289614 18960 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)C2CCC3(c4ccc(C#N)cc4)CC23)CC1 10.1016/j.bmcl.2010.09.037
10113523 129281 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1cccc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL367532 129281 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1cccc(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
11661999 77124 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 433 5 1 8 3.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(OC)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL208720 77124 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 433 5 1 8 3.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(OC)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
10117415 60484 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 492 5 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL176220 60484 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 492 5 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10298251 130840 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 460 5 2 3 5.3 CN1CCC(CNC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL368888 130840 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 460 5 2 3 5.3 CN1CCC(CNC(=O)Nc2ccc(F)c(F)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44414520 79846 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213932 79846 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
45279869 123057 0 None -1 2 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 462 4 1 8 2.5 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(N3CC(O)C3)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618334 123057 0 None -1 2 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 462 4 1 8 2.5 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(N3CC(O)C3)C2)nc1 10.1016/j.bmcl.2015.09.018
45279867 123072 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 425 6 1 7 3.6 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618363 123072 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 425 6 1 7 3.6 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)O 10.1016/j.bmcl.2015.09.018
10369833 92121 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 533 10 2 3 6.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1 10.1021/jm060381c
CHEMBL243338 92121 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 533 10 2 3 6.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1 10.1021/jm060381c
10161039 60196 0 None - 1 Human 8.8 pKi = 8.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 449 5 2 4 4.9 CN1CCC(CNC(=O)Nc2cccc(C#N)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL175815 60196 0 None - 1 Human 8.8 pKi = 8.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 449 5 2 4 4.9 CN1CCC(CNC(=O)Nc2cccc(C#N)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
11307645 81702 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 571 6 1 5 5.7 CS(=O)(=O)N1CCC(CN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216681 81702 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 571 6 1 5 5.7 CS(=O)(=O)N1CCC(CN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
11582825 78164 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 4 1 6 3.9 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL211223 78164 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 4 1 6 3.9 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
45279148 123063 0 None 1 2 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 517 9 1 9 3.0 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618340 123063 0 None 1 2 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 517 9 1 9 3.0 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
44416800 96381 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 494 6 1 4 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL265255 96381 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 494 6 1 4 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416911 168794 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 5 1 4 5.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL442064 168794 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 5 1 4 5.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416911 168794 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 5 1 4 5.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL442064 168794 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 5 1 4 5.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44413240 79392 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 486 5 1 7 4.3 O=c1c2ccc(-c3ccc(Cl)cc3)cc2cnn1-c1ccc(N2CC[C@H](NN3CCCC3)C2)nc1 10.1021/jm051263c
CHEMBL212053 79392 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 486 5 1 7 4.3 O=c1c2ccc(-c3ccc(Cl)cc3)cc2cnn1-c1ccc(N2CC[C@H](NN3CCCC3)C2)nc1 10.1021/jm051263c
44414497 178555 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL472083 178555 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL534717 178555 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)[C@@H]1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424212 85312 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 529 9 2 5 5.3 CC(C)N(CCO)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229113 85312 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 529 9 2 5 5.3 CC(C)N(CCO)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
44424213 85316 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 543 9 2 5 5.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.bmc.2007.05.068
CHEMBL229171 85316 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 543 9 2 5 5.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.bmc.2007.05.068
10174940 140548 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 542 8 1 3 6.9 N#Cc1cccc([C@]23CC[C@@H](N(CCCCN4CCCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL382668 140548 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 542 8 1 3 6.9 N#Cc1cccc([C@]23CC[C@@H](N(CCCCN4CCCCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
10301472 124123 0 None - 1 Human 8.8 pKi = 8.8 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 516 5 1 3 7.5 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL364162 124123 0 None - 1 Human 8.8 pKi = 8.8 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 516 5 1 3 7.5 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
11519451 139673 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 536 7 1 3 5.6 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(F)cc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL380509 139673 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 536 7 1 3 5.6 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(F)cc4)C[C@H]23)CC1 10.1021/jm050886n
11635674 200154 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607121 200154 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
45279402 123059 0 None 1 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618336 123059 0 None 1 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
10437982 92125 1 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 569 10 2 3 6.4 CC(C)C(=O)Nc1cc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(F)cc1F 10.1021/jm060381c
CHEMBL243355 92125 1 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 569 10 2 3 6.4 CC(C)C(=O)Nc1cc(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(F)cc1F 10.1021/jm060381c
10183297 92867 0 None 109 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL245231 92867 0 None 109 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 464 7 1 3 6.7 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)c1 10.1021/jm060383x
11168186 67671 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm0503852
CHEMBL191393 67671 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm0503852
44416859 140983 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 5 1 6 5.1 CN(C(=O)c1ccc(-c2ccc3c(c2)OCCO3)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL384622 140983 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 5 1 6 5.1 CN(C(=O)c1ccc(-c2ccc3c(c2)OCCO3)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
11612046 77416 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 5 1 6 4.3 CCN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL209172 77416 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 445 5 1 6 4.3 CCN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
11532214 138093 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 437 4 1 7 4.0 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL377588 138093 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 437 4 1 7 4.0 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(Cl)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44424215 136648 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 485 7 2 4 5.6 CC(C)NCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL374844 136648 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 485 7 2 4 5.6 CC(C)NCCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
16755871 92049 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 497 10 2 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243138 92049 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 497 10 2 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
16755870 143941 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 483 9 2 3 5.4 CC(C)C(=O)Nc1cccc(C2CCN(CCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL390679 143941 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 483 9 2 3 5.4 CC(C)C(=O)Nc1cccc(C2CCN(CCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
16756284 150942 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 521 9 2 3 6.3 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCCC2)CC1 10.1021/jm060381c
CHEMBL396234 150942 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 521 9 2 3 6.3 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCCC2)CC1 10.1021/jm060381c
11168831 123505 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 550 5 1 3 7.8 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(C(F)(F)F)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL363044 123505 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 550 5 1 3 7.8 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(C(F)(F)F)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
44416859 140983 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 5 1 6 5.1 CN(C(=O)c1ccc(-c2ccc3c(c2)OCCO3)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL384622 140983 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 5 1 6 5.1 CN(C(=O)c1ccc(-c2ccc3c(c2)OCCO3)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416670 141380 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 9 1 5 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL387013 141380 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 9 1 5 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
49869631 127566 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665347 127566 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CCNCC2 nan
58093389 127599 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 0 4 3.6 CN1CCCc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc3n2C)C1 nan
CHEMBL3665379 127599 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 0 4 3.6 CN1CCCc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc3n2C)C1 nan
49870047 127625 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 433 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665404 127625 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 433 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CCNCC2 nan
49868914 129269 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCCC1C2 nan
CHEMBL3675307 129269 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCCC1C2 nan
58092307 129278 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 4 0 6 4.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675316 129278 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 4 0 6 4.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)C1CCCN1CC2 nan
44424062 85419 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(F)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229791 85419 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(F)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44455368 95173 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 511 5 1 5 5.0 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257906 95173 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 511 5 1 5 5.0 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44416970 79903 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 462 6 1 3 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214227 79903 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 462 6 1 3 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416969 80085 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 468 6 1 4 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214774 80085 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 468 6 1 4 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416898 140921 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 512 6 1 6 3.5 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384282 140921 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 512 6 1 6 3.5 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
11719647 138365 0 None - 1 Rat 8.0 pKi = 8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 465 4 1 6 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL378309 138365 0 None - 1 Rat 8.0 pKi = 8 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 465 4 1 6 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
44414518 77541 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 459 4 0 5 5.6 Cc1cc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)ccc1Cl 10.1016/j.bmcl.2006.05.075
CHEMBL209416 77541 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 459 4 0 5 5.6 Cc1cc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)ccc1Cl 10.1016/j.bmcl.2006.05.075
44414327 79756 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 479 4 0 5 5.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213540 79756 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 479 4 0 5 5.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
9986044 80419 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 600 6 1 4 8.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215259 80419 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 600 6 1 4 8.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
16739324 149215 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 471 3 0 6 3.8 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL394823 149215 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 471 3 0 6 3.8 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44397031 126246 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccccc4Cl)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL365400 126246 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccccc4Cl)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44425810 142873 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 575 7 0 6 5.8 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cncc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389809 142873 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 575 7 0 6 5.8 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cncc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
9985634 79332 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL211746 79332 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424214 85317 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 531 9 1 4 6.3 CC(C)N(CCF)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229172 85317 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 531 9 1 4 6.3 CC(C)N(CCF)CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
11511671 140664 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL382841 140664 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N)c4)C[C@H]23)CC1 10.1021/jm050886n
16756185 149177 0 None - 1 Rat 8.0 pKi = 8 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL394793 149177 0 None - 1 Rat 8.0 pKi = 8 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
16756641 142045 0 None 12 2 Rat 8.0 pKi = 8 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL389128 142045 0 None 12 2 Rat 8.0 pKi = 8 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
49868672 127529 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665310 127529 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCNCC2 nan
49868941 127539 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 404 4 2 5 3.1 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665320 127539 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 404 4 2 5 3.1 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
49869071 127541 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 5 0 5 4.7 CC(C)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665322 127541 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 5 0 5 4.7 CC(C)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
44424195 85426 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1ccc(F)cc1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229822 85426 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1ccc(F)cc1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44415364 79407 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212135 79407 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
50903065 131290 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693989 131290 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
49869490 127560 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 6 3.6 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cn1 nan
CHEMBL3665341 127560 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 6 3.6 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cn1 nan
11752339 69041 0 None -1 2 Mouse 8.0 pKi = 8.0 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
CHEMBL193260 69041 0 None -1 2 Mouse 8.0 pKi = 8.0 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
49869347 127554 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665335 127554 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CNCCC2 nan
10053937 79823 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213835 79823 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
49869493 127564 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C(=O)NCCC2 nan
CHEMBL3665345 127564 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C(=O)NCCC2 nan
44425828 165729 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 506 6 0 5 5.2 COc1cccc(N2C(=O)N(C3CC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL427107 165729 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 506 6 0 5 5.2 COc1cccc(N2C(=O)N(C3CC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
16756405 92421 0 None 61 2 Rat 7.0 pKi = 7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 392 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)c(C)c3)CC2)c1 10.1021/jm060383x
CHEMBL244004 92421 0 None 61 2 Rat 7.0 pKi = 7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 392 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)c(C)c3)CC2)c1 10.1021/jm060383x
10139873 79681 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 466 10 0 4 6.5 COc1cc(N(C)C(=O)c2ccc(C3CCCCC3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213198 79681 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 466 10 0 4 6.5 COc1cc(N(C)C(=O)c2ccc(C3CCCCC3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
23567513 62050 0 None - 1 Human 7.0 pKi = 7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 554 8 2 3 7.0 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL177955 62050 0 None - 1 Human 7.0 pKi = 7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 554 8 2 3 7.0 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(F)c(Cl)c1 10.1016/j.bmcl.2005.05.039
44417830 80163 0 None - 1 Human 6.0 pKi = 6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1ccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)cc1OC 10.1016/j.bmcl.2006.07.053
CHEMBL215005 80163 0 None - 1 Human 6.0 pKi = 6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1ccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)cc1OC 10.1016/j.bmcl.2006.07.053
44415419 79365 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1cncc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)c1 10.1016/j.bmcl.2006.06.045
CHEMBL211934 79365 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1cncc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)c1 10.1016/j.bmcl.2006.06.045
44440593 148551 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 10 1 7 6.8 COc1cc(Nc2nc(-c3ccc(Oc4ccccc4)cc3)cs2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL394311 148551 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 10 1 7 6.8 COc1cc(Nc2nc(-c3ccc(Oc4ccccc4)cc3)cs2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44416797 80177 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 412 6 1 3 5.2 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2c(c1)CCc1ccccc1-2 10.1016/j.bmcl.2006.06.061
CHEMBL215075 80177 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 412 6 1 3 5.2 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2c(c1)CCc1ccccc1-2 10.1016/j.bmcl.2006.06.061
21101416 141345 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 475 7 0 6 5.2 COc1cc(-n2cnc3ccc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL386753 141345 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 475 7 0 6 5.2 COc1cc(-n2cnc3ccc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
12020151 193508 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL550545 193508 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 534 7 1 4 6.1 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
44440587 93201 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 447 9 2 5 5.6 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246790 93201 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 447 9 2 5 5.6 COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44389461 122097 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 7 0 3 6.2 CN(C(=O)N1CCC(N2Cc3cc(-c4ccc(C(F)(F)F)cc4)ccc3C2=O)C1)C1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL360327 122097 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 7 0 3 6.2 CN(C(=O)N1CCC(N2Cc3cc(-c4ccc(C(F)(F)F)cc4)ccc3C2=O)C1)C1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2004.12.036
44416474 79965 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 441 8 1 3 5.8 CCN(CC)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL214499 79965 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 441 8 1 3 5.8 CCN(CC)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)cc3)cccc2c1 10.1016/j.bmcl.2006.07.006
57524677 125879 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 2.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C(=O)NCC2 nan
CHEMBL3651089 125879 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 2.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C(=O)NCC2 nan
44389521 64217 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 548 6 0 6 4.4 COc1ccc(-c2ccc(C(=O)N(C)C3CCN(C(=O)N(C)C4CCN(C5CCC(C)(C)CC5)C4)C3)cc2)nn1 10.1016/j.bmcl.2004.12.036
CHEMBL181516 64217 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 548 6 0 6 4.4 COc1ccc(-c2ccc(C(=O)N(C)C3CCN(C(=O)N(C)C4CCN(C5CCC(C)(C)CC5)C4)C3)cc2)nn1 10.1016/j.bmcl.2004.12.036
57524582 125859 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 426 2 1 7 2.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)nc31)CNCC2 nan
CHEMBL3651069 125859 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 426 2 1 7 2.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)nc31)CNCC2 nan
45271219 193749 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 516 6 1 2 7.2 Cc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c(C)c1 10.1016/j.ejmech.2009.01.031
CHEMBL552292 193749 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 516 6 1 2 7.2 Cc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c(C)c1 10.1016/j.ejmech.2009.01.031
45279491 123045 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618322 123045 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
45271221 193782 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 7 1 4 5.7 Cc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL552498 193782 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 7 1 4 5.7 Cc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.ejmech.2009.01.031
12020161 193133 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 490 7 1 4 6.0 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL538968 193133 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 490 7 1 4 6.0 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2009.01.031
44416310 96197 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 586 6 1 4 7.7 N#Cc1ccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)cc1 10.1016/j.bmcl.2006.06.055
CHEMBL263771 96197 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 586 6 1 4 7.7 N#Cc1ccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)cc1 10.1016/j.bmcl.2006.06.055
44437544 151183 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 652 14 1 7 6.6 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL396448 151183 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 652 14 1 7 6.6 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437544 151183 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 652 14 1 7 6.6 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL396448 151183 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 652 14 1 7 6.6 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
23567394 60534 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL176230 60534 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2005.05.039
44415501 77576 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 554 6 1 4 5.4 Cc1ccc(CN[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)o1 10.1016/j.bmcl.2006.06.045
CHEMBL209584 77576 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 554 6 1 4 5.4 Cc1ccc(CN[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)o1 10.1016/j.bmcl.2006.06.045
44440588 93149 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 463 9 2 5 5.8 COc1cc(NC(=S)Nc2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246590 93149 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 463 9 2 5 5.8 COc1cc(NC(=S)Nc2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44389533 171860 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 574 5 1 4 5.3 CN(C(=O)c1c[nH]c(-c2ccc(C(F)(F)F)cc2)n1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL447835 171860 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 574 5 1 4 5.3 CN(C(=O)c1c[nH]c(-c2ccc(C(F)(F)F)cc2)n1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
20779413 60227 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 6 2 3 7.2 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL175964 60227 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 6 2 3 7.2 N#Cc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C4CCC4)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
20779393 123041 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 534 8 2 3 7.5 CCCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL361821 123041 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 534 8 2 3 7.5 CCCCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
49868664 129128 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 494 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673560 129128 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 494 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCC2CC1 nan
49870454 127590 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 4 1 5 5.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)cc31)CNCCC2 nan
CHEMBL3665370 127590 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 4 1 5 5.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)cc31)CNCCC2 nan
49870576 127602 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665382 127602 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CCNCC2 nan
58093397 127609 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 452 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CCNCC2 nan
CHEMBL3665389 127609 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 452 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CCNCC2 nan
58093339 127610 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 7 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665390 127610 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 7 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)nc31)CCNCC2 nan
49870706 127618 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CNCCC2 nan
CHEMBL3665398 127618 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CNCCC2 nan
49869331 129249 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCCN1CC2 nan
CHEMBL3675289 129249 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCCN1CC2 nan
44417905 82046 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL217637 82046 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 405 8 0 3 3.6 O=C1CN(CCc2ccccc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
44416970 79903 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 462 6 1 3 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214227 79903 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 462 6 1 3 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416969 80085 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 468 6 1 4 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214774 80085 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 468 6 1 4 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
11546697 76998 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 441 5 1 7 3.6 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(OC)cc5C)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL208551 76998 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 441 5 1 7 3.6 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(OC)cc5C)ccc4c3=O)cn2)C1 10.1021/jm051263c
11758076 79619 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 586 6 1 4 7.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212941 79619 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 586 6 1 4 7.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
9851676 137997 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 600 5 1 4 8.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL377519 137997 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 600 5 1 4 8.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44415364 79407 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212135 79407 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
10053937 79823 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213835 79823 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
46869326 65124 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 385 5 1 4 3.9 CN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830042 65124 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 385 5 1 4 3.9 CN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
56680482 65127 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 399 5 0 5 3.9 CN1CC(c2cn(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830045 65127 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 399 5 0 5 3.9 CN1CC(c2cn(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
44424217 85324 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 7 2 4 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229223 85324 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 7 2 4 5.5 CC1CC[C@@H](CO)N1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
44424186 165484 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 498 9 2 4 5.0 CCN(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL425664 165484 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 498 9 2 4 5.0 CCN(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
52942795 18963 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 389 2 1 4 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289619 18963 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 389 2 1 4 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
52941615 18979 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289722 18979 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
25205317 19106 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 434 5 0 5 5.1 O=c1cc(-c2ccc3ccccc3c2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290593 19106 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 434 5 0 5 5.1 O=c1cc(-c2ccc3ccccc3c2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
11605821 141047 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 503 7 1 5 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc([N+](=O)[O-])cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL385011 141047 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 503 7 1 5 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc([N+](=O)[O-])cc3C2)CC1 10.1016/j.bmcl.2006.12.080
11420543 67086 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 2 4 5.6 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1021/jm0503852
CHEMBL189029 67086 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 2 4 5.6 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1021/jm0503852
49869208 127548 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665329 127548 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CNCCC2 nan
25054289 18880 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 9 0 7 3.9 COC[C@H]1CCCN1CCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289054 18880 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 9 0 7 3.9 COC[C@H]1CCCN1CCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
49868940 127538 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 423 2 2 3 4.7 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665319 127538 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 423 2 2 3 4.7 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
11785761 140856 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 522 7 1 5 5.3 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL383976 140856 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 522 7 1 5 5.3 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
11785261 67228 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm050886n
CHEMBL190068 67228 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm050886n
57988809 80074 10 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to rat MCHR1Binding affinity to rat MCHR1
ChEMBL 504 6 1 7 5.3 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1021/acs.jmedchem.6b00676
CHEMBL2147472 80074 10 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to rat MCHR1Binding affinity to rat MCHR1
ChEMBL 504 6 1 7 5.3 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1021/acs.jmedchem.6b00676
49869775 127569 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 0 5 3.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665350 127569 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 0 5 3.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
49868805 127531 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665312 127531 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
49869488 127544 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCCNC2 nan
CHEMBL3665325 127544 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCCNC2 nan
50902183 124092 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640814 124092 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)C1CCC(C2)N1 nan
44416840 141306 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 515 5 0 7 5.1 CN1CCN(Cc2cnc3c(Cn4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
CHEMBL386507 141306 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 515 5 0 7 5.1 CN1CCN(Cc2cnc3c(Cn4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
44388277 62961 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 386 5 1 4 4.1 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)nc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179345 62961 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 386 5 1 4 4.1 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)nc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44415501 77576 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 554 6 1 4 5.4 Cc1ccc(CN[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)o1 10.1016/j.bmcl.2006.06.045
CHEMBL209584 77576 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 554 6 1 4 5.4 Cc1ccc(CN[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)o1 10.1016/j.bmcl.2006.06.045
44425792 85509 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 461 6 0 5 3.8 CCN1C(=O)N(Cc2ccccc2F)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)C1=O 10.1016/j.bmcl.2007.01.104
CHEMBL230082 85509 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 461 6 0 5 3.8 CCN1C(=O)N(Cc2ccccc2F)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)C1=O 10.1016/j.bmcl.2007.01.104
44388141 60163 0 None - 1 Human 5.0 pKi = 5.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 532 9 2 4 6.2 COc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL175581 60163 0 None - 1 Human 5.0 pKi = 5.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 532 9 2 4 6.2 COc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.05.039
49869916 127578 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 4 1 4 3.8 CC(=O)N1CCc2[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc3c2CC1 nan
CHEMBL3665359 127578 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 4 1 4 3.8 CC(=O)N1CCc2[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc3c2CC1 nan
11635674 200154 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607121 200154 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
1252415 154072 10 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 493 8 1 7 4.3 CCN(CC)Cc1cc(NC2=NS(=O)(=O)c3ccccc32)ccc1OC(=O)c1ccc(OC)cc1 10.1021/jm070759m
CHEMBL399302 154072 10 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 493 8 1 7 4.3 CCN(CC)Cc1cc(NC2=NS(=O)(=O)c3ccccc32)ccc1OC(=O)c1ccc(OC)cc1 10.1021/jm070759m
11238718 160935 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 593 5 1 5 7.7 CC(C)(C)OC(=O)N1CCC(CN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL412801 160935 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 593 5 1 5 7.7 CC(C)(C)OC(=O)N1CCC(CN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44414465 167801 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 583 8 2 4 6.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NC(=O)C(C)(C)C)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL434571 167801 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 583 8 2 4 6.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NC(=O)C(C)(C)C)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44416357 165508 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 567 6 1 4 7.9 O=C(CN1CCc2cc(-c3ccsc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL425791 165508 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 567 6 1 4 7.9 O=C(CN1CCc2cc(-c3ccsc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44425795 85510 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 509 6 0 5 5.0 O=C1N(c2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL230083 85510 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 509 6 0 5 5.0 O=C1N(c2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44416587 140872 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 456 6 2 5 3.9 O=C(NCc1cccc2cc(CN3CC[C@H](O)C3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
CHEMBL384079 140872 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 456 6 2 5 3.9 O=C(NCc1cccc2cc(CN3CC[C@H](O)C3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
44424263 85346 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 431 6 1 3 5.6 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccco2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229406 85346 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 431 6 1 3 5.6 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccco2)CC1 10.1016/j.bmc.2007.05.068
10311260 66911 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
CHEMBL188084 66911 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
45267849 194448 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 8 1 4 5.4 CC(CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
CHEMBL561092 194448 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 8 1 4 5.4 CC(CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
71450908 78524 0 None - 1 Human 5.9 pKi = 5.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 506 5 3 2 6.9 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc4[nH]ccc34)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL2112989 78524 0 None - 1 Human 5.9 pKi = 5.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 506 5 3 2 6.9 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc4[nH]ccc34)cc2)CC1 10.1016/j.bmcl.2005.05.085
10483604 79411 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 592 6 1 4 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)c(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212142 79411 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 592 6 1 4 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)c(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
2881764 94124 7 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 424 7 0 4 5.5 CCN(CC)CCCn1c(-c2ccc(Br)cc2)cn2c3ccccc3nc12 10.1021/jm070759m
CHEMBL251947 94124 7 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 424 7 0 4 5.5 CCN(CC)CCCn1c(-c2ccc(Br)cc2)cn2c3ccccc3nc12 10.1021/jm070759m
49870184 127580 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 4 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)cc31)CCNCC2 nan
CHEMBL3665360 127580 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 4 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)cc31)CCNCC2 nan
66886358 127594 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 2 0 6 4.2 CN1CCCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc3n2C)C1 nan
CHEMBL3665374 127594 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 2 0 6 4.2 CN1CCCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc3n2C)C1 nan
58093414 127635 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665414 127635 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)nc31)CCNCC2 nan
49869049 129247 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCCN1CC2 nan
CHEMBL3675287 129247 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCCN1CC2 nan
49869051 129248 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 494 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCCN1CC2 nan
CHEMBL3675288 129248 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 494 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCCN1CC2 nan
49870810 129257 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 449 2 1 3 5.7 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675296 129257 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 449 2 1 3 5.7 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
49868783 129259 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 447 4 1 4 4.9 O=c1cc(OCc2ccc(F)cc2F)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675298 129259 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 447 4 1 4 4.9 O=c1cc(OCc2ccc(F)cc2F)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
58092273 129275 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 426 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675313 129275 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 426 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C1CCCN1CC2 nan
66608367 124088 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 4 1 6 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3640808 124088 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 4 1 6 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
50901935 131302 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 5 0 5 5.4 CC(C)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3694007 131302 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 5 0 5 5.4 CC(C)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
44397309 67173 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL189602 67173 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)NC2CCN(C/C=C/c3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
44417861 80199 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.4 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C(C)c3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215113 80199 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.4 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C(C)c3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
44424063 141529 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3F)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL387989 141529 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3F)CC1=O)C2 10.1016/j.bmc.2006.12.028
44388293 62940 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 425 5 1 3 5.4 CN(C)C1CCN(c2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179260 62940 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 425 5 1 3 5.4 CN(C)C1CCN(c2ccc(NC(=O)C3CCC(c4ccc(Cl)cc4)CC3)cc2)C1 10.1016/j.bmcl.2005.05.130
44425832 150932 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 548 6 0 5 6.4 COc1cccc(N2C(=O)N(C3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL396221 150932 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 548 6 0 5 6.4 COc1cccc(N2C(=O)N(C3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
10257135 141107 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 6 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL385363 141107 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 6 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44424211 136647 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 514 9 1 3 6.4 CC(C)N(CCF)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL374843 136647 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 514 9 1 3 6.4 CC(C)N(CCF)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
45279680 123058 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 421 3 1 7 3.2 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(O)CC2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618335 123058 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 421 3 1 7 3.2 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(O)CC2)nc1 10.1016/j.bmcl.2015.09.018
45279871 123064 0 None 1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618341 123064 0 None 1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
45279064 123065 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OC[C@H](O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618342 123065 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OC[C@H](O)C1CC1 10.1016/j.bmcl.2015.09.018
25054804 18965 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 400 6 1 6 3.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289623 18965 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 400 6 1 6 3.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2010.09.039
49869492 127562 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 2 4 4.4 O=c1cc(-c2ccc(C(F)(F)F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
CHEMBL3665343 127562 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 2 4 4.4 O=c1cc(-c2ccc(C(F)(F)F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
49870553 129233 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
CHEMBL3675274 129233 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
10257135 141107 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 6 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL385363 141107 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 6 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
11295707 167648 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 541 5 1 2 8.8 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(Cl)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
CHEMBL433591 167648 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 541 5 1 2 8.8 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(Cl)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
44416786 79874 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 492 8 1 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)COC)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214078 79874 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 492 8 1 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)COC)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
52947616 18932 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 402 8 0 6 3.7 CN(C)CCCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289399 18932 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 402 8 0 6 3.7 CN(C)CCCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
44414368 141389 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 492 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL387055 141389 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 492 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424073 85184 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 7 0 3 3.3 O=C1CN(C(=O)Cc2ccc(F)cc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228294 85184 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 7 0 3 3.3 O=C1CN(C(=O)Cc2ccc(F)cc2)CCN1CCc1ccc(CN2CCCCC2)cc1 10.1016/j.bmc.2006.12.028
44437542 151181 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
CHEMBL396447 151181 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
44437542 151181 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
CHEMBL396447 151181 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
52947578 16849 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1OC(OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254556 16849 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 568 13 4 7 2.4 COC[C@H]1OC(OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
58092293 129882 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 463 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680177 129882 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 463 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
11610423 165455 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory concentration against human MCH-R1-stimulated [Ca2+] influxInhibitory concentration against human MCH-R1-stimulated [Ca2+] influx
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL425518 165455 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory concentration against human MCH-R1-stimulated [Ca2+] influxInhibitory concentration against human MCH-R1-stimulated [Ca2+] influx
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
23567355 62063 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccncc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL177981 62063 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccncc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
23567432 122091 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 638 8 2 3 8.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2005.05.039
CHEMBL360303 122091 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 638 8 2 3 8.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2005.05.039
49868666 129127 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673559 129127 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CN1CCC2CC1 nan
45278576 123056 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 408 3 1 8 2.2 O=c1c2cc(-c3ccc(Cl)cn3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618333 123056 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 408 3 1 8 2.2 O=c1c2cc(-c3ccc(Cl)cn3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
2729098 80069 2 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
CHEMBL214726 80069 2 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3cc(F)ccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
44417865 97727 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 387 5 1 3 4.3 CN(C)c1cccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL274102 97727 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 387 5 1 3 4.3 CN(C)c1cccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44416559 79460 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2C)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL212344 79460 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2C)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
17989356 168343 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 472 9 0 5 5.7 COc1cc(N2C(=O)c3ccc(-c4ccccc4)cc3C2=O)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL438637 168343 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 472 9 0 5 5.7 COc1cc(N2C(=O)c3ccc(-c4ccccc4)cc3C2=O)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.061
44416928 80172 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 488 7 0 6 6.2 CCN(CC)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL215040 80172 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 488 7 0 6 6.2 CCN(CC)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
52947297 19020 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 390 2 1 5 3.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cn5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290045 19020 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 390 2 1 5 3.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cn5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
44388219 62944 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 534 7 2 3 7.5 CCC(C)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL179275 62944 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 534 7 2 3 7.5 CCC(C)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
49869915 127577 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 4 3.4 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)cc31)CCNCC2 nan
CHEMBL3665358 127577 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 4 3.4 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)cc31)CCNCC2 nan
58093398 127608 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CCNCC2 nan
CHEMBL3665388 127608 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CCNCC2 nan
49870183 127622 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 420 4 1 4 2.9 Cn1c2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc31)CCNCC2 nan
CHEMBL3665401 127622 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 420 4 1 4 2.9 Cn1c2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc31)CCNCC2 nan
49869917 127623 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 0 4 3.2 CN1CCc2c(n(C)c3cc(N4CCN(CCc5ccc(F)cc5)CC4=O)ccc23)CC1 nan
CHEMBL3665402 127623 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 0 4 3.2 CN1CCc2c(n(C)c3cc(N4CCN(CCc5ccc(F)cc5)CC4=O)ccc23)CC1 nan
49869186 129251 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 440 4 0 6 4.3 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCC53)c(=O)c2)cn1 nan
CHEMBL3675290 129251 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 440 4 0 6 4.3 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCC53)c(=O)c2)cn1 nan
CHEMBL4115718 211147 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44417855 80966 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 392 5 1 3 4.4 COc1cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)ccc1F 10.1016/j.bmcl.2006.07.053
CHEMBL215934 80966 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 392 5 1 3 4.4 COc1cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)ccc1F 10.1016/j.bmcl.2006.07.053
44414319 141317 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 524 7 1 4 5.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccsc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL386552 141317 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 524 7 1 4 5.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccsc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44414392 79773 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 5 0 6 4.9 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213642 79773 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 5 0 6 4.9 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
10347754 82032 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 5 1 4 6.9 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL217581 82032 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 5 1 4 6.9 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44388289 62744 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 413 8 1 4 4.5 CN(C)C1CCN(c2ccc(NC(=O)CCCC(=O)c3ccc(Cl)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178882 62744 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 413 8 1 4 4.5 CN(C)C1CCN(c2ccc(NC(=O)CCCC(=O)c3ccc(Cl)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44425809 96661 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cncc(-c2ccc(CN3CCC4(CC3)C(=O)N(c3cccc(OC)c3)C(=O)N4Cc3ccccc3F)cc2)c1 10.1016/j.bmcl.2007.01.104
CHEMBL267690 96661 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cncc(-c2ccc(CN3CCC4(CC3)C(=O)N(c3cccc(OC)c3)C(=O)N4Cc3ccccc3F)cc2)c1 10.1016/j.bmcl.2007.01.104
44415389 80929 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 5 1 3 5.9 CC1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL215920 80929 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 5 1 3 5.9 CC1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44424253 85328 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 10 1 3 7.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN(C)C)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229230 85328 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 10 1 3 7.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN(C)C)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11634329 141756 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL388524 141756 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 477 7 2 5 5.0 NCc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
10238912 75612 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 2 4 4.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL205397 75612 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 2 4 4.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
11627316 140018 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 490 7 1 4 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccsc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL381162 140018 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 490 7 1 4 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccsc4)C[C@H]23)CC1 10.1021/jm050886n
10312052 140776 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 568 8 1 4 6.0 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(OC(F)(F)F)cc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL383432 140776 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 568 8 1 4 6.0 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(OC(F)(F)F)cc4)C[C@H]23)CC1 10.1021/jm050886n
58423512 123051 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618328 123051 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
45279871 123064 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618341 123064 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
45278578 123069 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 441 6 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618346 123069 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 441 6 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
58423512 123051 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618328 123051 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
25205152 19129 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 5 0 6 4.4 Cn1c(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)cc2ccccc21 10.1016/j.bmcl.2010.09.037
CHEMBL1290712 19129 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 5 0 6 4.4 Cn1c(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)cc2ccccc21 10.1016/j.bmcl.2010.09.037
44415389 80929 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 5 1 3 5.9 CC1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL215920 80929 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 5 1 3 5.9 CC1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
49868938 127536 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.5 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(F)cn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665317 127536 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.5 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(F)cn5)cc4=O)cc31)CCNCC2 nan
50903067 131293 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693992 131293 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
49868676 127542 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 5 0 6 4.3 CC(C)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc23)CC1 nan
CHEMBL3665323 127542 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 5 0 6 4.3 CC(C)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc23)CC1 nan
11489588 80445 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 539 8 1 5 5.6 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C=O)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL215277 80445 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 539 8 1 5 5.6 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C=O)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44388427 62997 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 462 7 1 4 5.7 CN(Cc1ccccn1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179417 62997 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 462 7 1 4 5.7 CN(Cc1ccccn1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
23567283 62920 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2Cl)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL179152 62920 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2Cl)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
11656728 81846 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 536 7 1 5 3.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(S(C)(=O)=O)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL217114 81846 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 536 7 1 5 3.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(S(C)(=O)=O)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
49868674 127532 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665313 127532 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
50901934 131301 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 4 0 5 4.5 CC(=O)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3694006 131301 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 453 4 0 5 4.5 CC(=O)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
44424166 85478 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 444 6 2 4 4.0 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229929 85478 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 444 6 2 4 4.0 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44417833 81738 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.5 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C[C@H]2C)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216964 81738 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.5 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C[C@H]2C)c1 10.1016/j.bmcl.2006.07.053
45272120 194784 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 469 7 0 5 5.2 O=C(Cc1ccc2c(c1)CCO2)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL563223 194784 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 469 7 0 5 5.2 O=C(Cc1ccc2c(c1)CCO2)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
44416833 141051 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 569 6 1 4 7.6 N#Cc1cccc(-c2ccc3c(c2)CCN(Cc2nc4cc(Cl)c(Cl)cc4[nH]2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL385038 141051 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 569 6 1 4 7.6 N#Cc1cccc(-c2ccc3c(c2)CCN(Cc2nc4cc(Cl)c(Cl)cc4[nH]2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44424174 85363 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 488 6 2 6 3.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc5c(c4)OCO5)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229556 85363 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 488 6 2 6 3.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc5c(c4)OCO5)CC2C3)c1 10.1016/j.bmc.2007.05.068
23567477 60171 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL175653 60171 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
44417881 79973 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 408 6 1 4 3.7 COc1cc(OC)cc(C(=O)NC2CCN(CC3CCc4ccccc4C3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214516 79973 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 408 6 1 4 3.7 COc1cc(OC)cc(C(=O)NC2CCN(CC3CCc4ccccc4C3)CC2)c1 10.1016/j.bmcl.2006.07.053
44416839 80688 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 531 7 0 7 4.9 CN(CC(=O)N(C)C)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL215635 80688 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 531 7 0 7 4.9 CN(CC(=O)N(C)C)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
49868937 127535 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 2 4 4.1 O=c1cc(-c2ccc(C(F)(F)F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665316 127535 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 2 4 4.1 O=c1cc(-c2ccc(C(F)(F)F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
44414522 96397 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 457 6 0 7 4.8 COc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL265365 96397 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 457 6 0 7 4.8 COc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
10436862 79408 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 524 6 1 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)cc2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212136 79408 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 524 6 1 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)cc2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
10347753 80208 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 6 1 4 6.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)c(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215118 80208 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 6 1 4 6.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(Cl)c(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
45271246 193527 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 406 7 1 4 4.0 O=C(NCC1CC1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL550683 193527 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 406 7 1 4 4.0 O=C(NCC1CC1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
44414651 136694 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 633 10 2 5 6.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(NC(=O)OCc5ccccc5)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL375132 136694 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 633 10 2 5 6.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(NC(=O)OCc5ccccc5)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
11340894 134054 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 1 4 6.7 COc1ccc(NC(=O)N(c2ccc(-c3cccc(C#N)c3)cc2)C2CCN(C3CCCC3)CC2)cc1 10.1021/jm0503852
CHEMBL371809 134054 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 1 4 6.7 COc1ccc(NC(=O)N(c2ccc(-c3cccc(C#N)c3)cc2)C2CCN(C3CCCC3)CC2)cc1 10.1021/jm0503852
49870457 127600 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 474 5 0 4 4.5 Cn1c2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc31)CN(C1CCC1)CCC2 nan
CHEMBL3665380 127600 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 474 5 0 4 4.5 Cn1c2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc31)CN(C1CCC1)CCC2 nan
49870809 129256 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 430 4 1 5 4.1 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675295 129256 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 430 4 1 5 4.1 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
49868781 129271 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 430 4 1 5 4.0 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675309 129271 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 430 4 1 5 4.0 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
49868782 129272 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 450 2 1 4 4.9 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675310 129272 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 450 2 1 4 4.9 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
50902181 124095 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 464 4 1 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640817 124095 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 464 4 1 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)C1CCC(C2)N1 nan
50903066 131292 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693991 131292 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL4115726 211148 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44416786 79874 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 492 8 1 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)COC)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214078 79874 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 492 8 1 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)COC)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
11641550 139190 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 482 4 0 7 3.9 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)n(C)c4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL379829 139190 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 482 4 0 7 3.9 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)n(C)c4c3=O)cn2)C1 10.1021/jm051263c
71714121 122021 3 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH-R1 expressed in CHO/Galpha16 cellsBinding affinity to human MCH-R1 expressed in CHO/Galpha16 cells
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
CHEMBL3601377 122021 3 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH-R1 expressed in CHO/Galpha16 cellsBinding affinity to human MCH-R1 expressed in CHO/Galpha16 cells
ChEMBL 422 9 0 8 2.5 COc1ccc(COc2cnn(CC(=O)c3ccc(CN(C)C)cc3C)c(=O)c2)nc1 10.1016/j.bmcl.2015.05.065
44414357 79328 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 479 4 0 5 6.0 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5Cl)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL211736 79328 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 479 4 0 5 6.0 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5Cl)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44430493 86567 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 521 4 0 7 4.0 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL232438 86567 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 521 4 0 7 4.0 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
44430500 86778 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 585 6 0 8 4.7 CCOc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(Cl)c1 10.1016/j.bmcl.2007.02.012
CHEMBL232835 86778 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 585 6 0 8 4.7 CCOc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(Cl)c1 10.1016/j.bmcl.2007.02.012
9986014 141288 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 598 7 1 5 7.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(Cc3ccoc3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL386411 141288 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 598 7 1 5 7.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(Cc3ccoc3)CC2)c1 10.1016/j.bmcl.2006.06.055
44388294 63526 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 391 5 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)C3CCC(c4ccccc4)CC3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL180364 63526 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 391 5 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)C3CCC(c4ccccc4)CC3)cc2)C1 10.1016/j.bmcl.2005.05.130
44397302 66592 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL186642 66592 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44415461 79876 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 654 8 0 3 7.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214103 79876 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 654 8 0 3 7.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415524 140672 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL382851 140672 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44389404 121950 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 676 8 0 5 5.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCS(=O)(=O)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL360102 121950 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 676 8 0 5 5.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCS(=O)(=O)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
45279772 123054 0 None 1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 393 3 1 7 2.4 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC(O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618331 123054 0 None 1 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 393 3 1 7 2.4 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC(O)C2)nc1 10.1016/j.bmcl.2015.09.018
52941152 18980 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 3 1 5 3.7 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
CHEMBL1289723 18980 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 3 1 5 3.7 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
52947251 18994 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 2 0 4 5.3 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(Cl)cc5Cl)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289830 18994 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 2 0 4 5.3 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(Cl)cc5Cl)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
52941195 19006 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 3 1 5 4.0 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)c(C)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289946 19006 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 3 1 5 4.0 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)c(C)c1 10.1016/j.bmcl.2010.09.122
25017298 19094 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 492 5 0 6 6.0 O=c1c2cc(-c3ccc(Cl)cc3Cl)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290493 19094 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 492 5 0 6 6.0 O=c1c2cc(-c3ccc(Cl)cc3Cl)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
16755970 91868 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 525 11 2 3 6.4 CCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
CHEMBL242901 91868 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 525 11 2 3 6.4 CCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
44415524 140672 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL382851 140672 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
11467626 159249 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 610 9 1 6 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCOCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL410566 159249 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 610 9 1 6 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCOCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
49868803 127528 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665309 127528 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CCNCC2 nan
44415461 79876 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 654 8 0 3 7.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214103 79876 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 654 8 0 3 7.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
49869073 127545 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCCNC2 nan
CHEMBL3665326 127545 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCCNC2 nan
49870553 129233 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
CHEMBL3675274 129233 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
44388263 165227 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 492 5 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)ccc2Cl)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL424784 165227 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 492 5 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)ccc2Cl)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
16756640 92833 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cc(Cl)cc(Cl)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL245008 92833 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cc(Cl)cc(Cl)c4)c3)CC2)c1 10.1021/jm060383x
44416475 79982 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 455 6 1 4 4.8 O=C(NCc1cccc2cc(CN3CCOCC3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
CHEMBL214547 79982 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 455 6 1 4 4.8 O=C(NCc1cccc2cc(CN3CCOCC3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
45266975 193096 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 552 6 1 2 8.1 Cc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c2ccccc12 10.1016/j.ejmech.2009.01.031
CHEMBL538211 193096 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 552 6 1 2 8.1 Cc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)c2ccccc12 10.1016/j.ejmech.2009.01.031
44417876 141178 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 407 6 1 5 3.6 COc1cc(OC)cc(C(=O)NC2CCN(Cc3cc4ccccc4n3C)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL385743 141178 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 407 6 1 5 3.6 COc1cc(OC)cc(C(=O)NC2CCN(Cc3cc4ccccc4n3C)CC2)c1 10.1016/j.bmcl.2006.07.053
44416737 80068 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 455 6 2 4 4.5 O=C(NCc1cccc2cc(CN3CC[C@H](O)C3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
CHEMBL214717 80068 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 455 6 2 4 4.5 O=C(NCc1cccc2cc(CN3CC[C@H](O)C3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
44424203 165486 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 528 9 2 3 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C(N)=O)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL425669 165486 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 528 9 2 3 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C(N)=O)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44389484 62628 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 393 7 0 3 3.4 CN1CCC(N(C)C(=O)CCCN(C)C(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178515 62628 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 393 7 0 3 3.4 CN1CCC(N(C)C(=O)CCCN(C)C(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2004.12.036
44430490 86373 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 495 3 0 8 2.9 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc6c(c5)OCCO6)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232231 86373 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 495 3 0 8 2.9 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc6c(c5)OCCO6)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44437612 91110 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240537 91110 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
44437612 91110 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240537 91110 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
44437558 91306 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240940 91306 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
44437558 91306 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240940 91306 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
44437612 91110 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240537 91110 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
44437558 91306 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240940 91306 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
44437612 91110 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240537 91110 0 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
44437558 91306 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240940 91306 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 2 3 6.2 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
44437495 91454 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241376 91454 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2007.02.049
44437495 91454 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241376 91454 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2010.09.014
44437495 91454 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241376 91454 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2007.02.049
44437495 91454 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241376 91454 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccc(-c2ccc(CNC(=O)NC3CCN(Cc4ccc(C)cc4)CC3)cc2)cc1 10.1016/j.bmc.2010.09.014
44424260 85337 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 443 6 1 4 4.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cncnc2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229348 85337 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 443 6 1 4 4.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cncnc2)CC1 10.1016/j.bmc.2007.05.068
49868936 127534 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 2 5 3.5 O=c1cc(-c2ccc(C(F)(F)F)nn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665315 127534 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 2 5 3.5 O=c1cc(-c2ccc(C(F)(F)F)nn2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
49870051 127629 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 432 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C(=O)NCCC2 nan
CHEMBL3665408 127629 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 432 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C(=O)NCCC2 nan
45267827 194551 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 518 7 1 3 6.6 COc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL561694 194551 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 518 7 1 3 6.6 COc1ccc(CN2CCC(=Cc3ccc(C(=O)N[C@H](C)c4ccc(Br)cc4)cc3)CC2)cc1 10.1016/j.ejmech.2009.01.031
44437609 90516 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239468 90516 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437609 90516 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239468 90516 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437609 90516 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239468 90516 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437609 90516 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239468 90516 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 561 12 3 4 5.7 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
49868668 129130 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 462 4 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CN1CCC2CC1 nan
CHEMBL3673562 129130 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 462 4 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CN1CCC2CC1 nan
58079421 129131 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CN1CCC2CC1 nan
CHEMBL3673563 129131 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CN1CCC2CC1 nan
66873457 127614 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665394 127614 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCCC2 nan
66873578 127616 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665396 127616 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCCC2 nan
57524507 125858 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 405 4 1 7 2.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCC2 nan
CHEMBL3651068 125858 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 405 4 1 7 2.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCC2 nan
57524583 125860 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCC2 nan
CHEMBL3651070 125860 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCC2 nan
66603668 129280 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675318 129280 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL4115747 211155 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44414606 96273 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 573 7 2 4 4.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5c(c4)CC(=O)N5)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL264350 96273 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 573 7 2 4 4.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5c(c4)CC(=O)N5)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
10348080 79375 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 6 1 4 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL211984 79375 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 6 1 4 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
10347752 80668 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 6 1 4 6.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215567 80668 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 558 6 1 4 6.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44430482 87921 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 451 3 0 6 3.4 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL234930 87921 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 451 3 0 6 3.4 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
44424171 85360 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cc(F)cc(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229505 85360 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cc(F)cc(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424179 85368 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC[C@@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229609 85368 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC[C@@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424182 85380 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 7 2 4 5.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCC(CO)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229664 85380 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 7 2 4 5.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCC(CO)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424255 141806 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 590 8 1 4 5.6 CN(C)Cc1cccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL388723 141806 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 590 8 1 4 5.6 CN(C)Cc1cccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424181 142234 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 508 6 1 3 6.6 CC1CCCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL389274 142234 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 508 6 1 3 6.6 CC1CCCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
44424185 168391 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 508 6 1 3 6.6 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCCCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL439013 168391 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 508 6 1 3 6.6 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCCCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44409479 74653 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 1 3 5.9 N#Cc1cccc([C@@]23CC[C@H](N(CCN4CCCC4)C(=O)Nc4cc(Cl)cc(Cl)c4)[C@@H]2C3)c1 10.1021/jm050886n
CHEMBL203388 74653 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 1 3 5.9 N#Cc1cccc([C@@]23CC[C@H](N(CCN4CCCC4)C(=O)Nc4cc(Cl)cc(Cl)c4)[C@@H]2C3)c1 10.1021/jm050886n
11699265 76364 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 518 7 1 3 5.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(Cl)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL206637 76364 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 518 7 1 3 5.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(Cl)c4)C[C@H]23)CC1 10.1021/jm050886n
45279772 123054 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 393 3 1 7 2.4 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC(O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618331 123054 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 393 3 1 7 2.4 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC(O)C2)nc1 10.1016/j.bmcl.2015.09.018
45279321 123067 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 518 9 1 10 2.4 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618344 123067 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 518 9 1 10 2.4 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
45278578 123069 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 441 6 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618346 123069 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 441 6 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
45278577 123070 0 None 1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 453 7 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618347 123070 0 None 1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 453 7 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
44194383 19092 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 355 2 1 4 3.6 Cn1c2c(c3ccc(-n4ccc(-c5ccccc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290491 19092 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 355 2 1 4 3.6 Cn1c2c(c3ccc(-n4ccc(-c5ccccc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
25205149 19004 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 418 5 0 5 4.6 O=c1cc(-c2ccc(Cl)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289941 19004 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 418 5 0 5 4.6 O=c1cc(-c2ccc(Cl)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
137640352 156242 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SNAP-7941 from recombinant human MCHR1 expressed in African green monkey COS7 cell membranesDisplacement of [3H]SNAP-7941 from recombinant human MCHR1 expressed in African green monkey COS7 cell membranes
ChEMBL 612 11 2 7 4.2 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(c3cccc(CC(C)=O)c3)CC2)C(=O)N1 10.1016/j.ejmech.2017.03.025
CHEMBL4071004 156242 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SNAP-7941 from recombinant human MCHR1 expressed in African green monkey COS7 cell membranesDisplacement of [3H]SNAP-7941 from recombinant human MCHR1 expressed in African green monkey COS7 cell membranes
ChEMBL 612 11 2 7 4.2 COCC1=C(C(=O)OC)[C@H](c2ccc(F)c(F)c2)N(C(=O)NCCCN2CCC(c3cccc(CC(C)=O)c3)CC2)C(=O)N1 10.1016/j.ejmech.2017.03.025
16072132 80002 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of binding to MCH-R1Inhibition of binding to MCH-R1
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
CHEMBL214629 80002 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of binding to MCH-R1Inhibition of binding to MCH-R1
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmcl.2006.10.052
44414464 96359 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 569 9 2 4 5.7 CC(C)C(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL265089 96359 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 569 9 2 4 5.7 CC(C)C(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
44409527 74508 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 530 6 2 4 5.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C[C@H]2C3)c1 10.1021/jm050886n
CHEMBL203166 74508 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 530 6 2 4 5.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)C[C@H]2C3)c1 10.1021/jm050886n
50903065 131290 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693989 131290 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
44417069 141369 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 7 1 5 5.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL386969 141369 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 7 1 5 5.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
17989369 141225 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 1 6 4.7 COc1cc(N2C(=O)c3ccc(Nc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL386050 141225 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 1 6 4.7 COc1cc(N2C(=O)c3ccc(Nc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
10139496 168761 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 0 4 6.1 COc1cc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL441855 168761 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 0 4 6.1 COc1cc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44397323 66794 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL187563 66794 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44425796 85662 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 523 7 0 5 5.0 O=C1N(Cc2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL231044 85662 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 523 7 0 5 5.0 O=C1N(Cc2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44425821 142878 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 606 8 1 5 6.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(NC(C)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389811 142878 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 606 8 1 5 6.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(NC(C)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44425801 85693 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 538 7 0 5 5.6 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5cccc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL231147 85693 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 538 7 0 5 5.6 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5cccc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
49870683 129244 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCCN1CC2 nan
CHEMBL3675284 129244 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCCN1CC2 nan
44430481 150609 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL395957 150609 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
20779441 63128 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 477 5 1 3 5.9 CN1CCC(CNC(=O)c2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL179869 63128 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 477 5 1 3 5.9 CN1CCC(CNC(=O)c2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
45272111 193535 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 478 6 1 3 6.2 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccco3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL550744 193535 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 478 6 1 3 6.2 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccco3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
44416585 79845 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2cccc(Cc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213923 79845 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2cccc(Cc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416389 138111 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3)c(C)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL377658 138111 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3)c(C)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
58093337 127611 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 454 5 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CCN(C1CCC1)CC2 nan
CHEMBL3665391 127611 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 454 5 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CCN(C1CCC1)CC2 nan
58092304 129277 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 462 4 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675315 129277 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 462 4 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)C1CCCN1CC2 nan
58092269 129876 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 426 4 0 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680171 129876 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 426 4 0 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CN1CCCC1C2 nan
44424061 85409 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 419 8 0 3 3.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229739 85409 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 419 8 0 3 3.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44417069 141369 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 7 1 5 5.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL386969 141369 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 7 1 5 5.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44414570 77670 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 471 6 0 7 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(OC)c1 10.1016/j.bmcl.2006.05.075
CHEMBL209905 77670 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 471 6 0 7 4.7 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(OC)c1 10.1016/j.bmcl.2006.05.075
10008279 79373 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 5 1 4 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL211978 79373 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 5 1 4 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
10100662 140884 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 638 8 1 5 8.0 COc1ccccc1CN1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL384115 140884 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 638 8 1 5 8.0 COc1ccccc1CN1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
10461033 140898 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 588 5 1 5 6.5 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCOCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL384163 140898 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 588 5 1 5 6.5 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCOCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44388303 62206 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 416 6 1 5 4.2 COc1ccc(-c2ccc(C(=O)Nc3ccc(N4CCC(N(C)C)C4)cc3)cn2)cc1 10.1016/j.bmcl.2005.05.130
CHEMBL178250 62206 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 416 6 1 5 4.2 COc1ccc(-c2ccc(C(=O)Nc3ccc(N4CCC(N(C)C)C4)cc3)cn2)cc1 10.1016/j.bmcl.2005.05.130
44397350 124891 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 464 5 0 4 3.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2005.05.015
CHEMBL364573 124891 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 464 5 0 4 3.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2005.05.015
44425834 150872 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 562 7 0 5 6.6 COc1cccc(N2C(=O)N(CC3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL396174 150872 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 562 7 0 5 6.6 COc1cccc(N2C(=O)N(CC3CCCCC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415413 137835 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 7 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC(F)(F)F)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL377208 137835 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 7 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC(F)(F)F)C2)C1 10.1016/j.bmcl.2006.06.045
44424177 141459 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 6 1 3 6.2 CC1CCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL387501 141459 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 6 1 3 6.2 CC1CCCN1CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
25206616 18777 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 470 5 0 5 5.1 O=c1cc(-c2ccc(C(F)(F)F)cc2F)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1287838 18777 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 470 5 0 5 5.1 O=c1cc(-c2ccc(C(F)(F)F)cc2F)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
50903066 131292 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693991 131292 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
44415413 137835 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 7 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC(F)(F)F)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL377208 137835 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 7 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC(F)(F)F)C2)C1 10.1016/j.bmcl.2006.06.045
11168108 79994 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 507 8 1 5 4.6 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C=O)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL214583 79994 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 507 8 1 5 4.6 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C=O)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44415483 95955 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 564 7 1 3 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL261955 95955 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 564 7 1 3 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
49869208 127548 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665329 127548 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CNCCC2 nan
11656805 141300 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 544 8 3 4 4.6 CCNC(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL386487 141300 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 544 8 3 4 4.6 CCNC(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
11648976 139793 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 497 7 1 4 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@@H](c3cccc(C#N)c3)C2)CC1 10.1021/jm050886n
CHEMBL380692 139793 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 497 7 1 4 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@@H](c3cccc(C#N)c3)C2)CC1 10.1021/jm050886n
11541231 140614 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 547 8 1 4 4.8 CS(=O)(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCCC4=O)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1021/jm050886n
CHEMBL382772 140614 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 547 8 1 4 4.8 CS(=O)(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCCC4=O)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1021/jm050886n
49870324 127583 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)nc4=O)cc31)CCNCC2 nan
CHEMBL3665363 127583 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)nc4=O)cc31)CCNCC2 nan
44388271 62633 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 491 6 1 3 5.9 CN1CCC(CNC(=O)Cc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL178549 62633 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 491 6 1 3 5.9 CN1CCC(CNC(=O)Cc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
15982955 93202 0 None 2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 9 0 6 4.9 COc1cc(N2CC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246794 93202 0 None 2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 9 0 6 4.9 COc1cc(N2CC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
23567310 167925 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 536 8 2 3 6.9 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cccc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL435329 167925 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 536 8 2 3 6.9 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cccc(Cl)c1 10.1016/j.bmcl.2005.05.039
44437614 144592 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391203 144592 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
44437614 144592 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391203 144592 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
11786476 66882 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 574 6 1 4 6.2 CCS(=O)(=O)N1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
CHEMBL187942 66882 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 574 6 1 4 6.2 CCS(=O)(=O)N1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
44437614 144592 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391203 144592 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2007.02.049
44437614 144592 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391203 144592 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 13 3 5 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2OC)cc1 10.1016/j.bmc.2010.09.014
25018075 19136 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 426 5 0 8 3.5 O=c1c2cc(-c3ncccn3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290722 19136 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 426 5 0 8 3.5 O=c1c2cc(-c3ncccn3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
44416381 79723 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 561 6 1 3 7.9 O=C(CN1CCc2cc(-c3ccccc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL213383 79723 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 561 6 1 3 7.9 O=C(CN1CCc2cc(-c3ccccc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44194482 19073 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 427 4 0 5 3.8 CC(=O)N1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1290381 19073 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 427 4 0 5 3.8 CC(=O)N1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
44417885 80178 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 0 4 4.6 COc1cc(OC)cc(C(=O)N(C)C2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215078 80178 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 0 4 4.6 COc1cc(OC)cc(C(=O)N(C)C2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44437541 145537 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391920 145537 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
44437541 145537 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391920 145537 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
49869779 127573 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)nc4=O)cc31)CCNCC2 nan
CHEMBL3665354 127573 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)nc4=O)cc31)CCNCC2 nan
58093367 127624 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 5 0 4 3.6 CCN1CCc2c(n(C)c3cc(N4CCN(CCc5ccc(F)cc5)CC4=O)ccc23)CC1 nan
CHEMBL3665403 127624 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 5 0 4 3.6 CCN1CCc2c(n(C)c3cc(N4CCN(CCc5ccc(F)cc5)CC4=O)ccc23)CC1 nan
57524675 125869 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 454 4 1 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)CNCC2 nan
CHEMBL3651079 125869 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 454 4 1 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)CNCC2 nan
66603581 129878 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680173 129878 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CN1CCCC1C2 nan
58092191 124085 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 4 3.4 Cn1c2c(c3ccc(N4CCN(CCc5ccccc5)CC4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3640805 124085 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 4 3.4 Cn1c2c(c3ccc(N4CCN(CCc5ccccc5)CC4=O)cc31)C1CCC(C2)N1 nan
50901932 131299 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 412 4 1 6 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccccn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3694004 131299 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 412 4 1 6 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccccn5)cc4=O)cc31)C1CCC(C2)N1 nan
44417862 80204 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 366 7 1 4 3.2 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215114 80204 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 366 7 1 4 3.2 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
44414650 79775 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 575 8 2 4 4.8 CNC(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
CHEMBL213649 79775 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 575 8 2 4 4.8 CNC(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
44430478 86811 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 555 5 0 7 4.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)C(C)(C)C)C1 10.1016/j.bmcl.2007.02.012
CHEMBL233027 86811 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 555 5 0 7 4.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)C(C)(C)C)C1 10.1016/j.bmcl.2007.02.012
44430452 149214 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 457 3 1 6 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCNC1 10.1016/j.bmcl.2007.02.012
CHEMBL394822 149214 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 457 3 1 6 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCNC1 10.1016/j.bmcl.2007.02.012
44430485 150899 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 505 3 0 6 4.1 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL396193 150899 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 505 3 0 6 4.1 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44415483 95955 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 564 7 1 3 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL261955 95955 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 564 7 1 3 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
11691468 168767 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 477 7 2 5 5.0 NCc1cnc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL441886 168767 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 477 7 2 5 5.0 NCc1cnc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
45278577 123070 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 453 7 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618347 123070 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 453 7 1 9 2.8 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
52947270 19005 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 3 1 5 4.3 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c4c(n(C)c3c2)CNCC4)c(=O)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289945 19005 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 3 1 5 4.3 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c4c(n(C)c3c2)CNCC4)c(=O)c1 10.1016/j.bmcl.2010.09.122
49870553 129233 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
CHEMBL3675274 129233 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCC21 nan
25054550 18995 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 442 7 0 7 3.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CC3CC2CO3)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289833 18995 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 442 7 0 7 3.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CC3CC2CO3)c1 10.1016/j.bmcl.2010.09.039
49869489 127559 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 384 2 1 5 3.7 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cn1 nan
CHEMBL3665340 127559 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 384 2 1 5 3.7 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cn1 nan
49869632 127567 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 446 5 1 5 4.2 CC(C)N1CCc2[nH]c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc3c2CC1 nan
CHEMBL3665348 127567 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 446 5 1 5 4.2 CC(C)N1CCc2[nH]c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc3c2CC1 nan
44417837 140858 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.5 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C[C@@H]2C)c1 10.1016/j.bmcl.2006.07.053
CHEMBL383981 140858 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.5 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C[C@@H]2C)c1 10.1016/j.bmcl.2006.07.053
44437541 145537 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391920 145537 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2007.02.049
44437541 145537 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391920 145537 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 657 15 1 7 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(OC)cc2)cc1 10.1016/j.bmc.2010.09.014
11445353 84703 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 456 8 1 3 6.6 Clc1ccc(-c2ccc(CNC3CCN(CC(c4ccccc4)c4ccccc4)C3)o2)cc1 10.1021/jm040084c
CHEMBL224943 84703 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 456 8 1 3 6.6 Clc1ccc(-c2ccc(CNC3CCN(CC(c4ccccc4)c4ccccc4)C3)o2)cc1 10.1021/jm040084c
3747253 94148 1 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 437 11 0 5 4.3 CCCCCCN(CS(=O)(=O)c1ccc(C)cc1)CS(=O)(=O)c1ccc(C)cc1 10.1021/jm070759m
CHEMBL252145 94148 1 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 437 11 0 5 4.3 CCCCCCN(CS(=O)(=O)c1ccc(C)cc1)CS(=O)(=O)c1ccc(C)cc1 10.1021/jm070759m
44437622 90931 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240287 90931 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437622 90931 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240287 90931 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
44437622 90931 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240287 90931 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437622 90931 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240287 90931 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 12 3 4 5.6 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
45267809 194354 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 532 6 1 4 6.3 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3cccc4c3OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL560290 194354 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 532 6 1 4 6.3 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3cccc4c3OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
49870681 129238 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cn5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675279 129238 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 2 0 5 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cn5)cc4=O)cc31)CCN1CCCCC21 nan
44440599 146162 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 455 6 2 5 4.1 O=C1N/C(=C\c2ccc(CN3CCC(O)C3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL392403 146162 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 455 6 2 5 4.1 O=C1N/C(=C\c2ccc(CN3CCC(O)C3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
49870182 127631 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)cc31)CNCCC2 nan
CHEMBL3665410 127631 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)cc31)CNCCC2 nan
44417841 81164 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216315 81164 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)c(F)c1 10.1016/j.bmcl.2006.07.053
44416782 80012 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 420 4 1 3 3.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214650 80012 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 420 4 1 3 3.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44414455 79847 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 442 5 0 7 4.1 COc1ccncc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
CHEMBL213933 79847 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 442 5 0 7 4.1 COc1ccncc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
44430498 87917 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 591 5 0 8 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(OC(F)(F)F)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL234920 87917 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 591 5 0 8 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(OC(F)(F)F)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44424246 137025 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 592 11 2 4 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CNS(C)(=O)=O)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL375465 137025 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 592 11 2 4 6.0 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CNS(C)(=O)=O)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11655701 138166 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 466 6 1 3 5.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL377955 138166 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 466 6 1 3 5.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
44389403 62682 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 628 8 0 4 6.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCOc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178810 62682 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 628 8 0 4 6.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCOc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
45278977 123052 0 None 1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618329 123052 0 None 1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
45279680 123058 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 421 3 1 7 3.2 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(O)CC2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618335 123058 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 421 3 1 7 3.2 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CCC(O)CC2)nc1 10.1016/j.bmcl.2015.09.018
16756639 92785 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)c(Cl)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244791 92785 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)c(Cl)c4)c3)CC2)c1 10.1021/jm060383x
10195667 134752 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 482 6 1 3 5.9 N#Cc1ccc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4cc(Cl)cc(Cl)c4)[C@H]2C3)cc1 10.1021/jm049035q
CHEMBL372721 134752 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 482 6 1 3 5.9 N#Cc1ccc([C@]23CC[C@@H](N(CCN4CCCC4)C(=O)Nc4cc(Cl)cc(Cl)c4)[C@H]2C3)cc1 10.1021/jm049035q
44415533 79557 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 8 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212715 79557 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 8 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415378 138792 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 1 4 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCOc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379275 138792 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 1 4 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCOc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44425827 150366 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 480 5 0 5 4.7 COc1cccc(N2C(=O)N(C)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL395763 150366 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 480 5 0 5 4.7 COc1cccc(N2C(=O)N(C)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415512 79925 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 551 6 1 4 4.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCc3ccccn3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214318 79925 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 551 6 1 4 4.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCc3ccccn3)C2)C1 10.1016/j.bmcl.2006.06.045
11504793 81144 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 536 6 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3cc(Br)ccc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL216209 81144 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 536 6 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3cc(Br)ccc3C2)CC1 10.1016/j.bmcl.2006.12.080
44397145 67035 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4cccc(C(F)(F)F)c4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL188766 67035 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4cccc(C(F)(F)F)c4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
10077022 16857 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254630 16857 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44424225 85336 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 571 5 2 3 6.1 CNC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229339 85336 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 571 5 2 3 6.1 CNC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
44415512 79925 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 551 6 1 4 4.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCc3ccccn3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214318 79925 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 551 6 1 4 4.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCc3ccccn3)C2)C1 10.1016/j.bmcl.2006.06.045
45270416 194968 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 8 1 4 5.8 CCC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
CHEMBL564409 194968 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 470 8 1 4 5.8 CCC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
44388058 165456 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 502 8 2 3 6.2 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccccc1 10.1016/j.bmcl.2005.05.039
CHEMBL425521 165456 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 502 8 2 3 6.2 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccccc1 10.1016/j.bmcl.2005.05.039
44437497 91545 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241588 91545 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437497 91545 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241588 91545 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437497 91545 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241588 91545 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437497 91545 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241588 91545 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 438 6 2 3 5.0 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44424167 141570 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4F)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL388302 141570 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccccc4F)CC2C3)c1 10.1016/j.bmc.2007.05.068
67970877 125878 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 5 0 6 3.8 CC(C)N1CCc2nc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccn3c2C1 nan
CHEMBL3651088 125878 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 5 0 6 3.8 CC(C)N1CCc2nc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccn3c2C1 nan
49868917 129254 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 454 4 0 6 4.7 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCCC53)c(=O)c2)cn1 nan
CHEMBL3675293 129254 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 454 4 0 6 4.7 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCCC53)c(=O)c2)cn1 nan
49868914 129269 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCCC1C2 nan
CHEMBL3675307 129269 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCCC1C2 nan
58092290 129273 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 463 4 1 4 5.2 O=c1cc(OCc2ccc(Cl)cc2F)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675311 129273 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 463 4 1 4 5.2 O=c1cc(OCc2ccc(Cl)cc2F)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
50902100 124097 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640819 124097 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)C1CCC(C2)N1 nan
50903067 131293 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693992 131293 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
44424069 85289 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 376 7 1 2 4.5 CN(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228987 85289 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 376 7 1 2 4.5 CN(C)Cc1ccc(CCNC(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
44424064 85420 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(Cl)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229792 85420 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(Cl)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44414499 79902 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 441 5 0 6 5.1 Cc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL214223 79902 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 441 5 0 6 5.1 Cc1ccc(Oc2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
44430496 86674 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 575 4 0 7 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(C(F)(F)F)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232634 86674 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 575 4 0 7 4.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(C(F)(F)F)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44397167 66887 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 440 4 0 4 3.6 Cc1ccccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
CHEMBL187968 66887 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 440 4 0 4 3.6 Cc1ccccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
44425825 150657 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 631 10 0 6 6.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(N(C)CCC#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL395986 150657 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 631 10 0 6 6.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(N(C)CCC#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415533 79557 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 8 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212715 79557 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 8 1 3 5.1 CN(C(=O)c1ccc(-c2ccc(F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415378 138792 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 1 4 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCOc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379275 138792 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 1 4 5.5 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCOc3ccc(F)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
25205827 19049 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 448 6 0 6 4.6 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290262 19049 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 448 6 0 6 4.6 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
11247985 67669 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 452 6 1 3 6.1 CN(C)CCN(C(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
CHEMBL191390 67669 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 452 6 1 3 6.1 CN(C)CCN(C(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
44416782 80012 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 420 4 1 3 3.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214650 80012 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 420 4 1 3 3.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44415526 80664 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL215550 80664 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416714 140910 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 550 9 1 4 6.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384234 140910 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 550 9 1 4 6.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
10300618 77960 12 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 500 10 0 4 6.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
CHEMBL2110360 77960 12 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 500 10 0 4 6.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
9954518 79603 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
CHEMBL212890 79603 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 432 10 0 4 5.4 CCN(CC)CCOc1ccc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
10225681 79913 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3cc(-c4ccccc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL214276 79913 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3cc(-c4ccccc4)sc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
17989329 80654 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 6 4.8 COc1cc(N2C(=O)c3ccc(Oc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL215508 80654 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 6 4.8 COc1cc(N2C(=O)c3ccc(Oc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
16046114 141366 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 441 7 0 6 4.5 COc1cc(-n2cnc3cc(-c4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL386925 141366 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 441 7 0 6 4.5 COc1cc(-n2cnc3cc(-c4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
10159797 165415 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 0 4 5.1 COc1cc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.056
CHEMBL425263 165415 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 0 4 5.1 COc1cc(N(C)C(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.056
44397126 123742 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@H](N(C)C(=O)N2CC[C@@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL363479 123742 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@H](N(C)C(=O)N2CC[C@@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
11612847 81869 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 488 7 1 4 4.5 COc1ccc2c(c1)CCC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)C2 10.1016/j.bmcl.2006.12.080
CHEMBL217182 81869 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 488 7 1 4 4.5 COc1ccc2c(c1)CCC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)C2 10.1016/j.bmcl.2006.12.080
12020164 194070 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 610 9 1 4 6.7 CCC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL557473 194070 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 610 9 1 4 6.7 CCC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44416224 138955 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 629 6 1 3 8.9 O=C(CN1CCc2cc(-c3cccc(C(F)(F)F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379457 138955 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 629 6 1 3 8.9 O=C(CN1CCc2cc(-c3cccc(C(F)(F)F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
49869190 129267 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 424 2 0 5 4.6 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCCN3C5)c(=O)c2)cn1 nan
CHEMBL3675305 129267 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 424 2 0 5 4.6 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCCN3C5)c(=O)c2)cn1 nan
44424065 85421 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3Cl)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229793 85421 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3Cl)CC1=O)C2 10.1016/j.bmc.2006.12.028
44416713 80039 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 469 6 2 4 4.9 O=C(NCc1cccc2cc(CN3CCC(O)CC3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
CHEMBL214667 80039 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 469 6 2 4 4.9 O=C(NCc1cccc2cc(CN3CCC(O)CC3)cnc12)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
45267812 194398 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 535 7 1 5 5.0 C[C@@H](NC(=O)c1ccc(CN2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL560689 194398 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 535 7 1 5 5.0 C[C@@H](NC(=O)c1ccc(CN2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
44424262 85338 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 430 6 2 2 5.4 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccc[nH]2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229350 85338 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 430 6 2 2 5.4 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2ccc[nH]2)CC1 10.1016/j.bmc.2007.05.068
44416910 80089 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 460 5 0 6 5.4 CN(C)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL214790 80089 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 460 5 0 6 5.4 CN(C)Cc1cnc2c(Cn3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)cccc2c1 10.1016/j.bmcl.2006.07.006
11387603 123735 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 575 5 1 2 9.1 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(C(F)(F)F)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
CHEMBL363459 123735 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 575 5 1 2 9.1 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(C(F)(F)F)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
44416711 80259 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 462 11 1 5 6.2 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL215141 80259 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 462 11 1 5 6.2 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416579 80681 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 8 1 4 5.6 CC(C)N(CCOc1ccc(NC(=O)c2ccc3c(c2)C(=O)c2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL215614 80681 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 8 1 4 5.6 CC(C)N(CCOc1ccc(NC(=O)c2ccc3c(c2)C(=O)c2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
44416817 168746 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 1 4 6.3 CC(C)N(CCOc1ccc(NC(=O)c2ccc3oc4ccccc4c3c2)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL441696 168746 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 1 4 6.3 CC(C)N(CCOc1ccc(NC(=O)c2ccc3oc4ccccc4c3c2)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
11569327 165440 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 485 7 1 4 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccnc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL425410 165440 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 485 7 1 4 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccnc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44416881 81981 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 510 6 1 5 4.1 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL217300 81981 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 510 6 1 5 4.1 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416800 96381 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 494 6 1 4 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL265255 96381 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 494 6 1 4 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
11635674 200154 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL607121 200154 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
11560835 139340 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 421 4 1 7 3.4 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL379933 139340 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 421 4 1 7 3.4 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44414451 168362 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 429 4 0 5 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL438792 168362 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 429 4 0 5 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44430460 86784 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 567 4 0 6 6.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232858 86784 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 567 4 0 6 6.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2007.02.012
11520239 3562 4 None -2 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm040084c
1313 3562 4 None -2 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm040084c
CHEMBL185271 3562 4 None -2 4 Rat 8.7 pKi = 8.7 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 10.1021/jm040084c
44396807 66750 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 504 6 0 5 4.4 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(Cl)c1 10.1016/j.bmcl.2005.05.015
CHEMBL187371 66750 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 504 6 0 5 4.4 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(Cl)c1 10.1016/j.bmcl.2005.05.015
44397630 67018 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL188654 67018 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44397288 67092 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 3 3.9 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4)cc3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL189043 67092 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 3 3.9 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4)cc3)C2)C1 10.1016/j.bmcl.2005.05.015
44397479 121522 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL359580 121522 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44424196 85427 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229823 85427 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11569327 165440 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 485 7 1 4 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccnc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL425410 165440 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 485 7 1 4 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccnc4)C[C@H]23)CC1 10.1021/jm050886n
11236807 81140 0 None 1 3 Rat 8.7 pKi = 8.7 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81140 0 None 1 3 Rat 8.7 pKi = 8.7 Binding
Inhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to rat MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
10165163 127971 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 524 6 3 3 6.4 CC(=O)Nc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
CHEMBL366703 127971 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 524 6 3 3 6.4 CC(=O)Nc1cccc(-c2ccc(C3(CNC(=O)Nc4cc(Cl)cc(Cl)c4)CCN(C)CC3)cc2)c1 10.1016/j.bmcl.2005.05.085
44414475 77706 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL210069 77706 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 445 4 0 5 5.3 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424190 165610 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1cccc(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL426369 165610 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 8 1 3 6.2 CC(C)N(CCN(C(=O)Nc1cccc(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44388215 60379 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 6 2 4 5.2 CS(=O)(=O)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL176079 60379 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 532 6 2 4 5.2 CS(=O)(=O)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10224210 62966 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 424 5 2 3 5.0 CN1CCC(CNC(=O)Nc2ccccc2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL179353 62966 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 424 5 2 3 5.0 CN1CCC(CNC(=O)Nc2ccccc2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
11353174 80170 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 7 1 5 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL215030 80170 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 7 1 5 5.7 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44416670 141380 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 9 1 5 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL387013 141380 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 566 9 1 5 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
10128900 140357 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL382140 140357 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
16756754 91683 21 None 81 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1 10.1021/jm060383x
CHEMBL242004 91683 21 None 81 3 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1 10.1021/jm060383x
11610423 165455 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL425518 165455 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
44424244 85318 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 514 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229177 85318 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 514 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11577410 76361 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 536 7 1 3 5.6 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL206616 76361 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 536 7 1 3 5.6 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
45279402 123059 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3618336 123059 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 439 6 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
45279868 123061 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618338 123061 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
44416877 140850 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 6 1 5 5.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL383933 140850 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 6 1 5 5.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
44481640 65131 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 373 5 1 5 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)CCN2C1CNC1 10.1016/j.bmcl.2011.07.020
CHEMBL1830049 65131 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 373 5 1 5 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)CCN2C1CNC1 10.1016/j.bmcl.2011.07.020
44424196 85427 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229823 85427 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 8 1 4 6.7 CC(C)N(CCN(C(=O)Nc1cc(Cl)nc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44424256 168222 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 579 7 2 5 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL437544 168222 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 579 7 2 5 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
45279148 123063 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 517 9 1 9 3.0 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618340 123063 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 517 9 1 9 3.0 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
50908739 18878 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 401 3 1 5 4.4 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
CHEMBL1289051 18878 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 401 3 1 5 4.4 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
10325618 92042 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 565 10 2 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060381c
CHEMBL243128 92042 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 565 10 2 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060381c
10273126 60803 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 412 8 2 3 5.1 CN(C)CCC(CNC(=O)Nc1ccccc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL176548 60803 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 412 8 2 3 5.1 CN(C)CCC(CNC(=O)Nc1ccccc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44417879 79958 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 493 5 1 4 6.5 N#Cc1cccc([C@]23CC[C@@H](N(CN4CCCCC4)c4nc5cc(Cl)c(Cl)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
CHEMBL214470 79958 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 493 5 1 4 6.5 N#Cc1cccc([C@]23CC[C@@H](N(CN4CCCCC4)c4nc5cc(Cl)c(Cl)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
11584710 140756 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL383340 140756 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
11524613 138690 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 421 4 1 7 3.4 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL378869 138690 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 421 4 1 7 3.4 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44481905 65132 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 387 5 0 5 3.1 CN1CC(N2CCc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830050 65132 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 387 5 0 5 3.1 CN1CC(N2CCc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2011.07.020
10289615 76899 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 544 8 1 4 5.8 N#Cc1cccc([C@]23CC[C@@H](N(CCCCN4CCOCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL208025 76899 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 544 8 1 4 5.8 N#Cc1cccc([C@]23CC[C@@H](N(CCCCN4CCOCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
11584710 140756 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL383340 140756 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
44417024 79964 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 6 0 5 4.4 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214497 79964 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 6 0 5 4.4 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416881 81981 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 510 6 1 5 4.1 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL217300 81981 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 510 6 1 5 4.1 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416877 140850 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 6 1 5 5.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL383933 140850 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 552 6 1 5 5.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCC(C)(C)CC5)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2006.06.049
10142124 60189 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 506 6 2 3 6.7 CCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL175783 60189 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 506 6 2 3 6.7 CCN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
10164110 128940 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 501 5 2 2 7.1 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(Cl)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL367215 128940 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 501 5 2 2 7.1 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(Cl)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44414600 138984 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 502 7 1 3 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(F)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL379535 138984 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 502 7 1 3 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(F)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
11626170 78771 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 5 1 7 3.9 CCc1ccc(-c2cc3cnn(-c4ccc(N5CC[C@@H](NC)C5)nc4)c(=O)c3s2)cc1 10.1021/jm051263c
CHEMBL211340 78771 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 431 5 1 7 3.9 CCc1ccc(-c2cc3cnn(-c4ccc(N5CC[C@@H](NC)C5)nc4)c(=O)c3s2)cc1 10.1021/jm051263c
45279493 123049 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618326 123049 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
24857598 18914 12 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
24857598 18914 12 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289283 18914 12 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289283 18914 12 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.122
50908738 19134 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 3 1 5 3.7 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
CHEMBL1290720 19134 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 3 1 5 3.7 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
24857598 18914 12 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289283 18914 12 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 414 7 0 6 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
10165503 125419 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 532 5 1 3 8.0 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cc(Cl)cc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL364871 125419 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 532 5 1 3 8.0 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cc(Cl)cc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
10115919 63013 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 466 8 3 3 6.0 CNCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL179493 63013 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 466 8 3 3 6.0 CNCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
11238080 75599 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL205285 75599 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44414622 77719 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 514 8 1 4 5.1 COc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL210155 77719 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 514 8 1 4 5.1 COc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
44424188 85408 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 503 9 1 5 5.9 CC(C)N(CCN(C(=O)Nc1cccc([N+](=O)[O-])c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229716 85408 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 503 9 1 5 5.9 CC(C)N(CCN(C(=O)Nc1cccc([N+](=O)[O-])c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11238080 75599 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL205285 75599 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm050886n
44194850 19112 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 389 2 1 4 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290601 19112 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 389 2 1 4 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
44399610 67417 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm049035q
CHEMBL190842 67417 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm049035q
11238080 75599 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL205285 75599 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 543 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.12.080
44424194 85417 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229769 85417 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11504906 75502 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 548 8 1 4 5.4 COc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1021/jm050886n
CHEMBL204881 75502 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 548 8 1 4 5.4 COc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1021/jm050886n
45279489 123050 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618327 123050 0 None 1 2 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
4033 1860 42 None -8 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2010.09.037
9826520 1860 42 None -8 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2010.09.037
CHEMBL214957 1860 42 None -8 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 481 7 0 7 5.3 COc1cc(ccc1OCCN1CCCC1)n1cnc2c(c1=O)sc(c2)c1ccc(cc1)Cl 10.1016/j.bmcl.2010.09.037
25206454 19048 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 448 6 0 6 4.6 COc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)c(Cl)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290261 19048 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 448 6 0 6 4.6 COc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)c(Cl)c1 10.1016/j.bmcl.2010.09.037
11671178 76188 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 548 8 1 4 5.4 COc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL206248 76188 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 548 8 1 4 5.4 COc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
16756074 92169 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 587 10 2 3 6.5 CC(C)C(=O)Nc1c(F)cc(F)c(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1F 10.1021/jm060381c
CHEMBL243578 92169 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 587 10 2 3 6.5 CC(C)C(=O)Nc1c(F)cc(F)c(C2CCN(CCCNC(=O)C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c1F 10.1021/jm060381c
66873578 127616 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665396 127616 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CNCCC2 nan
58092270 129237 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 474 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675278 129237 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 474 4 0 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CCN1CCCCC21 nan
12020149 194809 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 596 8 1 4 6.4 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL563412 194809 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 596 8 1 4 6.4 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44455417 96999 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 462 5 1 6 4.5 COC(=O)Nc1ccc2c(c1)C[C@@H](CN1CC[C@@H](n3c(C)nc4cc(C)ccc43)[C@H](OC)C1)C2 10.1016/j.bmcl.2008.01.010
CHEMBL270151 96999 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 462 5 1 6 4.5 COC(=O)Nc1ccc2c(c1)C[C@@H](CN1CC[C@@H](n3c(C)nc4cc(C)ccc43)[C@H](OC)C1)C2 10.1016/j.bmcl.2008.01.010
44425807 142870 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 565 7 1 6 5.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(N)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389808 142870 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 565 7 1 6 5.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(N)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44425817 142877 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 574 7 0 5 6.4 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389810 142877 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 574 7 0 5 6.4 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44424168 85491 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229983 85491 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424172 165608 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL426364 165608 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 480 6 2 4 4.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44389392 122555 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 584 8 0 3 6.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCC3CCCC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL360977 122555 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 584 8 0 3 6.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCC3CCCC3)C2)C1 10.1016/j.bmcl.2004.12.036
11238695 67239 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 591 6 1 3 9.0 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(OC(F)(F)F)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
CHEMBL190219 67239 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 591 6 1 3 9.0 O=C(Nc1cc(Cl)cc(Cl)c1)N(c1ccc(-c2cccc(OC(F)(F)F)c2)cc1)C1CCN(C2CCCC2)CC1 10.1021/jm0503852
10210351 122423 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 579 10 3 3 8.4 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(OC(F)(F)F)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL360732 122423 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 579 10 3 3 8.4 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(OC(F)(F)F)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
11317824 81117 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 490 7 1 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216068 81117 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 490 7 1 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
44415525 80685 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 585 5 1 4 4.3 CC(=O)N1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL215624 80685 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 585 5 1 4 4.3 CC(=O)N1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44425793 86238 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 489 8 0 5 4.6 CCCCN1C(=O)N(Cc2ccccc2F)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)C1=O 10.1016/j.bmcl.2007.01.104
CHEMBL231651 86238 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 489 8 0 5 4.6 CCCCN1C(=O)N(Cc2ccccc2F)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)C1=O 10.1016/j.bmcl.2007.01.104
16756519 92569 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 466 8 1 3 6.7 O=C(CCCN1CCC(c2cccc(NC(=O)C3CCCCC3)c2)CC1)c1ccc(Cl)cc1 10.1021/jm060383x
CHEMBL244163 92569 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 466 8 1 3 6.7 O=C(CCCN1CCC(c2cccc(NC(=O)C3CCCCC3)c2)CC1)c1ccc(Cl)cc1 10.1021/jm060383x
44424072 85183 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 402 8 1 2 5.8 Fc1ccc(-c2ccc(CNCCc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL228293 85183 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 402 8 1 2 5.8 Fc1ccc(-c2ccc(CNCCc3ccc(CN4CCCCC4)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
44416650 80249 0 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 456 6 1 5 4.2 O=C(NCc1cccc2cc(CN3CCOCC3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
CHEMBL215131 80249 0 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 456 6 1 5 4.2 O=C(NCc1cccc2cc(CN3CCOCC3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
10239389 126975 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 518 6 2 4 5.3 N#Cc1cccc([C@H]2CC[C@@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)CC2)c1 10.1021/jm049035q
CHEMBL366161 126975 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 518 6 2 4 5.3 N#Cc1cccc([C@H]2CC[C@@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)CC2)c1 10.1021/jm049035q
44437555 168678 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL441148 168678 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2007.02.049
44437555 168678 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL441148 168678 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2010.09.014
44437555 168678 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL441148 168678 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2007.02.049
44437555 168678 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL441148 168678 0 None 45 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)CO)cc2)cc1 10.1016/j.bmc.2010.09.014
44417880 141137 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 422 6 1 4 4.4 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL385535 141137 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 422 6 1 4 4.4 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)c1 10.1016/j.bmcl.2006.07.053
23567391 62927 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2005.05.039
CHEMBL179203 62927 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2005.05.039
45270386 193741 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1ccccc1[C@@H](C)NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL552229 193741 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1ccccc1[C@@H](C)NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
15983865 93486 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 496 6 1 5 4.2 CC(=O)N1CCN(Cc2ccc(/C=C3\NC(=O)N(c4ccc(Oc5ccccc5)cc4)C3=O)cc2)CC1 10.1016/j.bmcl.2007.04.012
CHEMBL248267 93486 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 496 6 1 5 4.2 CC(=O)N1CCN(Cc2ccc(/C=C3\NC(=O)N(c4ccc(Oc5ccccc5)cc4)C3=O)cc2)CC1 10.1016/j.bmcl.2007.04.012
20877140 94125 6 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 369 8 1 4 4.3 CC(C)N(CCCNC(=O)c1cc2sccc2n1C)Cc1ccccc1 10.1021/jm070759m
CHEMBL251948 94125 6 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 369 8 1 4 4.3 CC(C)N(CCCNC(=O)c1cc2sccc2n1C)Cc1ccccc1 10.1021/jm070759m
49870326 127585 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 469 4 1 7 3.8 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665365 127585 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 469 4 1 7 3.8 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
67970575 125873 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 372 4 1 6 2.7 O=c1cc(OCc2ccccc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651083 125873 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 372 4 1 6 2.7 O=c1cc(OCc2ccccc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
49868916 129253 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 439 4 0 5 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCCCN1CC2 nan
CHEMBL3675292 129253 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 439 4 0 5 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCCCN1CC2 nan
58092271 129276 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 445 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675314 129276 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 445 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)C1CCCN1CC2 nan
50902096 124089 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 412 4 1 6 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640809 124089 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 412 4 1 6 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)C1CCC(C2)N1 nan
16043220 77682 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 574 7 2 6 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5c(N)noc5c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL209964 77682 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 574 7 2 6 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5c(N)noc5c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44416714 140910 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 550 9 1 4 6.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384234 140910 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 550 9 1 4 6.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
11612491 139327 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 469 4 0 7 4.2 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)oc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL379927 139327 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 469 4 0 7 4.2 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)oc4c3=O)cn2)C1 10.1021/jm051263c
70695565 77620 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL2096889 77620 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44430487 86273 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 467 4 0 7 3.1 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL231816 86273 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 467 4 0 7 3.1 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
44415525 80685 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 585 5 1 4 4.3 CC(=O)N1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL215624 80685 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 585 5 1 4 4.3 CC(=O)N1CCC(N[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44424249 85326 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 584 10 2 4 6.5 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN4CC[C@H](O)C4)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229229 85326 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 584 10 2 4 6.5 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN4CC[C@H](O)C4)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44424232 85477 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 7 1 4 5.2 CCS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229926 85477 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 7 1 4 5.2 CCS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
45279488 123044 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 381 4 0 6 3.8 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618321 123044 0 None -2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 381 4 0 6 3.8 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL4115701 211130 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
11169159 96334 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 578 9 1 6 4.6 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCOCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL264906 96334 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 578 9 1 6 4.6 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCOCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44415526 80664 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215550 80664 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44425818 160704 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 574 7 0 5 6.4 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(C#N)cc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL412006 160704 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 574 7 0 5 6.4 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(C#N)cc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44425790 141721 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 433 5 1 5 3.1 O=C1NC(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL388491 141721 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 433 5 1 5 3.1 O=C1NC(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44424236 85489 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.bmc.2007.05.068
CHEMBL229980 85489 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.bmc.2007.05.068
44437528 145661 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392015 145661 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437528 145661 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392015 145661 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437528 145661 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392015 145661 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437528 145661 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392015 145661 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 645 14 1 6 6.9 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437524 145657 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392013 145657 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2007.02.049
44437524 145657 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392013 145657 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2010.09.014
44437524 145657 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392013 145657 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2007.02.049
44437524 145657 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392013 145657 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)COC(C)=O)cc1 10.1016/j.bmc.2010.09.014
10239389 68973 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 518 6 2 4 5.3 N#Cc1cccc([C@H]2CC[C@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)CC2)c1 10.1021/jm049035q
CHEMBL192923 68973 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 518 6 2 4 5.3 N#Cc1cccc([C@H]2CC[C@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)CC2)c1 10.1021/jm049035q
11511638 76397 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 497 7 1 4 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@H]2CC[C@@H](c3cccc(C#N)c3)C2)CC1 10.1021/jm050886n
CHEMBL206813 76397 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 497 7 1 4 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@H]2CC[C@@H](c3cccc(C#N)c3)C2)CC1 10.1021/jm050886n
66873837 127592 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(Cl)cc5Cl)cc4=O)cc31)CNCCC2 nan
CHEMBL3665372 127592 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(Cl)cc5Cl)cc4=O)cc31)CNCCC2 nan
49870049 127627 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)cc31)CCNCC2 nan
CHEMBL3665406 127627 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)cc31)CCNCC2 nan
49868918 129263 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 440 4 0 6 4.1 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCN3C5)c(=O)c2)cn1 nan
CHEMBL3675301 129263 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 440 4 0 6 4.1 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCN3C5)c(=O)c2)cn1 nan
44415526 80664 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL215550 80664 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
10392311 141222 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 532 5 1 4 6.4 CN1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL386041 141222 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 532 5 1 4 6.4 CN1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
44415526 80664 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215550 80664 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 584 8 1 3 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44415491 80684 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215621 80684 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 640 8 1 3 7.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCC(C)(C)c3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424183 85370 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 6 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC(O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229610 85370 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 6 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC(O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
10238912 75612 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 2 4 4.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL205397 75612 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 482 6 2 4 4.4 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
44389490 130135 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 573 8 1 3 6.3 CN(C(=O)Nc1ccc(-c2ccccc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL368249 130135 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 573 8 1 3 6.3 CN(C(=O)Nc1ccc(-c2ccccc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
25057124 18879 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 6 1 7 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CC2=NCCN2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289053 18879 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 6 1 7 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CC2=NCCN2)c1 10.1016/j.bmcl.2010.09.039
50903069 131297 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 2 2 4 4.7 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693996 131297 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 2 2 4 4.7 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
15983730 168552 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 439 6 1 4 5.2 O=C1N/C(=C\c2ccc(CN3CCCC3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL440229 168552 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 439 6 1 4 5.2 O=C1N/C(=C\c2ccc(CN3CCCC3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
44424176 193116 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 450 6 2 4 3.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)NC4CCCCC4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL538652 193116 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 450 6 2 4 3.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)NC4CCCCC4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44388077 165798 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccccc1C(F)(F)F 10.1016/j.bmcl.2005.05.039
CHEMBL427484 165798 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.3 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccccc1C(F)(F)F 10.1016/j.bmcl.2005.05.039
49868665 129126 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 465 2 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673558 129126 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 465 2 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)CN1CCC2CC1 nan
57524844 125877 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 410 2 1 5 3.8 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651087 125877 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 410 2 1 5 3.8 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
44417871 165375 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C(C)/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL425084 165375 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 7 1 4 3.6 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(C(C)/C=C/c3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
10257298 141000 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 562 6 1 4 7.2 O=C(CN1CCc2cc(-c3cccnc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL384738 141000 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 562 6 1 4 7.2 O=C(CN1CCc2cc(-c3cccnc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44424178 165609 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 537 7 2 4 4.9 CC(=O)NC1CCN(CCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.bmc.2007.05.068
CHEMBL426366 165609 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 537 7 2 4 4.9 CC(=O)NC1CCN(CCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)C1 10.1016/j.bmc.2007.05.068
45279319 122803 0 None 1 2 Rat 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 519 9 1 11 1.8 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3616496 122803 0 None 1 2 Rat 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 519 9 1 11 1.8 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
25205320 19019 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 468 6 0 6 4.8 O=c1cc(-c2ccc(OC(F)(F)F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290042 19019 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 468 6 0 6 4.8 O=c1cc(-c2ccc(OC(F)(F)F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
16756637 92757 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)cc4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244578 92757 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(Cl)cc4)c3)CC2)c1 10.1021/jm060383x
44415402 141080 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 6 0 3 6.2 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL385252 141080 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 6 0 3 6.2 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44425812 160703 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 584 7 0 5 6.6 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cnccc5Cl)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL412005 160703 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 584 7 0 5 6.6 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cnccc5Cl)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44417849 96141 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2006.07.053
CHEMBL263296 96141 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2006.07.053
11282697 66912 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 464 5 1 3 6.7 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccccc3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL188088 66912 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 464 5 1 3 6.7 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccccc3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
45268694 194458 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 549 7 1 5 5.5 CC(c1ccc(C(=O)N[C@@H](C)c2ccc(Br)cc2)cc1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2009.01.031
CHEMBL561148 194458 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 549 7 1 5 5.5 CC(c1ccc(C(=O)N[C@@H](C)c2ccc(Br)cc2)cc1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/j.ejmech.2009.01.031
58580251 125884 0 None - 1 Human 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 396 8 1 7 3.0 COc1cc(-n2ccc(COc3ccccn3)cc2=O)ccc1OCC(C)(C)O nan
CHEMBL3651707 125884 0 None - 1 Human 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 396 8 1 7 3.0 COc1cc(-n2ccc(COc3ccccn3)cc2=O)ccc1OCC(C)(C)O nan
49870578 127604 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 440 2 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665384 127604 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 440 2 1 7 2.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)nc31)CCNCC2 nan
49869913 127575 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 4 1 5 4.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)cc31)CCNCC2 nan
CHEMBL3665356 127575 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 4 1 5 4.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)cc31)CCNCC2 nan
49869187 129264 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 494 4 0 6 4.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCC1C2 nan
CHEMBL3675302 129264 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 494 4 0 6 4.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCC1C2 nan
49869189 129266 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 508 4 0 6 5.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCCC1C2 nan
CHEMBL3675304 129266 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 508 4 0 6 5.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCCC1C2 nan
44414342 77667 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 458 4 0 5 5.1 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL209895 77667 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 458 4 0 5 5.1 CN(C)C1CCN(c2ccc(-c3cn(C)c4cc(-c5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44414356 168341 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 495 5 0 6 5.6 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(OC(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL438615 168341 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 495 5 0 6 5.6 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(OC(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44416261 79567 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 542 6 1 4 6.2 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212756 79567 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 542 6 1 4 6.2 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
10099409 80699 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 562 6 1 4 7.2 O=C(CN1CCc2cc(-c3ccncc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215666 80699 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 562 6 1 4 7.2 O=C(CN1CCc2cc(-c3ccncc3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
10348749 95987 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 608 7 1 4 8.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL262175 95987 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 608 7 1 4 8.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2006.06.055
44415402 141080 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 6 0 3 6.2 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL385252 141080 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 6 0 3 6.2 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
25205153 18992 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 398 5 0 5 4.3 Cc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.037
CHEMBL1289824 18992 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 398 5 0 5 4.3 Cc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.037
9848699 60299 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL176024 60299 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 496 9 3 3 6.9 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
25056872 18996 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 429 7 1 7 2.7 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCNCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289834 18996 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 429 7 1 7 2.7 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCNCC2)c1 10.1016/j.bmcl.2010.09.039
50903150 131291 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693990 131291 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nn5)cc4=O)cc31)C1CCC(C2)N1 nan
23567276 62836 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 538 8 2 3 6.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(F)c(F)c1 10.1016/j.bmcl.2005.05.039
CHEMBL178998 62836 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 538 8 2 3 6.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(F)c(F)c1 10.1016/j.bmcl.2005.05.039
44388355 62632 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 393 5 1 5 3.5 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(N4CCCCC4)nc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178546 62632 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 393 5 1 5 3.5 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(N4CCCCC4)nc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44397312 67127 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 451 4 0 5 3.2 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C#N)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL189282 67127 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 451 4 0 5 3.2 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C#N)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
49869074 127546 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCCNC2 nan
CHEMBL3665327 127546 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCCNC2 nan
49868799 129132 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 445 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CN1CCC2CC1 nan
CHEMBL3673564 129132 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 445 4 0 7 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CN1CCC2CC1 nan
57524674 125868 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 CC1Cc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc3n2C)CN1 nan
CHEMBL3651078 125868 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.9 CC1Cc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc3n2C)CN1 nan
50901933 131298 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 2 5 3.6 O=c1cc(OCc2ccccn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3694003 131298 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 2 5 3.6 O=c1cc(OCc2ccccn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
44417869 80095 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.8 COc1cc(OC)cc(C(=O)NC2CCN(C(C)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214817 80095 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.8 COc1cc(OC)cc(C(=O)NC2CCN(C(C)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44424071 141553 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 416 7 1 2 6.1 O=C(CCc1ccc(CN2CCCCC2)cc1)Nc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL388181 141553 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 416 7 1 2 6.1 O=C(CCc1ccc(CN2CCCCC2)cc1)Nc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2006.12.028
44414444 138065 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 539 8 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N5CCC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL377570 138065 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 539 8 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N5CCC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44454966 154875 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 432 7 1 4 5.5 Cc1ccc2c(c1)nc(C)n2C1CCN(CCCc2cccc(NC(=O)C(C)C)c2)CC1 10.1016/j.bmcl.2008.01.010
CHEMBL403730 154875 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 432 7 1 4 5.5 Cc1ccc2c(c1)nc(C)n2C1CCN(CCCc2cccc(NC(=O)C(C)C)c2)CC1 10.1016/j.bmcl.2008.01.010
44416753 140893 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 508 5 1 4 5.3 CN(C(=O)c1ccc(-c2ccccc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL384145 140893 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 508 5 1 4 5.3 CN(C(=O)c1ccc(-c2ccccc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
10053890 79503 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 576 6 1 4 6.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212508 79503 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 576 6 1 4 6.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44425798 153204 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 559 6 0 5 6.2 O=C1N(c2cccc3ccccc23)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL398186 153204 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 559 6 0 5 6.2 O=C1N(c2cccc3ccccc23)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
17989409 79695 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 416 8 1 4 5.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL213255 79695 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 416 8 1 4 5.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
52948835 18946 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 467 4 0 5 4.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(C(F)(F)F)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289511 18946 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 467 4 0 5 4.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(C(F)(F)F)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
25205316 19107 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 440 5 0 6 5.2 O=c1cc(-c2cc3ccccc3s2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290594 19107 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 440 5 0 6 5.2 O=c1cc(-c2cc3ccccc3s2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
44416753 140893 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 508 5 1 4 5.3 CN(C(=O)c1ccc(-c2ccccc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL384145 140893 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 508 5 1 4 5.3 CN(C(=O)c1ccc(-c2ccccc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416388 79386 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 452 10 1 4 6.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL212032 79386 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 452 10 1 4 6.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416586 79949 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 9 1 3 6.4 Cc1cc(OCCN(C(C)C)C(C)C)ccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2006.06.056
CHEMBL214417 79949 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 9 1 3 6.4 Cc1cc(OCCN(C(C)C)C(C)C)ccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2006.06.056
21101402 140957 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 7 0 7 3.9 COc1cc(-n2nnc3cc(-c4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL384489 140957 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 7 0 7 3.9 COc1cc(-n2nnc3cc(-c4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
58092218 131296 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 416 4 2 5 3.8 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693995 131296 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 416 4 2 5 3.8 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
11410430 141271 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 562 9 1 5 5.4 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL386311 141271 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 562 9 1 5 5.4 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44415460 137600 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 0 3 7.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL376749 137600 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 0 3 7.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44388265 122337 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 379 8 1 4 3.8 CN(C)C1CCN(c2ccc(NC(=O)CCCC(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL360567 122337 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 379 8 1 4 3.8 CN(C)C1CCN(c2ccc(NC(=O)CCCC(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44437557 91305 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240939 91305 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2007.02.049
44437557 91305 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240939 91305 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2010.09.014
44437557 91305 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240939 91305 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2007.02.049
44437557 91305 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240939 91305 0 None 26 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 11 2 4 6.3 COc1ccccc1-c1ccc(CN(CCC2CCN(Cc3ccc(C)cc3)CC2)C(=O)NC(C)(C)CO)cc1 10.1016/j.bmc.2010.09.014
44416472 79992 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 514 10 1 4 7.1 COc1cc(NC(=O)c2ccc(-c3cccc(C(F)(F)F)c3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL214577 79992 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 514 10 1 4 7.1 COc1cc(NC(=O)c2ccc(-c3cccc(C(F)(F)F)c3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416428 80895 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 11 0 4 5.8 CCN(CC)CCOc1ccc(N(CC)C(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
CHEMBL215898 80895 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 11 0 4 5.8 CCN(CC)CCOc1ccc(N(CC)C(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
44416480 141233 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 432 10 2 4 5.4 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1C(C)O 10.1016/j.bmcl.2006.06.056
CHEMBL386111 141233 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 432 10 2 4 5.4 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1C(C)O 10.1016/j.bmcl.2006.06.056
44416816 79967 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 400 6 1 4 5.3 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2oc3ccccc3c2c1 10.1016/j.bmcl.2006.06.061
CHEMBL214504 79967 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 400 6 1 4 5.3 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2oc3ccccc3c2c1 10.1016/j.bmcl.2006.06.061
44416522 140855 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 450 7 1 4 6.2 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1O[C@H]1CCCC[C@@H]1N(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL383972 140855 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 450 7 1 4 6.2 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1O[C@H]1CCCC[C@@H]1N(C)C 10.1016/j.bmcl.2006.06.061
44437525 90985 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240339 90985 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437525 90985 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240339 90985 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
44437525 90985 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240339 90985 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437525 90985 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240339 90985 0 None 6 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 580 11 1 5 6.7 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
44437520 154058 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL399210 154058 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437520 154058 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL399210 154058 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
44437520 154058 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL399210 154058 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437520 154058 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL399210 154058 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 483 9 1 2 6.9 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccccc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
45272942 193998 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 488 6 1 2 6.6 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccccc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL556661 193998 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 488 6 1 2 6.6 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccccc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
49869776 123895 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 6 3.3 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCNCC5)c(=O)c2)cn1 nan
CHEMBL3639642 123895 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 1 6 3.3 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CCNCC5)c(=O)c2)cn1 nan
66874746 127617 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)CNCCC2 nan
CHEMBL3665397 127617 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)CNCCC2 nan
49868784 129274 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCN1CCCC21 nan
CHEMBL3675312 129274 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCN1CCCC21 nan
58092286 129880 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 4 0 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680175 129880 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 4 0 6 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
50902098 124093 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 4 1 6 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640815 124093 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 4 1 6 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)C1CCC(C2)N1 nan
44430489 152311 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 515 5 0 7 4.2 CCOc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(Cl)c1 10.1016/j.bmcl.2007.02.012
CHEMBL397421 152311 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 515 5 0 7 4.2 CCOc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(Cl)c1 10.1016/j.bmcl.2007.02.012
10436663 165444 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 518 5 2 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCNCC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL425434 165444 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 518 5 2 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCNCC2)c1 10.1016/j.bmcl.2006.06.055
44415460 137600 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 0 3 7.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL376749 137600 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 598 8 0 3 7.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44424233 85488 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 592 6 1 4 5.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229979 85488 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 592 6 1 4 5.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
45278977 123052 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618329 123052 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
25205321 19130 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 5 0 6 4.4 Cn1ccc2cc(-c3ccn(-c4ccc5c(cnn5CCN5CCCC5)c4)c(=O)c3)ccc21 10.1016/j.bmcl.2010.09.037
CHEMBL1290713 19130 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 437 5 0 6 4.4 Cn1ccc2cc(-c3ccn(-c4ccc5c(cnn5CCN5CCCC5)c4)c(=O)c3)ccc21 10.1016/j.bmcl.2010.09.037
10230235 131287 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(Cl)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL369392 131287 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(Cl)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
44415462 79596 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 668 9 0 3 8.1 CCN(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212874 79596 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 668 9 0 3 8.1 CCN(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44440586 150284 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 431 8 2 4 5.5 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL395699 150284 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 431 8 2 4 5.5 COc1cc(NC(=O)Nc2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44417989 165607 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 473 6 2 4 4.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(N)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL426339 165607 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 473 6 2 4 4.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(N)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
10054046 16866 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1OC(OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254711 16866 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 584 13 4 7 2.9 COC[C@H]1OC(OCc2ccc(Cl)cc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
44437498 147004 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL393078 147004 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437498 147004 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL393078 147004 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
12020169 193122 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1cccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.ejmech.2009.01.031
CHEMBL538711 193122 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1cccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)c1 10.1016/j.ejmech.2009.01.031
44437498 147004 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL393078 147004 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437498 147004 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL393078 147004 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 413 6 2 2 5.1 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccccc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
49870185 127581 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(Cl)cc5Cl)cc4=O)cc31)CCNCC2 nan
CHEMBL3665361 127581 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(Cl)cc5Cl)cc4=O)cc31)CCNCC2 nan
50902097 124090 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 426 4 0 6 4.0 CN1C2CCC1c1c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3640812 124090 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 426 4 0 6 4.0 CN1C2CCC1c1c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
44417828 80254 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215138 80254 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 404 6 1 4 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
11376122 81461 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 539 6 1 5 4.7 CS(=O)(=O)N1CCC(CN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216471 81461 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 539 6 1 5 4.7 CS(=O)(=O)N1CCC(CN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44415462 79596 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 668 9 0 3 8.1 CCN(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212874 79596 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 668 9 0 3 8.1 CCN(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424199 85435 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 478 6 2 4 4.6 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229875 85435 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 478 6 2 4 4.6 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11635674 200154 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607121 200154 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
16756753 91682 0 None 14 3 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060383x
CHEMBL242003 91682 0 None 14 3 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 478 7 1 3 7.0 Cc1ccc(C2CCN(Cc3ccc(Oc4ccc(F)c(F)c4)cc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060383x
25206134 18875 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 5 0 6 4.0 O=c1cc(-c2ccc(Cl)cn2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289044 18875 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 5 0 6 4.0 O=c1cc(-c2ccc(Cl)cn2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
44437517 90757 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239905 90757 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2007.02.049
44437517 90757 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239905 90757 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2010.09.014
25205150 19003 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 402 5 0 5 4.1 O=c1cc(-c2ccc(F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289940 19003 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 402 5 0 5 4.1 O=c1cc(-c2ccc(F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
44437517 90757 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239905 90757 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2007.02.049
44437517 90757 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239905 90757 0 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 513 10 1 3 6.9 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)C)cc2)cc1 10.1016/j.bmc.2010.09.014
50902099 124096 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 4 1 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640818 124096 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 4 1 6 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5Cl)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL4115716 211145 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44414466 136938 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 570 9 3 4 5.2 CCNC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL375386 136938 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 570 9 3 4 5.2 CCNC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
44414483 79308 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 461 5 0 6 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL211619 79308 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 461 5 0 6 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc(Cl)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44430499 86777 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 551 5 0 8 4.0 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
CHEMBL232834 86777 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 551 5 0 8 4.0 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
44415446 160808 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 0 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL412611 160808 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 0 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CC3)C2)C1 10.1016/j.bmcl.2006.06.045
45279319 122803 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 519 9 1 11 1.8 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3616496 122803 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 519 9 1 11 1.8 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
25017300 19076 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccccc3Cl)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290384 19076 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccccc3Cl)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
16756186 92726 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
CHEMBL244369 92726 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 467 9 2 3 5.2 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccc(F)cc2)CC1 10.1021/jm060381c
16756521 92729 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccccc4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244373 92729 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 428 7 1 3 6.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccccc4)c3)CC2)c1 10.1021/jm060383x
44415446 160808 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 0 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL412611 160808 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 528 6 0 3 5.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CC3)C2)C1 10.1016/j.bmcl.2006.06.045
44417863 79864 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 9 1 6 4.8 CO/N=C/c1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(F)c(F)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
CHEMBL214019 79864 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 9 1 6 4.8 CO/N=C/c1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(F)c(F)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
44415440 141209 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 5 0 3 6.2 CC1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL385959 141209 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 5 0 3 6.2 CC1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44425826 153201 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 466 5 1 5 4.3 COc1cccc(N2C(=O)NC3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL398184 153201 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 466 5 1 5 4.3 COc1cccc(N2C(=O)NC3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
23567290 63129 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccc(Cl)cc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL179872 63129 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 529 9 3 2 8.1 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccc(Cl)cc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
20779442 62930 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 513 6 1 4 5.5 CN1CCC(CNS(=O)(=O)c2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL179216 62930 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 513 6 1 4 5.5 CN1CCC(CNS(=O)(=O)c2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44417831 80041 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 434 7 1 5 4.3 COc1cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)cc(OC)c1OC 10.1016/j.bmcl.2006.07.053
CHEMBL214670 80041 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 434 7 1 5 4.3 COc1cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)cc(OC)c1OC 10.1016/j.bmcl.2006.07.053
49868667 129129 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 426 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CN1CCC2CC1 nan
CHEMBL3673561 129129 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 426 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CN1CCC2CC1 nan
49870577 127603 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665383 127603 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CCNCC2 nan
9799726 141330 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 374 5 1 3 4.2 COc1cccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL386660 141330 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 374 5 1 3 4.2 COc1cccc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44414481 138358 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 480 4 0 6 5.1 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5cnccc5C(F)(F)F)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL378283 138358 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 480 4 0 6 5.1 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5cnccc5C(F)(F)F)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
10256914 79748 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 546 5 1 4 6.7 CC(C)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL213491 79748 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 546 5 1 4 6.7 CC(C)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44415440 141209 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 5 0 3 6.2 CC1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL385959 141209 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 570 5 0 3 6.2 CC1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44424207 85492 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 11 1 4 7.3 CCO/N=C/c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229986 85492 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 11 1 4 7.3 CCO/N=C/c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11692643 76183 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 568 8 1 4 6.0 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(OC(F)(F)F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL206195 76183 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 568 8 1 4 6.0 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(OC(F)(F)F)c4)C[C@H]23)CC1 10.1021/jm050886n
16755968 92046 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 539 13 2 3 7.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243129 92046 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 539 13 2 3 7.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
1725351 125885 8 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 347 3 0 6 1.9 COc1ccc(/C=C2\SC(N3CCN(C)CC3)=NC2=O)cc1OC nan
CHEMBL3651708 125885 8 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 347 3 0 6 1.9 COc1ccc(/C=C2\SC(N3CCN(C)CC3)=NC2=O)cc1OC nan
49869629 127563 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 2 5 3.8 O=c1cc(-c2ccc(C(F)(F)F)nn2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
CHEMBL3665344 127563 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 2 5 3.8 O=c1cc(-c2ccc(C(F)(F)F)nn2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
44425823 142880 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 565 7 1 5 6.2 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389812 142880 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 565 7 1 5 6.2 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44539369 148811 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCHR1 (unknown origin)Binding affinity to MCHR1 (unknown origin)
ChEMBL 584 8 2 8 5.4 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC1(OP(=O)(O)O)CC(F)(F)C1 10.1021/acs.jmedchem.6b00676
CHEMBL3945242 148811 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCHR1 (unknown origin)Binding affinity to MCHR1 (unknown origin)
ChEMBL 584 8 2 8 5.4 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC1(OP(=O)(O)O)CC(F)(F)C1 10.1021/acs.jmedchem.6b00676
44424237 141961 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.5 CS(=O)(=O)N1CCCCC1CN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL389059 141961 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.5 CS(=O)(=O)N1CCCCC1CN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
16072132 80002 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL214629 80002 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 437 8 0 3 3.9 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
25110804 95033 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 458 5 1 6 4.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257280 95033 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 458 5 1 6 4.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(C#N)cc3C2)CC[C@H]1n1c(C(C)(C)O)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44417024 79964 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 6 0 5 4.4 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214497 79964 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 6 0 5 4.4 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44414309 138347 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 489 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Br)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL378230 138347 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 489 4 0 5 5.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc(Br)cc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44430475 86628 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232619 86628 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44430463 148855 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 511 5 0 6 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL394560 148855 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 511 5 0 6 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CC2)C1 10.1016/j.bmcl.2007.02.012
44397254 66949 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 474 4 0 4 4.3 Cc1cc(Cl)ccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
CHEMBL188330 66949 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 474 4 0 4 4.3 Cc1cc(Cl)ccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
44397095 67193 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 470 5 0 5 3.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2005.05.015
CHEMBL189756 67193 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 470 5 0 5 3.6 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2005.05.015
44397018 123377 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.6 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4Cl)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL362790 123377 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.6 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(Cl)cc4Cl)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44397086 123739 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 440 4 0 4 3.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL363470 123739 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 440 4 0 4 3.6 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44396800 126275 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 4 3.9 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2005.05.015
CHEMBL365443 126275 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 4 3.9 Cc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c(C)c1 10.1016/j.bmcl.2005.05.015
16756073 91842 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242689 91842 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C(c2ccccc2)c2ccccc2)CC1 10.1021/jm060381c
10310772 67420 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 466 6 1 3 5.9 N#Cc1cccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)c1 10.1021/jm049035q
CHEMBL190875 67420 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 466 6 1 3 5.9 N#Cc1cccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)c1 10.1021/jm049035q
44399610 67417 0 None -1 2 Mouse 8.5 pKi = 8.5 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm049035q
CHEMBL190842 67417 0 None -1 2 Mouse 8.5 pKi = 8.5 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 557 8 1 4 5.7 CN1CCN(CCCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1021/jm049035q
11752750 60381 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1cccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL176088 60381 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1cccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
46911310 125887 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 421 7 1 6 3.8 COc1cc(-n2ccc(-c3ccc(OC(F)(F)F)cc3)cc2=O)ccc1OCCO nan
CHEMBL3651710 125887 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 421 7 1 6 3.8 COc1cc(-n2ccc(-c3ccc(OC(F)(F)F)cc3)cc2=O)ccc1OCCO nan
11340348 128925 0 None - 1 Human 8.5 pKi = 8.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 468 5 2 3 5.8 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL367156 128925 0 None - 1 Human 8.5 pKi = 8.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 468 5 2 3 5.8 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44414399 80496 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 555 9 2 4 5.4 CCC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
CHEMBL215338 80496 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 555 9 2 4 5.4 CCC(=O)Nc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1016/j.bmcl.2006.05.069
11511147 165631 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 471 4 1 7 4.3 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL426507 165631 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 471 4 1 7 4.3 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44388409 165675 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 371 5 2 3 4.4 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL426777 165675 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 371 5 2 3 4.4 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
45279868 123061 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618338 123061 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 4 2 8 2.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1C[C@H](O)[C@H](O)C1 10.1016/j.bmcl.2015.09.018
25054013 18897 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 444 8 1 7 3.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCC[C@@H]2CO)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289169 18897 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 444 8 1 7 3.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCC[C@@H]2CO)c1 10.1016/j.bmcl.2010.09.039
11532924 137841 0 None 47 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL377241 137841 0 None 47 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 471 4 1 7 4.3 CN[C@@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
11547011 141070 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 455 5 0 6 5.0 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(C)c1 10.1016/j.bmcl.2006.05.075
CHEMBL385141 141070 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 455 5 0 6 5.0 COc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)c(C)c1 10.1016/j.bmcl.2006.05.075
44424258 85333 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 607 8 1 5 5.5 CN(C)Cc1cccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229291 85333 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 607 8 1 5 5.5 CN(C)Cc1cccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11518999 140362 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 502 7 1 3 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL382177 140362 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 502 7 1 3 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
11236807 81140 0 None -1 3 Mouse 8.5 pKi = 8.5 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81140 0 None -1 3 Mouse 8.5 pKi = 8.5 Binding
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
10203421 67105 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 436 6 1 3 5.6 CN(C)CCN(C(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
CHEMBL189147 67105 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 436 6 1 3 5.6 CN(C)CCN(C(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
45279061 123062 0 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 487 6 1 7 4.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618339 123062 0 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 487 6 1 7 4.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
25205319 19033 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 452 5 0 5 5.3 O=c1cc(-c2ccc(Cl)cc2Cl)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290150 19033 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 452 5 0 5 5.3 O=c1cc(-c2ccc(Cl)cc2Cl)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
11548597 75857 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 561 7 1 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)c(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL205838 75857 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 561 7 1 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(C#N)c(F)c4)C[C@H]23)CC1 10.1021/jm050886n
45279489 123050 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618327 123050 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 451 7 1 7 4.0 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC(O)C1CC1 10.1016/j.bmcl.2015.09.018
44194749 19051 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 429 6 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN(CCO)CC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290265 19051 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 429 6 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN(CCO)CC2 10.1016/j.bmcl.2010.09.122
44416895 80175 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 576 5 1 4 6.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL215067 80175 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 576 5 1 4 6.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
46187172 121178 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Antagonist activity at rat MCHR1 assessed as 2-(4-chlorophenyl)-5-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)-4,5-dihydropyrrolo[3,4-c]pyrazol-6(2H)-oneAntagonist activity at rat MCHR1 assessed as 2-(4-chlorophenyl)-5-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)-4,5-dihydropyrrolo[3,4-c]pyrazol-6(2H)-one
ChEMBL 484 8 1 8 3.4 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCC(C)(C)OC(=O)CN 10.1016/j.bmcl.2015.05.008
CHEMBL3588863 121178 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Antagonist activity at rat MCHR1 assessed as 2-(4-chlorophenyl)-5-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)-4,5-dihydropyrrolo[3,4-c]pyrazol-6(2H)-oneAntagonist activity at rat MCHR1 assessed as 2-(4-chlorophenyl)-5-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)-4,5-dihydropyrrolo[3,4-c]pyrazol-6(2H)-one
ChEMBL 484 8 1 8 3.4 COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1OCC(C)(C)OC(=O)CN 10.1016/j.bmcl.2015.05.008
45279061 123062 0 None -1 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 487 6 1 7 4.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618339 123062 0 None -1 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 487 6 1 7 4.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
52942456 19035 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 371 4 2 4 3.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCNC3 10.1016/j.bmcl.2010.09.122
CHEMBL1290155 19035 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 371 4 2 4 3.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCNC3 10.1016/j.bmcl.2010.09.122
16756187 92727 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 507 9 2 3 5.9 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCC2)CC1 10.1021/jm060381c
CHEMBL244370 92727 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 507 9 2 3 5.9 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)C2(c3ccc(F)cc3)CCCC2)CC1 10.1021/jm060381c
16006978 79648 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213052 79648 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
71450863 78193 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 585 5 0 4 6.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cn1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL2112322 78193 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 585 5 0 4 6.0 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cn1)[C@H]1CCN(C(=O)N(C)[C@@H]2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
25206612 19071 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 482 6 0 6 5.2 Cc1cc(OC(F)(F)F)ccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290378 19071 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 482 6 0 6 5.2 Cc1cc(OC(F)(F)F)ccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
16046124 80035 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 488 5 0 3 4.7 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214660 80035 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 488 5 0 3 4.7 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416895 80175 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 576 5 1 4 6.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL215067 80175 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 576 5 1 4 6.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416757 80722 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 7 1 3 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)C(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215754 80722 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 7 1 3 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)C(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
67970248 125874 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 391 4 1 7 2.2 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651084 125874 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 391 4 1 7 2.2 O=c1cc(OCc2ccc(F)cn2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL4115762 211168 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
45266979 193172 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 604 8 1 4 6.6 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4cncnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL539737 193172 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 604 8 1 4 6.6 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4cncnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44424261 143470 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 442 6 1 3 5.4 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cccnc2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL390288 143470 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 442 6 1 3 5.4 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cccnc2)CC1 10.1016/j.bmc.2007.05.068
11526592 74666 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 529 6 1 4 4.9 CN1CCN(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL203445 74666 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 529 6 1 4 4.9 CN1CCN(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
25057913 18981 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 413 6 0 7 3.1 CN1CCN=C1Cn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289726 18981 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 413 6 0 7 3.1 CN1CCN=C1Cn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
20779426 60210 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 405 4 2 2 5.1 Cc1ccc(C2(CNC(=O)Nc3cc(Cl)cc(Cl)c3)CCN(C)CC2)cc1 10.1016/j.bmcl.2005.05.085
CHEMBL175874 60210 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 405 4 2 2 5.1 Cc1ccc(C2(CNC(=O)Nc3cc(Cl)cc(Cl)c3)CCN(C)CC2)cc1 10.1016/j.bmcl.2005.05.085
44425800 148782 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 553 7 0 6 5.3 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5ccnc5C)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL394502 148782 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 553 7 0 6 5.3 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5ccnc5C)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
23567408 167652 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL433608 167652 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 570 8 2 3 7.5 O=C(NCC(CCN1CCC(N2CCCCC2)CC1)c1ccc(Cl)c(Cl)c1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2005.05.039
11330800 81848 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 592 10 2 6 4.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCC[C@H]5CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL217132 81848 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 592 10 2 6 4.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCC[C@H]5CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44388451 63152 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 413 5 1 3 4.7 CC(=O)N(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179974 63152 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 413 5 1 3 4.7 CC(=O)N(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
11664134 81799 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 565 8 1 5 3.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(S(=O)(=O)N(C)C)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL217080 81799 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 565 8 1 5 3.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(S(=O)(=O)N(C)C)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
11519652 82043 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 551 8 2 5 3.4 CNS(=O)(=O)c1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL217618 82043 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 551 8 2 5 3.4 CNS(=O)(=O)c1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
14514271 80056 11 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 354 6 1 4 3.1 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214684 80056 11 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 354 6 1 4 3.1 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
49870554 129234 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 439 4 0 5 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675275 129234 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 439 4 0 5 5.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCCC21 nan
49869188 129265 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 454 4 0 6 4.5 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCCN3C5)c(=O)c2)cn1 nan
CHEMBL3675303 129265 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 454 4 0 6 4.5 Cc1ccc(COc2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCCN3C5)c(=O)c2)cn1 nan
58092278 129881 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 462 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680176 129881 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 462 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CN1CCCC1C2 nan
44455443 95254 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 474 6 1 5 4.9 CO[C@@H]1CN(C[C@@H]2Cc3ccc(NC(=O)C(C)C)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL258260 95254 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 474 6 1 5 4.9 CO[C@@H]1CN(C[C@@H]2Cc3ccc(NC(=O)C(C)C)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44416629 80490 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 467 6 0 3 6.3 CN(Cc1cccc2cc(CN3CCCCC3)cnc12)C(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
CHEMBL215321 80490 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 467 6 0 3 6.3 CN(Cc1cccc2cc(CN3CCCCC3)cnc12)C(=O)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2006.07.006
44388425 62672 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 461 7 1 3 6.3 CN(Cc1ccccc1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178755 62672 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 461 7 1 3 6.3 CN(Cc1ccccc1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44424247 85319 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 10 2 3 6.6 CC(=O)NCc1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229178 85319 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 556 10 2 3 6.6 CC(=O)NCc1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424268 143474 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 7 1 4 6.3 CC(=O)c1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL390290 143474 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 7 1 4 6.3 CC(=O)c1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44389406 62172 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 584 5 0 3 6.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178195 62172 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 584 5 0 3 6.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
16756522 92730 0 None 41 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 442 7 1 3 6.8 Cc1ccc(Oc2cccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)c2)cc1 10.1021/jm060383x
CHEMBL244374 92730 0 None 41 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 442 7 1 3 6.8 Cc1ccc(Oc2cccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)c2)cc1 10.1021/jm060383x
44416990 80537 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 464 7 2 4 2.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCO)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215359 80537 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 464 7 2 4 2.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCO)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
17989409 79695 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 8 1 4 5.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.056
CHEMBL213255 79695 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 8 1 4 5.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.056
44416479 80066 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 10 1 4 5.5 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1C(C)=O 10.1016/j.bmcl.2006.06.056
CHEMBL214715 80066 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 10 1 4 5.5 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1C(C)=O 10.1016/j.bmcl.2006.06.056
16110074 80154 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 418 10 1 4 5.3 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
CHEMBL214968 80154 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 418 10 1 4 5.3 CCN(CC)CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1OC 10.1016/j.bmcl.2006.06.056
17989406 81877 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 8 0 6 5.1 COc1cc(N2C(=O)c3ccc(Sc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL217210 81877 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 8 0 6 5.1 COc1cc(N2C(=O)c3ccc(Sc4ccccc4)cc3C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
18672590 141082 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 10 1 4 6.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL385254 141082 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 10 1 4 6.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416627 79818 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 442 8 1 4 5.2 CCN(CC)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)nc3)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL213817 79818 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 442 8 1 4 5.2 CCN(CC)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)nc3)cccc2c1 10.1016/j.bmcl.2006.07.006
44416738 80141 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 531 7 1 5 5.0 CS(=O)(=O)C1CCN(Cc2cnc3c(CNC(=O)c4ccc(-c5ccc(F)cc5)cc4)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
CHEMBL214916 80141 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 531 7 1 5 5.0 CS(=O)(=O)C1CCN(Cc2cnc3c(CNC(=O)c4ccc(-c5ccc(F)cc5)cc4)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
44396904 66530 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 4 3.9 Cc1cccc(C)c1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
CHEMBL186338 66530 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 454 4 0 4 3.9 Cc1cccc(C)c1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
11385742 84635 4 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 350 9 1 2 3.8 O=C(CCCc1ccccc1)NC[C@H]1CCCN1CCc1ccccc1 10.1021/jm040084c
CHEMBL224438 84635 4 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 350 9 1 2 3.8 O=C(CCCc1ccccc1)NC[C@H]1CCCN1CCc1ccccc1 10.1021/jm040084c
45270393 193921 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 603 8 1 3 7.2 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4ccccc4n3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL555875 193921 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 603 8 1 3 7.2 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4ccccc4n3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44424228 85432 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 522 5 1 3 6.0 CC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229870 85432 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 522 5 1 3 6.0 CC(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
44437516 90756 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239904 90756 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437516 90756 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239904 90756 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
44437516 90756 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239904 90756 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437516 90756 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239904 90756 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 501 9 1 2 7.0 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
44425806 96563 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(OC)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL266739 96563 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(OC)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44424266 85347 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 481 6 1 3 6.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cc3ccccc3o2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229407 85347 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 481 6 1 3 6.8 O=C(Nc1ccc(F)c(Cl)c1)N(CCN1CCCC1)C1CC=C(c2cc3ccccc3o2)CC1 10.1016/j.bmc.2007.05.068
44416798 80147 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 456 8 0 3 6.2 CC(C)N(CCOc1ccc(N(C)C(=O)c2ccc3c(c2)CCc2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL214941 80147 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 456 8 0 3 6.2 CC(C)N(CCOc1ccc(N(C)C(=O)c2ccc3c(c2)CCc2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
17989383 82040 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 0 7 4.7 COc1cc(-n2cnc3ccc(Oc4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL217610 82040 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 0 7 4.7 COc1cc(-n2cnc3ccc(Oc4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
44417859 80086 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 422 6 1 4 4.4 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4cc(F)ccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214778 80086 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 422 6 1 4 4.4 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4cc(F)ccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44416990 80537 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 464 7 2 4 2.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCO)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215359 80537 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 464 7 2 4 2.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCO)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44397200 67020 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4cccc(Cl)c4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL188659 67020 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 460 4 0 4 4.0 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4cccc(Cl)c4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
11296279 80124 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 591 9 1 6 4.5 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCN(C)CC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL214858 80124 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 591 9 1 6 4.5 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCN(C)CC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
11410080 80709 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 9 1 5 4.9 CN(C)Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(F)c(F)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
CHEMBL215695 80709 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 536 9 1 5 4.9 CN(C)Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(F)c(F)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
49870580 127606 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665386 127606 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 419 4 1 7 2.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CCNCC2 nan
57524585 125862 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)nc31)CNCC2 nan
CHEMBL3651072 125862 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)nc31)CNCC2 nan
66603270 129879 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 465 2 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680174 129879 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 465 2 0 6 4.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)CN1CCCC1C2 nan
44415459 78312 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 599 5 0 4 4.7 CC(=O)N1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL211258 78312 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 599 5 0 4 4.7 CC(=O)N1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
11698964 75957 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 498 7 1 3 5.4 Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL205874 75957 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 498 7 1 3 5.4 Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
25054551 18966 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 416 6 2 7 2.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CC2C[C@@H](O)CN2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289624 18966 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 416 6 2 7 2.5 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CC2C[C@@H](O)CN2)c1 10.1016/j.bmcl.2010.09.039
44415459 78312 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 599 5 0 4 4.7 CC(=O)N1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
CHEMBL211258 78312 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 599 5 0 4 4.7 CC(=O)N1CCC(N(C)[C@@H]2CCN(C(=O)N3CC[C@H](N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2006.06.045
44415425 140912 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL384245 140912 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C)C2)C1 10.1016/j.bmcl.2006.06.045
44425804 85745 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 551 7 0 6 5.3 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cncnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL231216 85745 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 551 7 0 6 5.3 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cncnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44397168 167702 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 484 6 0 5 4.1 CC(C)Oc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL433961 167702 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 484 6 0 5 4.1 CC(C)Oc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
57524843 125876 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 4 1 7 3.1 O=c1cc(OCc2ccc(C(F)(F)F)nc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651086 125876 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 4 1 7 3.1 O=c1cc(OCc2ccc(C(F)(F)F)nc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
46878210 200153 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)N1CC[C@@H](N(C)C(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)s2)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL607120 200153 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 590 5 0 4 6.7 CN(C(=O)N1CC[C@@H](N(C)C(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)s2)C1)[C@H]1CCN(C2CCC(C)(C)CC2)C1 10.1016/j.bmcl.2004.12.036
49870811 129258 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 450 2 1 4 5.1 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675297 129258 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 450 2 1 4 5.1 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
9985881 79622 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 590 5 1 5 6.8 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCSC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212955 79622 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 590 5 1 5 6.8 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(C3CCSC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44388365 62740 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 391 5 1 4 4.8 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4cccs4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178864 62740 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 391 5 1 4 4.8 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4cccs4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
44415425 140912 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL384245 140912 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C)C2)C1 10.1016/j.bmcl.2006.06.045
44424198 85428 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 522 6 2 4 4.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Br)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229824 85428 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 522 6 2 4 4.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc(Br)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424204 85479 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 9 1 4 6.2 COC(=O)c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229930 85479 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 527 9 1 4 6.2 COC(=O)c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(F)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
16756184 91693 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242053 91693 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@@H](C)c2ccccc2)CC1 10.1021/jm060381c
44425794 86239 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 515 6 0 5 5.1 O=C1N(C2CCCCC2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL231652 86239 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 515 6 0 5 5.1 O=C1N(C2CCCCC2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44425799 153205 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 563 6 0 5 5.9 O=C1N(C2CCCc3ccccc32)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL398187 153205 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 563 6 0 5 5.9 O=C1N(C2CCCc3ccccc32)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
11698729 81115 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3cc(C#N)ccc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL216066 81115 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3cc(C#N)ccc3C2)CC1 10.1016/j.bmcl.2006.12.080
44397243 123846 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1ccccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
CHEMBL363876 123846 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1ccccc1-c1ccc(C(=O)N(C)[C@H]2CCN(C(=O)N(C)[C@@H]3CCN(C)C3)C2)s1 10.1016/j.bmcl.2005.05.015
15983733 93356 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 413 6 1 4 4.6 CN(C)Cc1ccc(/C=C2\NC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL247566 93356 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 413 6 1 4 4.6 CN(C)Cc1ccc(/C=C2\NC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)cc1 10.1016/j.bmcl.2007.04.012
2729502 80625 5 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
CHEMBL215388 80625 5 None - 1 Human 6.5 pKi = 6.5 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccccc1 10.1016/j.bmcl.2006.07.053
45267015 193097 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.4 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
CHEMBL538215 193097 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.4 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
44416364 140901 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 560 6 1 4 7.2 CC(C)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL384172 140901 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 560 6 1 4 7.2 CC(C)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
10029835 141206 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 526 6 1 4 5.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL385947 141206 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 526 6 1 4 5.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2ccc(F)c(F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
16756751 92865 0 None 40 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2ccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)cc2)cc1 10.1021/jm060383x
CHEMBL245229 92865 0 None 40 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2ccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)cc2)cc1 10.1021/jm060383x
173712 123789 19 None -20 3 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 391 6 1 3 4.9 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1 10.1021/jm060383x
CHEMBL363548 123789 19 None -20 3 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 391 6 1 3 4.9 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1 10.1021/jm060383x
16756401 150397 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 364 7 1 3 4.5 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccccc3)CC2)c1 10.1021/jm060383x
CHEMBL395788 150397 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 364 7 1 3 4.5 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccccc3)CC2)c1 10.1021/jm060383x
52947025 16878 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 548 14 4 7 1.8 COC[C@H]1OC(OCCc2ccccc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254796 16878 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 548 14 4 7 1.8 COC[C@H]1OC(OCCc2ccccc2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44416628 82055 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 469 6 1 5 4.1 CN1CCN(Cc2cnc3c(CNC(=O)c4ccc(-c5ccc(F)cc5)nc4)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
CHEMBL217699 82055 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 469 6 1 5 4.1 CN1CCN(Cc2cnc3c(CNC(=O)c4ccc(-c5ccc(F)cc5)nc4)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
45268725 194429 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 462 7 1 4 5.6 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)C1CCCCC1 10.1016/j.ejmech.2009.01.031
CHEMBL560953 194429 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 462 7 1 4 5.6 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)C1CCCCC1 10.1016/j.ejmech.2009.01.031
15983862 93399 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 467 6 1 4 6.0 O=C1N/C(=C\c2ccc(CN3CCCCCC3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL247764 93399 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 467 6 1 4 6.0 O=C1N/C(=C\c2ccc(CN3CCCCCC3)cc2)C(=O)N1c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.04.012
44417839 161099 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.053
CHEMBL413051 161099 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 362 4 1 2 4.4 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.053
10325994 80652 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 584 6 1 5 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(Cc3ccoc3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215501 80652 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 584 6 1 5 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCN(Cc3ccoc3)CC2)c1 10.1016/j.bmcl.2006.06.055
11353108 141569 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 418 5 1 3 5.1 O=C(Cc1csc2ccccc12)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
CHEMBL388298 141569 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 418 5 1 3 5.1 O=C(Cc1csc2ccccc12)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
16756403 150398 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 378 7 1 3 4.8 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm060383x
CHEMBL395789 150398 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 378 7 1 3 4.8 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm060383x
44416781 80010 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 5 1 4 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)o1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL214649 80010 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 5 1 4 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)o1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44440592 93250 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 9 0 6 4.9 COc1cc(N2C(=O)CN(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246992 93250 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 487 9 0 6 4.9 COc1cc(N2C(=O)CN(c3ccc(Oc4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
45272944 194013 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 494 6 1 2 7.0 C[C@@H](NC(=O)c1ccc(C=C2CCN(CC3CCCCC3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL556868 194013 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 494 6 1 2 7.0 C[C@@H](NC(=O)c1ccc(C=C2CCN(CC3CCCCC3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
58092298 129877 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 445 4 0 7 3.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CN1CCCC1C2 nan
CHEMBL3680172 129877 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 445 4 0 7 3.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)CN1CCCC1C2 nan
44397163 124520 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 444 4 0 4 3.5 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL364414 124520 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 444 4 0 4 3.5 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
10456385 91694 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccccc2)CC1 10.1021/jm060381c
CHEMBL242054 91694 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 449 9 2 3 5.1 Cc1ccc(NC(=O)C(C)C)cc1C1CCN(CCCNC(=O)[C@H](C)c2ccccc2)CC1 10.1021/jm060381c
10142464 128271 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 513 9 3 2 7.6 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(F)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL366934 128271 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 513 9 3 2 7.6 O=C(NCC(CCNC1CCCC1)c1ccc(-c2cccc(F)c2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
52941526 18933 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 418 8 1 7 2.7 CN(C)CC(O)Cn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289400 18933 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 418 8 1 7 2.7 CN(C)CC(O)Cn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
44424169 142485 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 474 7 2 5 4.0 COc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
CHEMBL389483 142485 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 474 7 2 5 4.0 COc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
44424068 85309 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3C(F)(F)F)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL229092 85309 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccccc3C(F)(F)F)CC1=O)C2 10.1016/j.bmc.2006.12.028
11786179 66490 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 552 5 1 3 7.1 CC(C)C(=O)N1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
CHEMBL186156 66490 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 552 5 1 3 7.1 CC(C)C(=O)N1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
50902182 124091 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 431 4 1 7 3.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640813 124091 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 431 4 1 7 3.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)nc31)C1CCC(C2)N1 nan
11756387 141077 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 518 4 1 4 6.0 CN1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL385218 141077 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 518 4 1 4 6.0 CN1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
10098577 141352 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 532 5 1 4 6.3 CCN1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL386819 141352 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 532 5 1 4 6.3 CCN1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44415439 81026 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 3 5.3 CC(C)CN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215951 81026 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 3 5.3 CC(C)CN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
1314 3657 18 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2007.04.012
9865843 3657 18 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2007.04.012
CHEMBL178707 3657 18 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2007.04.012
25017297 19093 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3cccc(Cl)c3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290492 19093 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3cccc(Cl)c3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
44415439 81026 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 3 5.3 CC(C)CN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL215951 81026 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 530 6 0 3 5.3 CC(C)CN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
11698276 82001 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 458 6 1 3 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL217430 82001 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 458 6 1 3 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2006.12.080
44437547 91301 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240912 91301 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437547 91301 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240912 91301 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
44437547 91301 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240912 91301 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437547 91301 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240912 91301 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 627 14 1 6 6.8 CCC(COC(C)=O)(COC(C)=O)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
20779429 60206 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 454 5 3 3 5.5 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCNCC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.085
CHEMBL175860 60206 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 454 5 3 3 5.5 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCNCC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.085
50903068 131295 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693994 131295 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
44430486 86272 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 521 4 0 7 4.0 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(OC(F)(F)F)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL231815 86272 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 521 4 0 7 4.0 CN1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(OC(F)(F)F)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44415401 79837 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 7 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCn3cccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213898 79837 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 7 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCn3cccc3)C2)C1 10.1016/j.bmcl.2006.06.045
16116777 65777 1 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL184037 65777 1 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416498 79719 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3C)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213370 79719 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 10 1 4 6.4 COc1cc(NC(=O)c2ccc(-c3ccccc3C)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416539 79809 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 1 4 5.5 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCCC1 10.1016/j.bmcl.2006.06.056
CHEMBL213767 79809 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 8 1 4 5.5 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN1CCCCC1 10.1016/j.bmcl.2006.06.056
21101400 79875 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 8 4.1 COc1cc(-n2nnc3ccc(Oc4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL214081 79875 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 8 4.1 COc1cc(-n2nnc3ccc(Oc4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
44416521 140854 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 422 7 1 4 5.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC[C@@H]1CCCN1C 10.1016/j.bmcl.2006.06.061
CHEMBL383971 140854 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 422 7 1 4 5.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC[C@@H]1CCCN1C 10.1016/j.bmcl.2006.06.061
11318577 67668 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 532 6 2 4 5.5 C[C@]1(c2cccc(C#N)c2)CC[C@H](N(CCN2CC[C@@H](O)C2)C(=O)Nc2ccc(F)c(C(F)(F)F)c2)CC1 10.1021/jm049035q
CHEMBL191388 67668 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 532 6 2 4 5.5 C[C@]1(c2cccc(C#N)c2)CC[C@H](N(CCN2CC[C@@H](O)C2)C(=O)Nc2ccc(F)c(C(F)(F)F)c2)CC1 10.1021/jm049035q
11678666 76341 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 577 9 2 5 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NS(C)(=O)=O)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL206498 76341 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 577 9 2 5 4.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NS(C)(=O)=O)c4)C[C@H]23)CC1 10.1021/jm050886n
44415396 79741 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2cccnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213465 79741 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2cccnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
10160079 79677 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 434 9 1 3 6.2 CC(C)N(CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1F)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213171 79677 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 434 9 1 3 6.2 CC(C)N(CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1F)C(C)C 10.1016/j.bmcl.2006.06.056
10277257 79976 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 476 11 0 5 6.3 COc1cc(N(C)C(=O)c2cccc(Oc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL214527 79976 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 476 11 0 5 6.3 COc1cc(N(C)C(=O)c2cccc(Oc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
17989325 80417 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 9 0 4 6.0 COc1cc(N2Cc3ccc(-c4ccccc4)cc3C2=O)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL215257 80417 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 9 0 4 6.0 COc1cc(N2Cc3ccc(-c4ccccc4)cc3C2=O)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.061
44416402 138029 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 8 0 3 6.0 CC(C)N(CCOc1ccc(N(C)C(=O)c2ccc3c(c2)Cc2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
CHEMBL377541 138029 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 442 8 0 3 6.0 CC(C)N(CCOc1ccc(N(C)C(=O)c2ccc3c(c2)Cc2ccccc2-3)cc1)C(C)C 10.1016/j.bmcl.2006.06.061
44416781 80010 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 5 1 4 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)o1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL214649 80010 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 5 1 4 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)o1)[C@H]1CCN(C(=O)N2CC[C@@H](NC3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2006.06.049
44415466 139619 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 567 9 2 4 4.9 CC(=O)Nc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL380306 139619 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 567 9 2 4 4.9 CC(=O)Nc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
9978490 121895 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Antagonist activity against rat MCHR1Antagonist activity against rat MCHR1
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
CHEMBL3600828 121895 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Antagonist activity against rat MCHR1Antagonist activity against rat MCHR1
ChEMBL 402 5 0 3 5.3 Clc1ccc(-c2ccc(C#Cc3ccc(OCCN4CCCC4)cc3)nc2)cc1 10.1016/j.bmcl.2015.05.077
44417887 140940 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Cl)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL384400 140940 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 453 8 0 3 4.4 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Cl)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44424066 141530 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 497 8 0 3 4.5 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Br)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL387990 141530 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 497 8 0 3 4.5 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(Br)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
16046124 80035 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 488 5 0 3 4.7 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214660 80035 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 488 5 0 3 4.7 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416757 80722 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 7 1 3 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)C(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215754 80722 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 7 1 3 4.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N[C@@H](C)C(C)C)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44430471 86364 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 5 0 7 4.2 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232209 86364 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 5 0 7 4.2 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOC2)C1 10.1016/j.bmcl.2007.02.012
44430459 86722 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 525 4 0 6 5.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232662 86722 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 525 4 0 6 5.1 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(C2CCCC2)C1 10.1016/j.bmcl.2007.02.012
44430468 91915 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 537 5 0 7 4.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(Cc2ccoc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL243045 91915 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 537 5 0 7 4.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(Cc2ccoc2)C1 10.1016/j.bmcl.2007.02.012
44397245 67179 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL189650 67179 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44397293 123536 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 510 5 0 5 4.2 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(OC(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL363238 123536 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 510 5 0 5 4.2 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(OC(F)(F)F)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
16006978 79648 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213052 79648 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 556 9 1 4 5.6 CSc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
11706744 75174 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 561 7 1 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(F)c(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL204407 75174 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 561 7 1 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(F)c(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
44417965 81721 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 523 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL216820 81721 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 523 7 1 4 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.12.080
11376081 67675 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 536 6 1 3 7.3 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(C(F)(F)F)c3)C3CCN(CC4CC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL191409 67675 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 536 6 1 3 7.3 N#Cc1cccc(-c2ccc(N(C(=O)Nc3ccc(F)c(C(F)(F)F)c3)C3CCN(CC4CC4)CC3)cc2)c1 10.1021/jm0503852
11752750 60381 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1cccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL176088 60381 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1cccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
46911363 125889 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 445 8 1 6 4.9 COc1cc(-n2ccc(SCc3ccc(Cl)cc3)cc2=O)ccc1OCC(C)(C)O nan
CHEMBL3651712 125889 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 445 8 1 6 4.9 COc1cc(-n2ccc(SCc3ccc(Cl)cc3)cc2=O)ccc1OCC(C)(C)O nan
44414432 77569 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 411 4 0 5 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL209542 77569 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 411 4 0 5 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424206 167826 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 10 1 4 6.9 CO/N=C/c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL434747 167826 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 10 1 4 6.9 CO/N=C/c1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
10195637 76343 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 480 6 1 3 5.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCCC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL206503 76343 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 480 6 1 3 5.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCCCC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)c1 10.1021/jm050886n
44424269 85354 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 472 6 1 4 6.0 N#Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229461 85354 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 472 6 1 4 6.0 N#Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44194954 19091 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 4 1 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290490 19091 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 4 1 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
25017571 19113 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 476 5 0 6 5.5 O=c1c2cc(-c3ccc(Cl)cc3F)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290602 19113 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 476 5 0 6 5.5 O=c1c2cc(-c3ccc(Cl)cc3F)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
44193792 19133 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290719 19133 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.7 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
56673836 65129 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 417 7 1 4 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(C3CN(CCF)C3)c[nH]c2c1 10.1016/j.bmcl.2011.07.020
CHEMBL1830047 65129 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 417 7 1 4 4.3 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(C3CN(CCF)C3)c[nH]c2c1 10.1016/j.bmcl.2011.07.020
10140707 62998 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 480 9 3 3 6.4 CCNCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL179425 62998 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 480 9 3 3 6.4 CCNCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44414318 80138 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL214907 80138 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
11684498 77283 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 485 4 0 7 4.7 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL208845 77283 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 485 4 0 7 4.7 CN(C)[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)sc4c3=O)cn2)C1 10.1021/jm051263c
44424216 168751 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 8 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCNCCF)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL441726 168751 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 8 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCNCCF)C(=O)Nc4cc(Cl)nc(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11678040 75093 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 520 7 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(F)c(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL204212 75093 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 520 7 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(F)c(F)c4)C[C@H]23)CC1 10.1021/jm050886n
45279493 123049 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618326 123049 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 465 7 0 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2015.09.018
44424193 141525 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1cc(F)cc(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL387962 141525 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 494 8 1 3 6.3 CC(C)N(CCN(C(=O)Nc1cc(F)cc(F)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44194849 19050 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 4 0 5 3.9 CN1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1290264 19050 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 4 0 5 3.9 CN1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
49836013 127589 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 4 3.8 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)cc31)CNCCC2 nan
CHEMBL3665369 127589 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 436 4 1 4 3.8 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)cc31)CNCCC2 nan
49868670 127547 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665328 127547 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CNCCC2 nan
49869209 127549 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665330 127549 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CNCCC2 nan
57383959 125864 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CNCC2 nan
CHEMBL3651074 125864 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 424 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CNCC2 nan
44414571 79850 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 455 4 0 7 4.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc6c(c5)OCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213949 79850 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 455 4 0 7 4.4 CN(C)C1CCN(c2ccc(-c3coc4cc(-c5ccc6c(c5)OCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
45279583 123060 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 436 4 1 7 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618337 123060 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 436 4 1 7 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
25057388 18913 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 388 7 0 6 3.3 CN(C)CCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
CHEMBL1289282 18913 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 388 7 0 6 3.3 CN(C)CCn1ncc2cc(-n3ccc(OCc4ccccc4)cc3=O)ccc21 10.1016/j.bmcl.2010.09.039
25054288 18948 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 430 7 1 7 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CC[C@H](O)C2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289515 18948 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 430 7 1 7 2.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CC[C@H](O)C2)c1 10.1016/j.bmcl.2010.09.039
11236807 81140 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
CHEMBL216192 81140 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPAInhibition of [125I]MCH binding to human MCHR1 expressed in HEK293 cells by HT-SPA
ChEMBL 472 8 3 4 5.6 Cc1ccc(Oc2ccc(C(=O)NCCN3CCCC3)cc2NC(=O)Nc2ccccc2)cc1C 10.1016/j.bmcl.2006.07.040
10184368 62955 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 480 8 2 3 6.4 CN(C)CCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL179326 62955 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 480 8 2 3 6.4 CN(C)CCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44414375 79679 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
CHEMBL213187 79679 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 541 8 2 4 5.0 CC(=O)Nc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
45279583 123060 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 436 4 1 7 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618337 123060 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 436 4 1 7 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
49869350 127558 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 415 3 1 5 4.8 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cc1 nan
CHEMBL3665339 127558 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 415 3 1 5 4.8 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCCNC5)c(=O)c2)cc1 nan
11454965 82088 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 506 7 1 5 4.8 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL217761 82088 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 506 7 1 5 4.8 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
11455871 141219 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 568 9 1 5 5.9 CN(C)Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(Cl)c(Cl)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
CHEMBL386035 141219 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 568 9 1 5 5.9 CN(C)Cc1cccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)c4nc5cc(Cl)c(Cl)cc5[nH]4)C[C@H]2C3)c1 10.1016/j.bmcl.2006.07.058
44416405 140904 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 544 9 1 3 6.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384181 140904 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 544 9 1 3 6.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44481638 65133 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 419 7 0 5 3.4 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)CCN2C1CN(CCF)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830051 65133 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 419 7 0 5 3.4 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)CCN2C1CN(CCF)C1 10.1016/j.bmcl.2011.07.020
44462720 65134 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 391 3 0 4 3.8 CN1CC(N2CCc3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830052 65134 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 391 3 0 4 3.8 CN1CC(N2CCc3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2011.07.020
50908737 18930 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289395 18930 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 385 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNC2 10.1016/j.bmcl.2010.09.122
44417840 81462 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 392 5 1 2 4.1 O=C(NCc1ccc(F)c(F)c1)[C@@H]1[C@H]2CN(Cc3ccc4ccccc4c3)C[C@H]21 10.1016/j.bmcl.2006.07.053
CHEMBL216472 81462 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 392 5 1 2 4.1 O=C(NCc1ccc(F)c(F)c1)[C@@H]1[C@H]2CN(Cc3ccc4ccccc4c3)C[C@H]21 10.1016/j.bmcl.2006.07.053
10304239 194143 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 604 8 1 4 6.6 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4nccnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL558277 194143 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 604 8 1 4 6.6 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4nccnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44415401 79837 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 7 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCn3cccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213898 79837 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 7 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCn3cccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44425797 165765 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 537 8 0 5 5.1 O=C1N(CCc2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
CHEMBL427262 165765 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 537 8 0 5 5.1 O=C1N(CCc2ccccc2)C(=O)C2(CCN(Cc3ccc(-n4ccnc4)cc3)CC2)N1Cc1ccccc1F 10.1016/j.bmcl.2007.01.104
44415396 79741 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2cccnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL213465 79741 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2cccnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415466 139619 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 567 9 2 4 4.9 CC(=O)Nc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL380306 139619 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 567 9 2 4 4.9 CC(=O)Nc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
11410594 96740 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 576 9 1 5 5.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL268385 96740 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 576 9 1 5 5.8 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CCCCC5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44416140 79368 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 548 5 2 5 5.7 CC(O)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL211964 79368 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 548 5 2 5 5.7 CC(O)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44415414 138138 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 6 0 3 5.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL377814 138138 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 6 0 3 5.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
45272984 194033 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.4 CC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
CHEMBL557070 194033 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.4 CC(NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.031
44416391 81107 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 414 6 1 4 4.4 CN(C)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)nc3)cccc2c1 10.1016/j.bmcl.2006.07.006
CHEMBL216038 81107 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 414 6 1 4 4.4 CN(C)Cc1cnc2c(CNC(=O)c3ccc(-c4ccc(F)cc4)nc3)cccc2c1 10.1016/j.bmcl.2006.07.006
44440589 148548 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 471 8 0 5 4.8 COc1cc(N2CC(=O)N(c3ccc(-c4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL394310 148548 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 471 8 0 5 4.8 COc1cc(N2CC(=O)N(c3ccc(-c4ccccc4)cc3)C2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
44424067 142643 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(C(F)(F)F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL389618 142643 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3ccc(C(F)(F)F)cc3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44415414 138138 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 6 0 3 5.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL377814 138138 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 542 6 0 3 5.4 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)CC3CCC3)C2)C1 10.1016/j.bmcl.2006.06.045
49869211 127551 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665332 127551 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
44437522 90794 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240126 90794 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437522 90794 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240126 90794 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437522 90794 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240126 90794 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2007.02.049
44437522 90794 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240126 90794 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 573 11 1 4 7.0 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmc.2010.09.014
44437496 91544 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241587 91544 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437496 91544 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241587 91544 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437496 91544 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241587 91544 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437496 91544 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241587 91544 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 443 7 2 3 5.1 COc1ccccc1-c1ccc(CNC(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44414552 79630 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 535 7 2 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(O)nc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL212979 79630 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 535 7 2 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(O)nc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44416322 80078 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 595 6 1 3 8.5 O=C(CN1CCc2cc(-c3cccc(Cl)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL214750 80078 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 595 6 1 3 8.5 O=C(CN1CCc2cc(-c3cccc(Cl)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44388311 62677 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 366 7 2 3 3.6 CN(C)C1CCN(c2ccc(NC(=O)NCCCc3ccccc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL178772 62677 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 366 7 2 3 3.6 CN(C)C1CCN(c2ccc(NC(=O)NCCCc3ccccc3)cc2)C1 10.1016/j.bmcl.2005.05.130
16745305 145835 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392156 145835 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
16745305 145835 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392156 145835 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
16756524 143376 0 None 23 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2cccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)c2)cc1 10.1021/jm060383x
CHEMBL390212 143376 0 None 23 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 458 8 1 4 6.5 COc1ccc(Oc2cccc(CN3CCC(c4cccc(NC(=O)C(C)C)c4)CC3)c2)cc1 10.1021/jm060383x
25057645 18982 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 430 7 0 7 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCOCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1289727 18982 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 430 7 0 7 3.1 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(cnn2CCN2CCOCC2)c1 10.1016/j.bmcl.2010.09.039
44415431 79640 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cn1 10.1016/j.bmcl.2006.06.045
CHEMBL213010 79640 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cn1 10.1016/j.bmcl.2006.06.045
16745305 145835 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392156 145835 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
16745305 145835 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392156 145835 0 None 26 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 10 2 4 6.1 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
44388309 122758 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 399 6 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)Cc3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL361423 122758 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 399 6 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)Cc3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
49870700 129125 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673557 129125 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 444 4 0 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCC2CC1 nan
49870325 127584 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 403 4 1 5 2.5 Cn1c2c(c3ccc(N4CCN(CCc5ccccn5)CC4=O)cc31)CNCCC2 nan
CHEMBL3665364 127584 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 403 4 1 5 2.5 Cn1c2c(c3ccc(N4CCN(CCc5ccccn5)CC4=O)cc31)CNCCC2 nan
66873755 127639 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 4 1 7 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CNCCC2 nan
CHEMBL3665418 127639 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 4 1 7 3.0 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CNCCC2 nan
44425803 96562 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 550 7 0 5 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccncc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL266738 96562 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 550 7 0 5 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccncc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415431 79640 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cn1 10.1016/j.bmcl.2006.06.045
CHEMBL213010 79640 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 541 9 1 5 4.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cn1 10.1016/j.bmcl.2006.06.045
44417868 80429 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 578 9 2 6 4.4 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL215273 80429 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 578 9 2 6 4.4 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
58092274 129236 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675277 129236 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCN1CCCCC21 nan
9984325 96229 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 524 6 1 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cccc(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL263975 96229 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 524 6 1 4 6.1 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cccc(Cl)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44430501 150644 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 565 4 0 9 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc5c(c4)OCCO5)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL395979 150644 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 565 4 0 9 3.4 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc5c(c4)OCCO5)sc3c2=O)C1)[C@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44425837 85589 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 436 4 1 4 4.3 N#Cc1cccc(-c2ccc(CN3CCC4(CC3)C(=O)NC(=O)N4c3ccccc3)cc2)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230626 85589 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 436 4 1 4 4.3 N#Cc1cccc(-c2ccc(CN3CCC4(CC3)C(=O)NC(=O)N4c3ccccc3)cc2)c1 10.1016/j.bmcl.2007.01.104
44416346 79433 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 550 6 2 3 7.2 O=C(CN1CCc2cc(-c3ccc[nH]3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL212230 79433 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 550 6 2 3 7.2 O=C(CN1CCc2cc(-c3ccc[nH]3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44389546 64427 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 591 5 0 5 6.1 CN(C(=O)c1cnc(-c2ccc(C(F)(F)F)cc2)s1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL181931 64427 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 591 5 0 5 6.1 CN(C(=O)c1cnc(-c2ccc(C(F)(F)F)cc2)s1)C1CCN(C(=O)N(C)C2CCN(C3CCC(C)(C)CC3)C2)C1 10.1016/j.bmcl.2004.12.036
45267814 194418 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 549 7 1 5 5.4 CC1CN(Cc2ccc3c(c2)OCO3)CCN1Cc1ccc(C(=O)N[C@@H](C)c2ccc(Br)cc2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL560888 194418 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 549 7 1 5 5.4 CC1CN(Cc2ccc3c(c2)OCO3)CCN1Cc1ccc(C(=O)N[C@@H](C)c2ccc(Br)cc2)cc1 10.1016/j.ejmech.2009.01.031
44414601 138394 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 574 7 2 6 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5onc(N)c5c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL378439 138394 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 574 7 2 6 5.2 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc5onc(N)c5c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44430488 86312 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 481 4 0 7 3.4 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
CHEMBL232027 86312 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 481 4 0 7 3.4 COc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
44416178 139351 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 627 7 2 4 8.2 O=C(CN1CCc2cc(-c3cccc(-c4ncc[nH]4)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379940 139351 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 627 7 2 4 8.2 O=C(CN1CCc2cc(-c3cccc(-c4ncc[nH]4)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44424252 137029 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 570 12 1 3 7.8 CCN(CC)Cc1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL375466 137029 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 570 12 1 3 7.8 CCN(CC)Cc1cccc([C@]23CC[C@@H](N(CCN(C(C)C)C(C)C)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
10229815 61992 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1ccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL177900 61992 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 9 3 3 7.4 N#Cc1ccc(-c2ccc(C(CCNC3CCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL4115703 211132 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44389604 63946 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 544 7 2 4 5.4 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCN(S(=O)(=O)c2ccccc2)CC1)Nc1ccccc1F 10.1016/j.bmcl.2005.05.085
CHEMBL181020 63946 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 544 7 2 4 5.4 O=C(NCC1(c2ccc(-c3cccnc3)cc2)CCN(S(=O)(=O)c2ccccc2)CC1)Nc1ccccc1F 10.1016/j.bmcl.2005.05.085
45272117 193581 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 468 6 1 4 5.3 O=C(N[C@@H]1CCc2ccccc21)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL551149 193581 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 468 6 1 4 5.3 O=C(N[C@@H]1CCc2ccccc21)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
49869774 127570 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 2 0 5 4.4 CC(=O)N1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)ccc23)CC1 nan
CHEMBL3665351 127570 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 2 0 5 4.4 CC(=O)N1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)ccc23)CC1 nan
57524506 125857 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 389 4 1 5 2.1 Cn1c2c(c3ccc(N4CCN(CCc5ccccc5)CC4=O)nc31)CNCC2 nan
CHEMBL3651067 125857 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 389 4 1 5 2.1 Cn1c2c(c3ccc(N4CCN(CCc5ccccc5)CC4=O)nc31)CNCC2 nan
58092289 129240 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 453 4 0 5 5.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCCCC21 nan
CHEMBL3675280 129240 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 453 4 0 5 5.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCN1CCCCCC21 nan
66603252 129279 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 465 2 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)C1CCCN1CC2 nan
CHEMBL3675317 129279 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 465 2 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc31)C1CCCN1CC2 nan
44455367 95172 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 389 4 0 4 4.3 CO[C@@H]1CN(CC2Cc3ccccc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL257905 95172 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 389 4 0 4 4.3 CO[C@@H]1CN(CC2Cc3ccccc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
16755967 92124 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 525 12 2 3 6.6 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243354 92124 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 525 12 2 3 6.6 CC(C)C(=O)Nc1cccc(C2CCN(CCCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
44415463 79597 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 682 8 0 3 7.6 CC(=O)N(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212875 79597 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 682 8 0 3 7.6 CC(=O)N(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415385 79584 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 512 8 1 5 3.7 CN(C(=O)c1ccc(-c2cncnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212829 79584 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 512 8 1 5 3.7 CN(C(=O)c1ccc(-c2cncnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415463 79597 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 682 8 0 3 7.6 CC(=O)N(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212875 79597 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 682 8 0 3 7.6 CC(=O)N(CCC(C)(C)c1ccc(Cl)cc1)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424205 85480 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 515 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CO)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229931 85480 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 515 9 2 3 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CO)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
44424173 142486 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 6 2 4 4.4 Cc1ccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)cc1F 10.1016/j.bmc.2007.05.068
CHEMBL389484 142486 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 6 2 4 4.4 Cc1ccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)cc1F 10.1016/j.bmc.2007.05.068
44389354 63590 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 552 11 0 4 5.0 CN(C(=O)CCCC(=O)c1ccc(Cl)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccccc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL180658 63590 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 552 11 0 4 5.0 CN(C(=O)CCCC(=O)c1ccc(Cl)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccccc3)C2)C1 10.1016/j.bmcl.2004.12.036
25017299 19114 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 488 6 0 7 5.4 COc1cc(Cl)ccc1-c1cc2c(=O)n(-c3ccc4c(cnn4CCN4CCCC4)c3)ccc2o1 10.1016/j.bmcl.2010.09.039
CHEMBL1290603 19114 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 488 6 0 7 5.4 COc1cc(Cl)ccc1-c1cc2c(=O)n(-c3ccc4c(cnn4CCN4CCCC4)c3)ccc2o1 10.1016/j.bmcl.2010.09.039
44415516 138749 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 535 8 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C#N)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379166 138749 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 535 8 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C#N)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415385 79584 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 512 8 1 5 3.7 CN(C(=O)c1ccc(-c2cncnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212829 79584 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 512 8 1 5 3.7 CN(C(=O)c1ccc(-c2cncnc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
49870679 129235 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 2 0 5 5.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCN1CCCCC21 nan
CHEMBL3675276 129235 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 2 0 5 5.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)cc31)CCN1CCCCC21 nan
44417852 141115 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL385393 141115 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
49868939 127537 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 384 2 1 5 3.4 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNCC5)c(=O)c2)cn1 nan
CHEMBL3665318 127537 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 384 2 1 5 3.4 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNCC5)c(=O)c2)cn1 nan
CHEMBL4115761 211167 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44430484 86271 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 465 3 0 6 3.7 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
CHEMBL231814 86271 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 465 3 0 6 3.7 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
44415516 138749 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 535 8 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C#N)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379166 138749 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 535 8 1 4 4.8 CN(C(=O)c1ccc(-c2ccc(C#N)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
16756404 92420 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 456 9 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL244003 92420 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 456 9 1 4 6.3 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Oc4ccccc4)cc3)CC2)c1 10.1021/jm060383x
49869348 127555 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 0 5 4.3 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665336 127555 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 413 4 0 5 4.3 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
49869349 127556 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 0 5 4.7 CCN1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665337 127556 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 0 5 4.7 CCN1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
49870453 127588 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665368 127588 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CNCCC2 nan
45270392 193356 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 603 8 1 3 7.2 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4cccnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL549395 193356 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 603 8 1 3 7.2 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4cccnc4c3)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44455414 96955 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL269939 96955 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 467 4 0 4 5.1 CO[C@@H]1CN(C[C@H]2Cc3ccc(Br)cc3C2)CC[C@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
44416801 79882 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 504 6 1 4 4.0 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214126 79882 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 504 6 1 4 4.0 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44417025 96673 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL267797 96673 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430455 86410 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 499 4 0 6 4.6 CC(C)N1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232257 86410 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 499 4 0 6 4.6 CC(C)N1CC[C@H](N(C)C(=O)N2CC[C@H](n3cnc4cc(-c5ccc(Cl)cc5)sc4c3=O)C2)C1 10.1016/j.bmcl.2007.02.012
44430483 87931 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 465 4 0 6 3.7 CCc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL234931 87931 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 465 4 0 6 3.7 CCc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
44397497 66936 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 450 5 0 4 3.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)cc2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL188206 66936 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 450 5 0 4 3.3 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)cc2)cc1 10.1016/j.bmcl.2005.05.015
44397273 67113 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 468 5 0 4 4.4 CC(C)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL189190 67113 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 468 5 0 4 4.4 CC(C)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44424187 85407 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229715 85407 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
25205318 19018 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 452 5 0 5 5.0 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290041 19018 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 452 5 0 5 5.0 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
10137322 148864 0 None 123 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 426 8 1 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL394569 148864 0 None 123 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 426 8 1 3 5.8 CC(C)C(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
44416801 79882 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 504 6 1 4 4.0 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL214126 79882 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 504 6 1 4 4.0 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44417025 96673 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL267797 96673 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 454 5 0 4 3.9 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)C)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416405 140904 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 544 9 1 3 6.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL384181 140904 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 544 9 1 3 6.2 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416390 141133 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 9 1 4 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL385496 141133 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 9 1 4 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2006.06.049
44455444 94589 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 460 8 1 5 4.9 CO[C@H]1CN(CCCc2cccc(NC(=O)C3CC3)c2)CC[C@@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
CHEMBL255112 94589 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 460 8 1 5 4.9 CO[C@H]1CN(CCCc2cccc(NC(=O)C3CC3)c2)CC[C@@H]1n1c(C)nc2cc(C)ccc21 10.1016/j.bmcl.2008.01.010
11610423 165455 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL425518 165455 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2006.05.075
44388227 60460 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 385 5 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL176142 60460 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 385 5 1 3 4.7 CN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
56660001 65128 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 429 8 1 5 3.9 COCCN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830046 65128 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 429 8 1 5 3.9 COCCN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
44424210 85311 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.bmc.2007.05.068
CHEMBL229112 85311 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@@H](C)CO 10.1016/j.bmc.2007.05.068
52941699 18931 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 4 0 5 3.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289396 18931 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 4 0 5 3.9 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
25017033 19075 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccc(Cl)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290383 19075 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 458 5 0 6 5.4 O=c1c2cc(-c3ccc(Cl)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
49869346 127553 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665334 127553 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
50903153 124087 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3640807 124087 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
44389379 64288 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 592 9 0 4 6.2 CN(C(=O)c1ccc(Oc2ccc(F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL181776 64288 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 592 9 0 4 6.2 CN(C(=O)c1ccc(Oc2ccc(F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
45279773 123055 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 407 3 1 7 2.8 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618332 123055 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 407 3 1 7 2.8 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
16756642 92834 0 None 20 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)cc4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL245010 92834 0 None 20 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 462 7 1 3 7.1 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)cc4)cc3)CC2)c1 10.1021/jm060383x
44414576 79613 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 576 8 1 5 5.2 COC(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
CHEMBL212922 79613 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 576 8 1 5 5.2 COC(=O)c1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1016/j.bmcl.2006.05.069
44414589 79739 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 473 4 0 7 4.0 CN(C)C1CCN(c2ccc(-c3coc4cc(C5=CCC6OCCOC6C5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213459 79739 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 473 4 0 7 4.0 CN(C)C1CCN(c2ccc(-c3coc4cc(C5=CCC6OCCOC6C5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424231 85476 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 6 1 4 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229925 85476 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 542 6 1 4 4.9 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
10186375 78523 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 8 2 3 7.3 N#Cc1cccc(-c2ccc(C(CCN3CCCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL2112988 78523 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 520 8 2 3 7.3 N#Cc1cccc(-c2ccc(C(CCN3CCCCC3)CNC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)c1 10.1016/j.bmcl.2005.05.039
10141528 122422 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 495 6 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C=O)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL360731 122422 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 495 6 2 3 6.3 CN1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccc(C=O)c3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44388428 62962 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 425 7 1 3 5.5 CN(CC1CC1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179346 62962 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 425 7 1 3 5.5 CN(CC1CC1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
1314 3657 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.12.036
9865843 3657 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.12.036
CHEMBL178707 3657 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 402 5 1 2 5.4 CN(CC1CCc2c(C1)ccc(c2)NC(=O)c1ccc(cc1)c1ccc(cc1)F)C 10.1016/j.bmcl.2004.12.036
45279773 123055 0 None -1 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 407 3 1 7 2.8 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618332 123055 0 None -1 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 407 3 1 7 2.8 O=c1c2cc(-c3ccc(Cl)cc3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
11329623 81669 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 506 7 1 5 4.8 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216570 81669 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 506 7 1 5 4.8 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
52942796 18964 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 403 2 0 4 4.6 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289620 18964 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 403 2 0 4 4.6 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
11752320 67375 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 496 6 1 3 6.5 N#Cc1cccc(-c2ccc(N(CCN3CCCC3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
CHEMBL190780 67375 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 496 6 1 3 6.5 N#Cc1cccc(-c2ccc(N(CCN3CCCC3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
10206922 130169 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 494 9 3 3 6.8 CC(C)NCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL368417 130169 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 494 9 3 3 6.8 CC(C)NCCC(CNC(=O)Nc1cc(Cl)cc(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
44416390 141133 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 9 1 4 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2006.06.049
CHEMBL385496 141133 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 560 9 1 4 6.0 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCCCC5CCCCC5)C4)C3)cc2)c(C)c1 10.1016/j.bmcl.2006.06.049
44424189 141524 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 536 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1cccc(Br)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL387961 141524 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 536 8 1 3 6.8 CC(C)N(CCN(C(=O)Nc1cccc(Br)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
49869491 127561 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 385 4 2 4 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
CHEMBL3665342 127561 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 385 4 2 4 3.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCCNC3 nan
25205829 19034 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 486 5 0 5 5.6 O=c1cc(-c2ccc(C(F)(F)F)cc2Cl)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290151 19034 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 486 5 0 5 5.6 O=c1cc(-c2ccc(C(F)(F)F)cc2Cl)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
11420621 66825 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 498 5 1 3 7.3 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cccc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
CHEMBL187721 66825 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 498 5 1 3 7.3 N#Cc1cccc(-c2ccc(N(C(=O)Nc3cccc(Cl)c3)C3CCN(C4CCCC4)CC3)cc2)c1 10.1021/jm0503852
49870699 129124 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCC2CC1 nan
CHEMBL3673556 129124 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 425 4 0 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCC2CC1 nan
66873929 127638 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665417 127638 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)nc31)CNCCC2 nan
44388417 62877 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 399 6 1 3 5.1 CCN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL179072 62877 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 399 6 1 3 5.1 CCN(C)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
11785261 67228 0 None 1 2 Mouse 8.2 pKi = 8.2 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm049035q
CHEMBL190068 67228 0 None 1 2 Mouse 8.2 pKi = 8.2 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm049035q
44430465 92854 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 553 5 0 6 5.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCCCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL245135 92854 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 553 5 0 6 5.7 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCCCC2)C1 10.1016/j.bmcl.2007.02.012
44425789 85508 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 539 7 0 6 5.0 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5ccnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230080 85508 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 539 7 0 6 5.0 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-n5ccnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
16755872 92050 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 11 2 3 6.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL243139 92050 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 11 2 3 6.2 CC(C)C(=O)Nc1cccc(C2CCN(CCCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
10185187 62954 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 495 9 3 2 7.5 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
CHEMBL179325 62954 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 495 9 3 2 7.5 O=C(NCC(CCNC1CCCC1)c1ccc(-c2ccccc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2005.05.039
44416553 79498 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 434 6 1 4 5.6 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC12CCCN(CC1)C2 10.1016/j.bmcl.2006.06.061
CHEMBL212487 79498 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 434 6 1 4 5.6 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC12CCCN(CC1)C2 10.1016/j.bmcl.2006.06.061
44416503 79963 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 10 1 3 5.9 CCc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(CC)CC 10.1016/j.bmcl.2006.06.056
CHEMBL214494 79963 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 10 1 3 5.9 CCc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(CC)CC 10.1016/j.bmcl.2006.06.056
17989373 80420 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 0 7 4.7 COc1cc(-n2cnc3cc(Oc4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL215261 80420 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 457 8 0 7 4.7 COc1cc(-n2cnc3cc(Oc4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
44416606 80650 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 390 8 1 4 4.6 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL215493 80650 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 390 8 1 4 4.6 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C)C 10.1016/j.bmcl.2006.06.056
44416502 168386 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 466 10 1 4 6.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C)Cc1ccccc1 10.1016/j.bmcl.2006.06.056
CHEMBL438966 168386 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 466 10 1 4 6.1 COc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C)Cc1ccccc1 10.1016/j.bmcl.2006.06.056
44416880 82023 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 6 0 4 4.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)CC(F)(F)F)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL217544 82023 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 6 0 4 4.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)CC(F)(F)F)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44427407 141557 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.1 Cc1ccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060381c
CHEMBL388234 141557 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.1 Cc1ccc(C2CCN(CCCNC(=O)C(c3ccccc3)c3ccccc3)CC2)cc1NC(=O)C(C)C 10.1021/jm060381c
46911144 125886 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 428 8 2 6 4.3 COc1cc(-n2ccc(CNc3ccc(Cl)cc3)cc2=O)ccc1OCC(C)(C)O nan
CHEMBL3651709 125886 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 428 8 2 6 4.3 COc1cc(-n2ccc(CNc3ccc(Cl)cc3)cc2=O)ccc1OCC(C)(C)O nan
11273638 84711 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 402 8 1 3 6.2 CC(CCN1CCC(NCc2ccc(-c3ccc(Cl)cc3)o2)C1)CC(C)(C)C 10.1021/jm040084c
CHEMBL225073 84711 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 402 8 1 3 6.2 CC(CCN1CCC(NCc2ccc(-c3ccc(Cl)cc3)o2)C1)CC(C)(C)C 10.1021/jm040084c
44416880 82023 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 6 0 4 4.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)CC(F)(F)F)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL217544 82023 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 522 6 0 4 4.8 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N(C)CC(F)(F)F)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44416580 141393 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 398 6 1 3 5.0 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmcl.2006.06.061
CHEMBL387081 141393 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 398 6 1 3 5.0 O=C(Nc1ccc(OCCN2CCCC2)cc1)c1ccc2c(c1)Cc1ccccc1-2 10.1016/j.bmcl.2006.06.061
44416623 79995 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 10 1 4 6.1 COc1cc(NC(=O)c2cccc(-c3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL214584 79995 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 446 10 1 4 6.1 COc1cc(NC(=O)c2cccc(-c3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44417878 140839 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 398 8 2 5 3.0 COc1cc(OC)cc(C(=O)NC2CCN(CC[C@H](O)c3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL383859 140839 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 398 8 2 5 3.0 COc1cc(OC)cc(C(=O)NC2CCN(CC[C@H](O)c3ccccc3)CC2)c1 10.1016/j.bmcl.2006.07.053
44437519 90793 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240116 90793 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437519 90793 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240116 90793 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
12020152 193772 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 582 7 1 4 6.0 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL552432 193772 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 582 7 1 4 6.0 C[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
16046157 140968 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 516 5 1 7 5.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1Cc1cccc2cc(CN3CCC(O)CC3)cnc12 10.1016/j.bmcl.2006.07.006
CHEMBL384548 140968 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 516 5 1 7 5.3 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1Cc1cccc2cc(CN3CCC(O)CC3)cnc12 10.1016/j.bmcl.2006.07.006
44415427 79614 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C3CCOCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212927 79614 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C3CCOCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44415409 139512 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 3 1 3 3.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL380036 139512 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 3 1 3 3.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N)C2)C1 10.1016/j.bmcl.2006.06.045
44424265 143473 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 459 7 1 4 5.5 O=Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)o1 10.1016/j.bmc.2007.05.068
CHEMBL390289 143473 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 459 7 1 4 5.5 O=Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)o1 10.1016/j.bmc.2007.05.068
44415427 79614 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C3CCOCC3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL212927 79614 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N(C)C3CCOCC3)C2)C1 10.1016/j.bmcl.2006.06.045
44415409 139512 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 3 1 3 3.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL380036 139512 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 460 3 1 3 3.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](N)C2)C1 10.1016/j.bmcl.2006.06.045
11342100 84667 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 454 7 1 3 5.7 O=C(Cc1ccc(Oc2ccccc2)cc1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
CHEMBL224686 84667 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 454 7 1 3 5.7 O=C(Cc1ccc(Oc2ccccc2)cc1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
10483729 16754 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 600 13 4 7 3.4 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253625 16754 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 600 13 4 7 3.4 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
45269555 194435 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 564 7 1 2 8.3 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccc(-c4ccccc4)cc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL561011 194435 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 564 7 1 2 8.3 C[C@@H](NC(=O)c1ccc(C=C2CCN(Cc3ccc(-c4ccccc4)cc3)CC2)cc1)c1ccc(Br)cc1 10.1016/j.ejmech.2009.01.031
44437519 90793 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240116 90793 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2007.02.049
44437519 90793 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240116 90793 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 508 9 1 3 6.8 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4cccc(C#N)c4)cc3)C(=O)NC(C)C)CC2)cc1 10.1016/j.bmc.2010.09.014
44388314 130132 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 396 8 2 4 3.6 COc1ccc(CCCNC(=O)Nc2ccc(N3CCC(N(C)C)C3)cc2)cc1 10.1016/j.bmcl.2005.05.130
CHEMBL368228 130132 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 396 8 2 4 3.6 COc1ccc(CCCNC(=O)Nc2ccc(N3CCC(N(C)C)C3)cc2)cc1 10.1016/j.bmcl.2005.05.130
58093407 127607 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 420 4 1 8 1.9 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(F)cn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665387 127607 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 420 4 1 8 1.9 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(F)cn5)cc4=O)nc31)CCNCC2 nan
44415410 77565 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL209526 77565 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424184 85381 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 496 6 1 4 5.0 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCOCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229665 85381 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 496 6 1 4 5.0 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCOCC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44415410 77565 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL209526 77565 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415426 141295 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 502 5 0 3 4.7 CCN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL386449 141295 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 502 5 0 3 4.7 CCN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424175 85364 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 472 6 2 4 4.6 Cc1cc(C)cc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
CHEMBL229557 85364 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 472 6 2 4 4.6 Cc1cc(C)cc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
25205493 18977 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 398 5 0 5 4.3 Cc1ccccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1289718 18977 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 398 5 0 5 4.3 Cc1ccccc1-c1ccn(-c2ccc3c(cnn3CCN3CCCC3)c2)c(=O)c1 10.1016/j.bmcl.2010.09.037
10348147 79740 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 576 6 1 4 6.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(F)cc(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL213464 79740 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 576 6 1 4 6.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(F)cc(C(F)(F)F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44415426 141295 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 502 5 0 3 4.7 CCN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL386449 141295 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 502 5 0 3 4.7 CCN(C)[C@@H]1CCN(C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424170 85359 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)cc4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229504 85359 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 462 6 2 4 4.1 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)cc4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424250 85490 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 597 10 1 4 6.7 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN4CCN(C)CC4)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229981 85490 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 597 10 1 4 6.7 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(CN4CCN(C)CC4)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
45278576 123056 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 408 3 1 8 2.2 O=c1c2cc(-c3ccc(Cl)cn3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
CHEMBL3618333 123056 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 408 3 1 8 2.2 O=c1c2cc(-c3ccc(Cl)cn3)cn2ncn1-c1ccc(N2CC[C@@H](O)C2)nc1 10.1016/j.bmcl.2015.09.018
16756523 92755 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 484 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(C(C)(C)C)cc4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244576 92755 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 484 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4ccc(C(C)(C)C)cc4)c3)CC2)c1 10.1021/jm060383x
44437494 91453 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241375 91453 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437494 91453 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241375 91453 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437494 91453 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241375 91453 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437494 91453 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241375 91453 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 431 6 2 2 5.3 Cc1ccc(CN2CCC(NC(=O)NCc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44424238 85315 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 544 6 1 4 5.1 CS(=O)(=O)N1CCC[C@H]1CN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229164 85315 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 544 6 1 4 5.1 CS(=O)(=O)N1CCC[C@H]1CN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
44417829 80162 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 432 8 1 4 5.0 CCOc1cc(OCC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215004 80162 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 432 8 1 4 5.0 CCOc1cc(OCC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
44414506 141308 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 525 7 1 5 4.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4nccs4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL386512 141308 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 525 7 1 5 4.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4nccs4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
45268721 195054 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 442 7 1 4 4.8 O=C(NCc1ccccc1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL565119 195054 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 442 7 1 4 4.8 O=C(NCc1ccccc1)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
49870327 127586 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 4 0 6 3.7 CC(=O)N1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
CHEMBL3665366 127586 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 4 0 6 3.7 CC(=O)N1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
44414461 79825 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 553 8 1 4 5.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N5CCCC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL213840 79825 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 553 8 1 4 5.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N5CCCC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44424270 85356 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 473 6 1 5 5.4 N#Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229463 85356 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 473 6 1 5 5.4 N#Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44389509 62328 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN1CCC(N(C)C(=O)N2CCC(N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178388 62328 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 488 4 0 3 4.3 CN1CCC(N(C)C(=O)N2CCC(N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
44417984 141280 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 360 4 2 3 3.9 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cccc(O)c1 10.1016/j.bmcl.2006.07.053
CHEMBL386354 141280 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 360 4 2 3 3.9 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cccc(O)c1 10.1016/j.bmcl.2006.07.053
57524672 125866 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 421 4 1 5 2.6 CC1Cc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)nc3n2C)CN1 nan
CHEMBL3651076 125866 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 421 4 1 5 2.6 CC1Cc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)nc3n2C)CN1 nan
44437499 91546 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241589 91546 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437499 91546 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241589 91546 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437499 91546 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL241589 91546 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437499 91546 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL241589 91546 0 None -4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 9 2 4 5.3 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4ccc(F)cc4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
49870807 129243 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 410 2 0 5 4.2 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCN3C5)c(=O)c2)cn1 nan
CHEMBL3675283 129243 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 410 2 0 5 4.2 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCCN3C5)c(=O)c2)cn1 nan
50902014 124086 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 396 2 1 5 4.0 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCC5N3)c(=O)c2)cn1 nan
CHEMBL3640806 124086 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 396 2 1 5 4.0 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CC3CCC5N3)c(=O)c2)cn1 nan
10029161 141347 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 504 4 2 4 5.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCNCC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL386759 141347 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 504 4 2 4 5.6 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C32CCNCC2)c1 10.1016/j.bmcl.2006.06.055
25018073 19135 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 425 5 0 7 4.1 O=c1c2cc(-c3ccccn3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290721 19135 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 425 5 0 7 4.1 O=c1c2cc(-c3ccccn3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
44437523 145656 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392012 145656 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2007.02.049
44437523 145656 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392012 145656 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2010.09.014
44437523 145656 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL392012 145656 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2007.02.049
44437523 145656 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL392012 145656 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 585 12 1 5 6.8 COc1ccc(-c2ccc(CN(CCC3CCN(Cc4ccc(C)cc4)CC3)C(=O)NC(C)(C)COC(C)=O)cc2)cc1 10.1016/j.bmc.2010.09.014
49868806 127533 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 385 4 2 4 3.6 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
CHEMBL3665314 127533 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 385 4 2 4 3.6 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCNCC3 nan
49870050 127628 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 417 4 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665407 127628 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 417 4 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)cc31)CNCCC2 nan
49836011 129255 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 411 4 1 4 4.6 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
CHEMBL3675294 129255 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 411 4 1 4 4.6 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CCN1CCCC31 nan
44416862 80639 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 440 5 1 4 3.5 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215446 80639 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 440 5 1 4 3.5 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430453 87480 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 575 7 0 6 5.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL233889 87480 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 575 7 0 6 5.8 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCCc2ccccc2)C1 10.1016/j.bmcl.2007.02.012
44425835 85575 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 542 6 0 5 6.2 COc1cccc(N2C(=O)N(c3ccccc3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230521 85575 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 542 6 0 5 6.2 COc1cccc(N2C(=O)N(c3ccccc3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44425839 150684 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 526 5 0 4 6.5 Cc1cccc(N2C(=O)N(c3ccccc3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL396008 150684 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 526 5 0 4 6.5 Cc1cccc(N2C(=O)N(c3ccccc3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
16006976 82018 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 544 8 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(Cl)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL217528 82018 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 544 8 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(Cl)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424191 85415 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 492 8 1 3 6.7 CC(C)N(CCN(C(=O)Nc1cccc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229767 85415 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 492 8 1 3 6.7 CC(C)N(CCN(C(=O)Nc1cccc(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11627700 82030 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 515 7 2 4 4.5 CC(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL217574 82030 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 515 7 2 4 4.5 CC(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
11452967 67174 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 422 6 2 3 5.3 CNCCN(C(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
CHEMBL189611 67174 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 422 6 2 3 5.3 CNCCN(C(=O)Nc1ccc(F)c(Cl)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
10140070 67267 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 470 6 1 3 6.0 CN(C)CCN(C(=O)Nc1ccc(C(F)(F)F)c(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
CHEMBL190401 67267 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 470 6 1 3 6.0 CN(C)CCN(C(=O)Nc1ccc(C(F)(F)F)c(F)c1)c1ccc(-c2cccc(C#N)c2)cc1 10.1021/jm0503852
49869212 127552 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 2 1 4 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665333 127552 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 2 1 4 5.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCCC2 nan
25017572 19053 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 442 5 0 6 4.8 O=c1c2cc(-c3ccc(F)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290267 19053 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 442 5 0 6 4.8 O=c1c2cc(-c3ccc(F)cc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
11329860 141138 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 520 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL385539 141138 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 520 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
44416862 80639 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 440 5 1 4 3.5 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215446 80639 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 440 5 1 4 3.5 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NC)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
49836016 129123 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 411 4 0 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCC2C1 nan
CHEMBL3673555 129123 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 ug protein) were incubated for 60 min at 25 C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 uM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester. The filters were counted for radioactivity.
ChEMBL 411 4 0 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCC2C1 nan
49869210 127550 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665331 127550 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 468 4 1 6 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CNCCC2 nan
66873757 127615 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665395 127615 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CNCCC2 nan
9895005 138890 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 602 6 1 5 7.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCOCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379391 138890 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 602 6 1 5 7.0 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCOCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
16006976 82018 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 544 8 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(Cl)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL217528 82018 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 544 8 1 3 5.6 CN(C(=O)c1ccc(-c2ccc(Cl)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
50903153 124087 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3640807 124087 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 450 2 1 5 4.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
44481364 65135 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 423 5 0 4 4.2 O=c1cc(-c2ccc(Cl)cc2)ccn1-c1ccc2c(c1)CCN2C1CN(CCF)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830053 65135 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 423 5 0 4 4.2 O=c1cc(-c2ccc(Cl)cc2)ccn1-c1ccc2c(c1)CCN2C1CN(CCF)C1 10.1016/j.bmcl.2011.07.020
45279064 123065 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OC[C@H](O)C1CC1 10.1016/j.bmcl.2015.09.018
CHEMBL3618342 123065 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 452 7 1 8 3.4 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OC[C@H](O)C1CC1 10.1016/j.bmcl.2015.09.018
45279062 123068 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 488 6 1 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618345 123068 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 488 6 1 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
45279062 123068 0 None -1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 488 6 1 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618345 123068 0 None -1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 488 6 1 8 3.7 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
11168918 81235 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 555 6 1 5 5.2 CS(=O)(=O)N1CCC(CN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216368 81235 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 555 6 1 5 5.2 CS(=O)(=O)N1CCC(CN(c2nc3cc(F)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
56666883 65125 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 403 5 1 4 4.1 CN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5F)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830043 65125 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 403 5 1 4 4.1 CN1CC(c2c[nH]c3cc(-n4ccc(OCc5ccccc5F)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
44194853 19074 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 453 4 1 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1290382 19074 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 453 4 1 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)cc5)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
11191656 140847 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 522 7 1 5 5.3 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL383901 140847 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 522 7 1 5 5.3 CN1CCN(CCCN(c2nc3cc(Cl)c(Cl)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
44414654 79911 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 567 9 2 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NC(=O)C5CC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL214254 79911 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 567 9 2 4 5.4 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(NC(=O)C5CC5)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
10077403 138389 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 604 10 2 5 6.9 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(CCCCCO)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL378428 138389 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 604 10 2 5 6.9 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(CCCCCO)CC2)c1 10.1016/j.bmcl.2006.06.055
58093324 127612 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 428 5 0 6 3.7 CCN1CCc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665392 127612 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 428 5 0 6 3.7 CCN1CCc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
49869778 127572 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 4 0 6 3.4 CC(=O)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc23)CC1 nan
CHEMBL3665353 127572 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 460 4 0 6 3.4 CC(=O)N1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc23)CC1 nan
49870328 127587 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 2 0 5 4.7 CC(=O)N1CCCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665367 127587 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 480 2 0 5 4.7 CC(=O)N1CCCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc3n2C)C1 nan
49868678 127633 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)nc4=O)cc31)CNCCC2 nan
CHEMBL3665412 127633 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)nc4=O)cc31)CNCCC2 nan
44416607 165374 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 8 1 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL425082 165374 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 8 1 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
44424197 142519 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 7 2 6 3.9 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc([N+](=O)[O-])c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL389517 142519 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 489 7 2 6 3.9 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4cccc([N+](=O)[O-])c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11192044 77619 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 432 6 1 3 5.5 O=C(Cc1csc2ccccc12)NC[C@@H]1CCCN1Cc1ccc(Cl)c(Cl)c1 10.1021/jm040084c
CHEMBL2096864 77619 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 432 6 1 3 5.5 O=C(Cc1csc2ccccc12)NC[C@@H]1CCCN1Cc1ccc(Cl)c(Cl)c1 10.1021/jm040084c
44397103 123900 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 504 5 0 6 2.7 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(S(C)(=O)=O)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL363965 123900 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 504 5 0 6 2.7 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(S(C)(=O)=O)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
44437501 153887 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL399004 153887 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437501 153887 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL399004 153887 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
11641333 168167 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 468 6 1 3 6.0 N#Cc1cccc(C2=CC(N(CCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)CC2)c1 10.1021/jm050886n
CHEMBL437130 168167 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 468 6 1 3 6.0 N#Cc1cccc(C2=CC(N(CCN3CCCC3)C(=O)Nc3cc(Cl)cc(Cl)c3)CC2)c1 10.1021/jm050886n
44437501 153887 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL399004 153887 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437501 153887 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL399004 153887 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 543 10 2 5 5.2 COc1ccccc1-c1ccc(CN(CC(=O)C(C)(C)O)C(=O)NC2CCN(Cc3ccc(C)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44396985 124118 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccccc4C(F)(F)F)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL364134 124118 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 494 4 0 4 4.3 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccccc4C(F)(F)F)s3)C2)C1 10.1016/j.bmcl.2005.05.015
11720881 81452 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 543 8 2 4 5.1 CC(C)C(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL216460 81452 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 543 8 2 4 5.1 CC(C)C(=O)Nc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
11610423 165455 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibitory concentration against human MCH-R1 by GTPgammaS assayInhibitory concentration against human MCH-R1 by GTPgammaS assay
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL425518 165455 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibitory concentration against human MCH-R1 by GTPgammaS assayInhibitory concentration against human MCH-R1 by GTPgammaS assay
ChEMBL 372 5 2 4 3.8 CNC1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cn2)C1 10.1016/j.bmcl.2005.05.130
67970371 125875 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 2 1 6 3.2 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
CHEMBL3651085 125875 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 2 1 6 3.2 O=c1cc(-c2ccc(C(F)(F)F)nc2)ccn1-c1ccn2c3c(nc2c1)CCNC3 nan
57524762 125871 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 372 4 1 6 2.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)nc1n2CCNC1 nan
CHEMBL3651081 125871 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 372 4 1 6 2.9 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c(c1)nc1n2CCNC1 nan
44417860 80087 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 378 5 1 3 4.0 COc1cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)ccc1F 10.1016/j.bmcl.2006.07.053
CHEMBL214779 80087 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 378 5 1 3 4.0 COc1cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)ccc1F 10.1016/j.bmcl.2006.07.053
52942550 19088 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 436 5 0 5 4.7 O=c1cc(-c2ccc(Cl)cc2F)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290484 19088 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 436 5 0 5 4.7 O=c1cc(-c2ccc(Cl)cc2F)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.037
44425820 96832 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 579 8 0 5 6.5 COc1cccc(-c2ccc(CN3CCC4(CC3)C(=O)N(c3cccc(OC)c3)C(=O)N4Cc3ccccc3F)cc2)c1 10.1016/j.bmcl.2007.01.104
CHEMBL269061 96832 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 579 8 0 5 6.5 COc1cccc(-c2ccc(CN3CCC4(CC3)C(=O)N(c3cccc(OC)c3)C(=O)N4Cc3ccccc3F)cc2)c1 10.1016/j.bmcl.2007.01.104
44417870 80000 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 405 6 1 5 3.6 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4n3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL214606 80000 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 405 6 1 5 3.6 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4ccccc4n3)CC2)c1 10.1016/j.bmcl.2006.07.053
10029836 80683 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 526 6 1 4 5.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(F)cc(F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215619 80683 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 526 6 1 4 5.7 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(F)cc(F)c2)C32CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44396975 121727 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 470 6 0 5 3.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
CHEMBL359782 121727 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 470 6 0 5 3.7 CCOc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)cc1 10.1016/j.bmcl.2005.05.015
44416916 80983 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 5 0 4 3.6 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215945 80983 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 5 0 4 3.6 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44416607 165374 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 8 1 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
CHEMBL425082 165374 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 590 8 1 4 6.7 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)s1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCC3CCCCC3)C2)C1 10.1016/j.bmcl.2006.06.049
44416561 79724 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 9 1 3 6.4 Cc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213386 79724 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 430 9 1 3 6.4 Cc1cc(NC(=O)c2ccc(-c3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416664 82396 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 1 4 5.1 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC1CCN(C)C1 10.1016/j.bmcl.2006.06.061
CHEMBL218030 82396 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 408 6 1 4 5.1 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC1CCN(C)C1 10.1016/j.bmcl.2006.06.061
10295411 165573 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 9 1 3 6.1 CC(C)N(CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL426147 165573 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 416 9 1 3 6.1 CC(C)N(CCOc1ccc(NC(=O)c2ccc(-c3ccccc3)cc2)cc1)C(C)C 10.1016/j.bmcl.2006.06.056
11489282 143585 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 406 5 1 4 3.7 O=C(Cc1ccc2c(c1)OCO2)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
CHEMBL390377 143585 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 406 5 1 4 3.7 O=C(Cc1ccc2c(c1)OCO2)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
44415381 80149 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 9 2 4 4.0 CN(C(=O)c1ccc(-c2ccc(C(N)=O)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214946 80149 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 9 2 4 4.0 CN(C(=O)c1ccc(-c2ccc(C(N)=O)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415381 80149 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 9 2 4 4.0 CN(C(=O)c1ccc(-c2ccc(C(N)=O)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL214946 80149 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 553 9 2 4 4.0 CN(C(=O)c1ccc(-c2ccc(C(N)=O)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44415407 138897 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2ccncc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379395 138897 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2ccncc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
52944805 16755 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 586 12 4 7 3.0 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253626 16755 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 586 12 4 7 3.0 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CCN=C(N)N)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
44437514 89900 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL238605 89900 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437514 89900 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL238605 89900 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44437514 89900 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL238605 89900 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2007.02.049
44437514 89900 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL238605 89900 0 None -2 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 538 9 2 5 5.1 Cc1ccc(CN2CCC(NC(=O)N(CC(=O)C(C)(C)O)Cc3ccc(-c4cccc(C#N)c4)cc3)CC2)cc1 10.1016/j.bmc.2010.09.014
44389526 62904 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCNC2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL179115 62904 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 474 4 1 3 3.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCNC2)C1 10.1016/j.bmcl.2004.12.036
44389375 63987 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 530 7 0 3 5.4 CCCCN1CCC(N(C)C(=O)N2CCC(N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL181176 63987 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 530 7 0 3 5.4 CCCCN1CCC(N(C)C(=O)N2CCC(N(C)C(=O)c3ccc(-c4ccc(C(F)(F)F)cc4)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
44425805 85531 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 564 7 0 5 6.2 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(C)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230307 85531 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 564 7 0 5 6.2 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccc(C)nc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415407 138897 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2ccncc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL379395 138897 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 511 8 1 4 4.3 CN(C(=O)c1ccc(-c2ccncc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
11670645 85361 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 505 8 1 5 5.6 CN(C)Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229512 85361 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 505 8 1 5 5.6 CN(C)Cc1ncc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44417854 80387 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(F)cc(F)c1 10.1016/j.bmcl.2006.07.053
CHEMBL215224 80387 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 380 4 1 2 4.5 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(F)cc(F)c1 10.1016/j.bmcl.2006.07.053
16756638 92784 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cccc(C(F)(F)F)c4)c3)CC2)c1 10.1021/jm060383x
CHEMBL244790 92784 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.5 CC(C)C(=O)Nc1cccc(C2CCN(Cc3cccc(Oc4cccc(C(F)(F)F)c4)c3)CC2)c1 10.1021/jm060383x
52948254 16891 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 556 11 4 7 2.1 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254883 16891 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingDisplacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation counting
ChEMBL 556 11 4 7 2.1 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NC(=O)CN=C(N)N)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
44417853 81113 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 360 5 1 3 3.9 COc1cccc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216056 81113 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 360 5 1 3 3.9 COc1cccc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
44389378 63674 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 568 9 0 4 5.3 CN(C(=O)COc1ccc(C(C)(C)C)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL180717 63674 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 568 9 0 4 5.3 CN(C(=O)COc1ccc(C(C)(C)C)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
50903154 131294 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693993 131294 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 2 1 6 4.2 Cn1c2c(c3ccc(-n4ccc(-c5cnc(C(F)(F)F)nc5)cc4=O)cc31)C1CCC(C2)N1 nan
44388096 63165 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 516 8 2 3 6.5 Cc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.05.039
CHEMBL180009 63165 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 516 8 2 3 6.5 Cc1cccc(NC(=O)NCC(CCN2CCC(N3CCCCC3)CC2)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.05.039
49870579 127605 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665385 127605 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 2 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cn5)cc4=O)nc31)CCNCC2 nan
44416916 80983 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 5 0 4 3.6 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215945 80983 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 490 5 0 4 3.6 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](N5CCOCC5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.049
44430480 87920 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL234929 87920 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 541 4 0 7 4.3 CN(C(=O)N1CC[C@@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@@H]1CCN(C2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
58092292 129246 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 411 4 1 4 4.4 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675286 129246 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 411 4 1 4 4.4 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
49869327 129268 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 2 0 5 5.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCCC1C2 nan
CHEMBL3675306 129268 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 478 2 0 5 5.3 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCCC1C2 nan
44417850 81231 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216362 81231 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 390 6 1 4 3.9 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccc4ccccc4c3)C2)c1 10.1016/j.bmcl.2006.07.053
44424070 85310 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 390 7 0 2 4.9 CN(C)Cc1ccc(CCN(C)C(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
CHEMBL229093 85310 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 390 7 0 2 4.9 CN(C)Cc1ccc(CCN(C)C(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1 10.1016/j.bmc.2006.12.028
44430477 86776 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 569 6 0 7 5.0 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL232823 86776 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 569 6 0 7 5.0 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CCC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
10031575 138716 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 604 6 1 5 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCSC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379002 138716 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 604 6 1 5 7.3 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCSC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44430476 151762 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 555 5 0 7 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL396957 151762 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 555 5 0 7 4.6 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC2CCOCC2)C1 10.1016/j.bmcl.2007.02.012
44397087 66792 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 469 5 0 5 3.4 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(N(C)C)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
CHEMBL187558 66792 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 469 5 0 5 3.4 CN1CC[C@@H](N(C)C(=O)N2CC[C@H](N(C)C(=O)c3ccc(-c4ccc(N(C)C)cc4)s3)C2)C1 10.1016/j.bmcl.2005.05.015
16006977 139620 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 594 9 1 4 5.8 CN(C(=O)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL380307 139620 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 594 9 1 4 5.8 CN(C(=O)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
44424180 141460 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC[C@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL387502 141460 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 510 7 2 4 5.2 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CCC[C@H]4CO)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
11692133 75064 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 520 7 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cc(F)cc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL204161 75064 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 520 7 1 3 5.3 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cc(F)cc(F)c4)C[C@H]23)CC1 10.1021/jm050886n
44194579 18911 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 3 1 5 4.3 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c4c(n(C)c3c2)CCNC4)c(=O)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289278 18911 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 419 3 1 5 4.3 COc1cc(Cl)ccc1-c1ccn(-c2ccc3c4c(n(C)c3c2)CCNC4)c(=O)c1 10.1016/j.bmcl.2010.09.122
46911147 125888 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 433 6 1 5 4.7 COc1cc(-n2ccc(-c3ccc(C(F)(F)F)cc3)cc2=O)ccc1OCC(C)(C)O nan
CHEMBL3651711 125888 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).Radioligand Binding Assay: Compounds were characterized in an in vitro binding assay to determine their Ki or ability to antagonized binding of a peptide agonist to the human melanin concentration hormone receptor (MCHR1).
ChEMBL 433 6 1 5 4.7 COc1cc(-n2ccc(-c3ccc(C(F)(F)F)cc3)cc2=O)ccc1OCC(C)(C)O nan
49868804 127530 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665311 127530 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.1 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
57524505 125856 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 386 4 1 6 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CNCC2 nan
CHEMBL3651066 125856 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 386 4 1 6 2.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc31)CNCC2 nan
44414540 79901 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 459 4 0 5 5.6 Cc1cc(Cl)ccc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
CHEMBL214221 79901 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 459 4 0 5 5.6 Cc1cc(Cl)ccc1-c1ccc2c(=O)c(-c3ccc(N4CCC(N(C)C)C4)nc3)coc2c1 10.1016/j.bmcl.2006.05.075
10217978 140542 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 516 6 2 4 4.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
CHEMBL382631 140542 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 516 6 2 4 4.7 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)c1 10.1021/jm050886n
44399507 124637 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 516 6 2 4 4.7 N#Cc1ccccc1[C@]12CC[C@@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)[C@H]1C2 10.1021/jm049035q
CHEMBL364500 124637 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 516 6 2 4 4.7 N#Cc1ccccc1[C@]12CC[C@@H](N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)[C@H]1C2 10.1021/jm049035q
11420203 67557 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 478 6 2 4 5.1 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1021/jm0503852
CHEMBL191078 67557 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 478 6 2 4 5.1 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(Cl)c3)cc2)c1 10.1021/jm0503852
11752579 67558 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 510 5 1 3 6.9 CCN1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
CHEMBL191079 67558 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 510 5 1 3 6.9 CCN1CCC(N(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
122180707 121239 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Antagonist activity at rat MCHR1 assessed as 6-(4-chlorophenyl)-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-oneAntagonist activity at rat MCHR1 assessed as 6-(4-chlorophenyl)-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one
ChEMBL 513 8 1 9 4.4 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)OC(=O)CN 10.1016/j.bmcl.2015.05.008
CHEMBL3589155 121239 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Antagonist activity at rat MCHR1 assessed as 6-(4-chlorophenyl)-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-oneAntagonist activity at rat MCHR1 assessed as 6-(4-chlorophenyl)-3-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one
ChEMBL 513 8 1 9 4.4 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)OC(=O)CN 10.1016/j.bmcl.2015.05.008
49869072 127543 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 1 4 4.7 CC(C)N1CCc2[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc3c2CC1 nan
CHEMBL3665324 127543 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 1 4 4.7 CC(C)N1CCc2[nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc3c2CC1 nan
49869630 127565 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665346 127565 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CCNCC2 nan
44414391 79772 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 427 5 0 6 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL213641 79772 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 427 5 0 6 4.8 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccccc5)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
44424229 85433 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229871 85433 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 558 6 1 4 5.4 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
16718619 121238 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
CHEMBL3589154 121238 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 456 6 1 7 4.9 COc1cc(-n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)ccc1OCC(C)(C)O 10.1016/j.bmcl.2015.09.018
52949941 18896 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5Cl)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
CHEMBL1289166 18896 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 423 2 1 4 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(Cl)cc5Cl)cc4=O)cc31)CNCC2 10.1016/j.bmcl.2010.09.122
49870323 127582 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 417 4 1 5 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665362 127582 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 417 4 1 5 3.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)cc31)CCNCC2 nan
49870455 127591 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)cc31)CNCCC2 nan
CHEMBL3665371 127591 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 5 4.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)cc31)CNCCC2 nan
44389391 122554 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 626 8 0 3 6.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL360976 122554 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 626 8 0 3 6.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCCc3ccc(Cl)cc3)C2)C1 10.1016/j.bmcl.2004.12.036
11156521 66877 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@H](O)C3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
CHEMBL187931 66877 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@H](O)C3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
49869912 127574 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665355 127574 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cn5)cc4=O)cc31)CCNCC2 nan
50903067 131293 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693992 131293 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 430 4 1 6 3.8 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCC(C2)N1 nan
10159789 60226 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1ccc(F)cc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL175943 60226 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 430 8 2 3 5.2 CN(C)CCC(CNC(=O)Nc1ccc(F)cc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
16006977 139620 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 594 9 1 4 5.8 CN(C(=O)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL380307 139620 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 594 9 1 4 5.8 CN(C(=O)c1ccc(-c2ccc(OC(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
58093333 127597 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 472 5 0 6 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN(C1CCC1)CCC2 nan
CHEMBL3665377 127597 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 472 5 0 6 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN(C1CCC1)CCC2 nan
16755969 91869 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
CHEMBL242902 91869 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 511 10 2 3 6.0 CC(C)C(=O)Nc1cccc(C2CCN(CCCNC(=O)C(C)(c3ccccc3)c3ccccc3)CC2)c1 10.1021/jm060381c
49870181 127630 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 433 4 1 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CNCCC2 nan
CHEMBL3665409 127630 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 433 4 1 5 4.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)cc31)CNCCC2 nan
44424192 85416 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 483 8 1 4 5.9 CC(C)N(CCN(C(=O)Nc1cccc(C#N)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229768 85416 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 483 8 1 4 5.9 CC(C)N(CCN(C(=O)Nc1cccc(C#N)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
52947558 18912 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 3 1 5 4.0 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)c(C)c1 10.1016/j.bmcl.2010.09.122
CHEMBL1289279 18912 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 399 3 1 5 4.0 COc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCNC5)c(=O)c2)c(C)c1 10.1016/j.bmcl.2010.09.122
52941539 18947 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 433 4 0 5 4.6 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1289512 18947 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 433 4 0 5 4.6 CN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
49869914 127576 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)cc31)CCNCC2 nan
CHEMBL3665357 127576 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 435 4 1 5 3.9 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)cc31)CCNCC2 nan
66874257 127619 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665399 127619 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 438 2 1 5 4.4 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)cc5)cc4=O)nc31)CNCCC2 nan
50903065 131290 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
CHEMBL3693989 131290 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 411 4 1 5 4.3 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)C1CCC(C2)N1 nan
44224161 65126 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 389 3 1 3 4.7 CN1CC(c2c[nH]c3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
CHEMBL1830044 65126 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 389 3 1 3 4.7 CN1CC(c2c[nH]c3cc(-n4ccc(-c5ccc(Cl)cc5)cc4=O)ccc23)C1 10.1016/j.bmcl.2011.07.020
44424202 85437 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 547 8 1 2 7.2 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3cccc(Br)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL229877 85437 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 547 8 1 2 7.2 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3cccc(Br)c3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
52944997 19111 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 387 2 0 4 4.1 CN1CCc2c(c3ccc(-n4ccc(-c5ccc(F)cc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1290600 19111 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 387 2 0 4 4.1 CN1CCc2c(c3ccc(-n4ccc(-c5ccc(F)cc5)cc4=O)cc3n2C)C1 10.1016/j.bmcl.2010.09.122
11785262 69036 0 None 1 2 Mouse 8.1 pKi = 8.1 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@@H]2C3)c1 10.1021/jm049035q
CHEMBL193164 69036 0 None 1 2 Mouse 8.1 pKi = 8.1 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@@H]2C3)c1 10.1021/jm049035q
45279233 123071 0 None 1 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 489 6 1 9 3.1 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618348 123071 0 None 1 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 489 6 1 9 3.1 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
11752339 69041 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
CHEMBL193260 69041 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1021/jm049035q
44416989 80486 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 7 1 5 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215308 80486 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 7 1 5 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430495 167066 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 535 4 0 7 4.3 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
CHEMBL430162 167066 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 535 4 0 7 4.3 Cc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)c(C)c1 10.1016/j.bmcl.2007.02.012
16756402 92400 0 None 20 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 398 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL243794 92400 0 None 20 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 398 7 1 3 5.1 CC(=O)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
11409615 141221 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 509 8 2 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL386039 141221 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 509 8 2 5 4.3 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(CO)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
15983864 93485 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 456 9 2 5 4.2 CN(C)CCNCc1ccc(/C=C2\NC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)cc1 10.1016/j.bmcl.2007.04.012
CHEMBL248266 93485 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 456 9 2 5 4.2 CN(C)CCNCc1ccc(/C=C2\NC(=O)N(c3ccc(Oc4ccccc4)cc3)C2=O)cc1 10.1016/j.bmcl.2007.04.012
52944068 19021 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 388 2 0 5 3.5 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(F)cn5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
CHEMBL1290046 19021 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 388 2 0 5 3.5 CN1CCc2c(n(C)c3cc(-n4ccc(-c5ccc(F)cn5)cc4=O)ccc23)C1 10.1016/j.bmcl.2010.09.122
58093391 127636 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 4 1 7 2.7 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CCNCC2 nan
CHEMBL3665415 127636 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 437 4 1 7 2.7 Cn1c2c(c3ccc(-n4ccc(OCc5ncc(F)cc5F)cc4=O)nc31)CCNCC2 nan
57524584 125861 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 455 4 1 7 3.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCC2 nan
CHEMBL3651071 125861 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 455 4 1 7 3.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)nc31)CNCC2 nan
57524587 125865 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 428 4 0 6 3.2 CC(=O)N1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)C1 nan
CHEMBL3651075 125865 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 428 4 0 6 3.2 CC(=O)N1CCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)C1 nan
44416287 138760 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 596 6 1 5 5.7 CS(=O)(=O)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL379201 138760 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 596 6 1 5 5.7 CS(=O)(=O)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
11577708 75190 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 562 8 1 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(S(C)(=O)=O)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL204514 75190 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 562 8 1 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(S(C)(=O)=O)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL4115717 211146 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
44416311 79647 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 579 6 1 3 8.0 O=C(CN1CCc2cc(-c3cccc(F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL213050 79647 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 579 6 1 3 8.0 O=C(CN1CCc2cc(-c3cccc(F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44415467 79655 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 9 1 5 4.7 COC(=O)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213089 79655 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 9 1 5 4.7 COC(=O)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
49869777 127571 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 469 4 1 7 3.4 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665352 127571 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 469 4 1 7 3.4 Cn1c2c(c3ccc(-n4ncc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc31)CCNCC2 nan
44415467 79655 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 9 1 5 4.7 COC(=O)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL213089 79655 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 568 9 1 5 4.7 COC(=O)c1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
50901936 131303 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 472 4 0 6 4.1 CC(=O)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc13)C2 nan
CHEMBL3694008 131303 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 472 4 0 6 4.1 CC(=O)N1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccc(F)cn5)cc4=O)ccc13)C2 nan
44389422 168041 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(C3CCOCC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL436081 168041 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 558 5 0 4 4.8 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(C3CCOCC3)C2)C1 10.1016/j.bmcl.2004.12.036
3575822 153797 2 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 393 9 0 3 6.6 Cc1ccccc1SCN(CCc1ccccc1)CSc1ccccc1C 10.1021/jm070759m
CHEMBL398687 153797 2 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 393 9 0 3 6.6 Cc1ccccc1SCN(CCc1ccccc1)CSc1ccccc1C 10.1021/jm070759m
3787955 154073 12 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 443 8 0 5 4.0 Cc1ccc(S(=O)(=O)CN(Cc2ccccc2)CS(=O)(=O)c2ccc(C)cc2)cc1 10.1021/jm070759m
CHEMBL399303 154073 12 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 443 8 0 5 4.0 Cc1ccc(S(=O)(=O)CN(Cc2ccccc2)CS(=O)(=O)c2ccc(C)cc2)cc1 10.1021/jm070759m
49870682 129245 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 410 2 0 5 4.4 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCC53)c(=O)c2)cn1 nan
CHEMBL3675285 129245 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 410 2 0 5 4.4 Cc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CCN3CCCC53)c(=O)c2)cn1 nan
45278657 123046 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618323 123046 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
44437620 145144 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391618 145144 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437620 145144 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391618 145144 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
44416172 77721 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 589 7 1 4 7.7 O=Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL210167 77721 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 589 7 1 4 7.7 O=Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44416225 137846 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 645 7 1 4 8.8 O=C(CN1CCc2cc(-c3cccc(OC(F)(F)F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL377251 137846 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 645 7 1 4 8.8 O=C(CN1CCc2cc(-c3cccc(OC(F)(F)F)c3)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44416966 140924 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 579 6 0 8 4.5 CS(=O)(=O)N1CCN(Cc2cnc3c(Cn4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
CHEMBL384302 140924 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 579 6 0 8 4.5 CS(=O)(=O)N1CCN(Cc2cnc3c(Cn4cnc5cc(-c6ccc(Cl)cc6)sc5c4=O)cccc3c2)CC1 10.1016/j.bmcl.2006.07.006
12020156 194598 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL562016 194598 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 486 8 1 5 5.4 COc1ccc([C@@H](C)NC(=O)c2ccc(CC3CCN(Cc4ccc5c(c4)OCO5)CC3)cc2)cc1 10.1016/j.ejmech.2009.01.031
44437620 145144 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL391618 145144 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2007.02.049
44437620 145144 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL391618 145144 0 None 11 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 568 12 3 5 5.5 CCC(CO)(CO)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmc.2010.09.014
67970689 125863 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 2 0 6 3.7 CC(=O)N1CCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc3n2C)C1 nan
CHEMBL3651073 125863 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 467 2 0 6 3.7 CC(=O)N1CCc2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)nc3n2C)C1 nan
44414542 79910 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 469 5 0 7 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc6c(c5)CCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
CHEMBL214252 79910 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 469 5 0 7 4.7 CN(C)C1CCN(c2ccc(-c3coc4cc(Oc5ccc6c(c5)CCO6)ccc4c3=O)cn2)C1 10.1016/j.bmcl.2006.05.075
4826270 94123 5 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 368 6 2 6 3.8 Cc1ccccc1Nc1nc(N)nc(CN(C)Cc2cccc(Cl)c2)n1 10.1021/jm070759m
CHEMBL251946 94123 5 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 368 6 2 6 3.8 Cc1ccccc1Nc1nc(N)nc(CN(C)Cc2cccc(Cl)c2)n1 10.1021/jm070759m
16116777 65777 1 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for Melanin-concentrating hormone 1 receptor expressed in CHO cells; Range is 40-79Binding affinity for Melanin-concentrating hormone 1 receptor expressed in CHO cells; Range is 40-79
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1021/jm040762v
CHEMBL184037 65777 1 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for Melanin-concentrating hormone 1 receptor expressed in CHO cells; Range is 40-79Binding affinity for Melanin-concentrating hormone 1 receptor expressed in CHO cells; Range is 40-79
ChEMBL 460 11 1 4 6.0 COc1cc(NC(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1021/jm040762v
44416554 79499 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 437 7 1 5 4.9 CCN1CCN(Oc2ccc(NC(=O)c3ccc(C4CCCCC4)cc3)cc2OC)CC1 10.1016/j.bmcl.2006.06.061
CHEMBL212488 79499 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 437 7 1 5 4.9 CCN1CCN(Oc2ccc(NC(=O)c3ccc(C4CCCCC4)cc3)cc2OC)CC1 10.1016/j.bmcl.2006.06.061
44416584 79844 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 514 10 1 4 7.1 COc1cc(NC(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL213922 79844 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 514 10 1 4 7.1 COc1cc(NC(=O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416968 81112 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 8 4.1 COc1cc(-n2nnc3cc(Oc4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL216054 81112 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 458 8 0 8 4.1 COc1cc(-n2nnc3cc(Oc4ccccc4)ccc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
44416495 141055 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 422 7 1 4 5.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC[C@H]1CCCN1C 10.1016/j.bmcl.2006.06.061
CHEMBL385054 141055 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 422 7 1 4 5.5 COc1cc(NC(=O)c2ccc(C3CCCCC3)cc2)ccc1OC[C@H]1CCCN1C 10.1016/j.bmcl.2006.06.061
44416735 141081 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 462 11 1 5 6.2 COc1cc(NC(=O)c2cccc(Oc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL385253 141081 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 462 11 1 5 6.2 COc1cc(NC(=O)c2cccc(Oc3ccccc3)c2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
10277136 141321 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 11 0 4 6.1 COc1cc(N(C)C(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
CHEMBL386600 141321 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 474 11 0 4 6.1 COc1cc(N(C)C(=O)c2ccc(Cc3ccccc3)cc2)ccc1OCCN(C(C)C)C(C)C 10.1016/j.bmcl.2006.06.056
44416841 79880 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3sc(-c4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
CHEMBL214123 79880 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cellsDisplacement of radiolabeled iodo-MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 447 7 0 7 4.6 COc1cc(-n2cnc3sc(-c4ccccc4)cc3c2=O)ccc1OCCN1CCCC1 10.1016/j.bmcl.2006.06.061
12020168 193147 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 632 8 1 4 6.9 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL539227 193147 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 632 8 1 4 6.9 CC[C@@H](NC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OC(F)(F)O4)CC2)cc1)c1ccc(I)cc1 10.1016/j.ejmech.2009.01.031
44416174 141383 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 612 6 1 4 8.4 O=C(CN1CCc2cc(-c3cccc4cccnc34)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL387025 141383 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 612 6 1 4 8.4 O=C(CN1CCc2cc(-c3cccc4cccnc34)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44416989 80486 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 7 1 5 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
CHEMBL215308 80486 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1 by competitive binding assayBinding affinity to MCHR1 by competitive binding assay
ChEMBL 524 7 1 5 4.3 CCc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@@H](NCC5CCOCC5)C4)C3)s2)cc1 10.1016/j.bmcl.2006.06.049
44430494 86568 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 535 5 0 7 4.2 CCc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
CHEMBL232439 86568 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 535 5 0 7 4.2 CCc1ccc(-c2cc3ncn([C@H]4CCN(C(=O)N(C)[C@H]5CCN(C6CCOCC6)C5)C4)c(=O)c3s2)cc1 10.1016/j.bmcl.2007.02.012
16739310 85590 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 470 4 1 4 5.0 N#Cc1cc(Cl)cc(-c2ccc(CN3CCC4(CC3)C(=O)NC(=O)N4c3ccccc3)cc2)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230627 85590 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 470 4 1 4 5.0 N#Cc1cc(Cl)cc(-c2ccc(CN3CCC4(CC3)C(=O)NC(=O)N4c3ccccc3)cc2)c1 10.1016/j.bmcl.2007.01.104
44425811 96529 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cnccc5OC)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL266513 96529 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 580 8 0 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cnccc5OC)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44415451 79631 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 540 9 1 4 4.9 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL212983 79631 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 540 9 1 4 4.9 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
11533835 76403 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 529 7 2 4 5.0 N#Cc1ccc([C@]23CC[C@@H](N(CCCN4CCNCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1021/jm050886n
CHEMBL206831 76403 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 529 7 2 4 5.0 N#Cc1ccc([C@]23CC[C@@H](N(CCCN4CCNCC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cc1 10.1021/jm050886n
45279488 123044 0 None 2 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 381 4 0 6 3.8 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618321 123044 0 None 2 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 381 4 0 6 3.8 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
58092287 129241 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCCC1C2 nan
CHEMBL3675281 129241 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 0 5 4.4 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CN1CCCC1C2 nan
44415451 79631 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 540 9 1 4 4.9 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
CHEMBL212983 79631 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 540 9 1 4 4.9 COc1ccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N4CC[C@H](NCCCc5ccccc5)C4)C3)cc2)cc1 10.1016/j.bmcl.2006.06.045
66873669 127593 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 4 1 5 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)cc31)CNCCC2 nan
CHEMBL3665373 127593 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 451 4 1 5 4.7 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)cc31)CNCCC2 nan
11719877 85355 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 7 2 4 5.6 NCc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229462 85355 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 476 7 2 4 5.6 NCc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
16756752 142047 0 None 354 3 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)c(Cl)c4)cc3)CC2)c1 10.1021/jm060383x
CHEMBL389129 142047 0 None 354 3 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 496 7 1 3 7.8 CC(C)C(=O)Nc1cccc(C2CCN(Cc3ccc(Oc4ccc(Cl)c(Cl)c4)cc3)CC2)c1 10.1021/jm060383x
11260997 66893 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 525 6 1 4 5.7 CN1CCN(CCN(C(=O)Nc2ccc(C(F)(F)F)c(F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
CHEMBL187996 66893 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 525 6 1 4 5.7 CN1CCN(CCN(C(=O)Nc2ccc(C(F)(F)F)c(F)c2)c2ccc(-c3cccc(C#N)c3)cc2)CC1 10.1021/jm0503852
57524676 125870 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 422 4 1 6 3.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CNCC2 nan
CHEMBL3651080 125870 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 422 4 1 6 3.2 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5F)cc4=O)nc31)CNCC2 nan
49869050 129262 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCC1C2 nan
CHEMBL3675300 129262 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 464 2 0 5 4.9 Cn1c2c(c3ccc(-n4ccc(-c5ccc(C(F)(F)F)nc5)cc4=O)cc31)CN1CCCC1C2 nan
49868915 129252 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCCCN1CC2 nan
CHEMBL3675291 129252 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 458 4 0 6 4.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)C1CCCCN1CC2 nan
11272081 81032 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 504 7 1 5 4.7 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL215964 81032 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 504 7 1 5 4.7 CN1CCN(CCCN(c2nc3cc(F)c(F)cc3[nH]2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@@H]3C2)CC1 10.1016/j.bmcl.2006.07.058
11590806 77899 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 465 4 1 6 4.3 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
CHEMBL210926 77899 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cellsBinding affinity to chimeric rat/human MCH1R stably expressed in HEK293 cells
ChEMBL 465 4 1 6 4.3 CN[C@H]1CCN(c2ccc(-n3ncc4cc(-c5ccc(C(F)(F)F)cc5)ccc4c3=O)cn2)C1 10.1021/jm051263c
52941621 18993 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 401 3 1 5 4.4 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
CHEMBL1289829 18993 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 401 3 1 5 4.4 CSc1ccc(-c2ccn(-c3ccc4c5c(n(C)c4c3)CNCC5)c(=O)c2)cc1 10.1016/j.bmcl.2010.09.122
66898224 127596 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 482 4 0 6 4.7 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665376 127596 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 482 4 0 6 4.7 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(C(F)(F)F)nc5)cc4=O)cc3n2C)C1 nan
49869048 129260 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 1 4 4.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCCN1C3 nan
CHEMBL3675299 129260 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 425 4 1 4 4.8 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCCN1C3 nan
49868780 129270 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 449 2 1 3 5.5 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
CHEMBL3675308 129270 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 449 2 1 3 5.5 O=c1cc(-c2ccc(C(F)(F)F)cc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCCN1C3 nan
44414649 139415 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 596 8 1 5 4.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(S(C)(=O)=O)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL379978 139415 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 596 8 1 5 4.8 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4ccc(S(C)(=O)=O)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
16755971 92136 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 567 14 2 3 7.5 CCCCCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
CHEMBL243507 92136 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cellsDisplacement of [3H]SNAP 7941 from rat MCHR1 expressed in HEK293 cells
ChEMBL 567 14 2 3 7.5 CCCCCC(C(=O)NCCCN1CCC(c2cccc(NC(=O)C(C)C)c2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm060381c
11691555 3717 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 10.1016/j.bmcl.2006.12.080
1319 3717 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 10.1016/j.bmcl.2006.12.080
CHEMBL384701 3717 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 10.1016/j.bmcl.2006.12.080
44417835 81736 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 540 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
CHEMBL216953 81736 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 540 7 1 5 5.2 CN1CCN(CCCN(c2nc3cc(F)c(C(F)(F)F)cc3[nH]2)[C@@H]2CC[C@]3(c4ccc(C#N)cc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.07.058
44414528 138112 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 549 8 1 5 4.8 COc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cn1 10.1016/j.bmcl.2006.05.069
CHEMBL377664 138112 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 549 8 1 5 4.8 COc1ccc([C@]23CC[C@@H](N(CCCN4CCN(C)CC4)C(=O)Nc4ccc(F)c(C(F)(F)F)c4)[C@H]2C3)cn1 10.1016/j.bmcl.2006.05.069
44388442 122593 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 489 9 1 3 6.7 CN(CCCc1ccccc1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
CHEMBL361139 122593 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCHBinding affinity towards human MCH-R1 evaluated by its ability to displace radioligand [125I]Tyr13]-MCH
ChEMBL 489 9 1 3 6.7 CN(CCCc1ccccc1)C1CCN(c2ccc(NC(=O)c3ccc(-c4ccccc4)cc3)cc2)C1 10.1016/j.bmcl.2005.05.130
58093393 127613 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 0 6 3.3 CN1CCc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665393 127613 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 4 0 6 3.3 CN1CCc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
44424224 85330 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 564 6 1 4 6.6 N#Cc1cccc([C@]23CC[C@@H](N(CC4CCN(C5CCOCC5)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL229285 85330 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 564 6 1 4 6.6 N#Cc1cccc([C@]23CC[C@@H](N(CC4CCN(C5CCOCC5)CC4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
44424208 85493 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 512 9 2 4 5.4 CC(C)N(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
CHEMBL229988 85493 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 512 9 2 4 5.4 CC(C)N(CCO)CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1 10.1016/j.bmc.2007.05.068
45279321 123067 0 None 1 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 518 9 1 10 2.4 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618344 123067 0 None 1 2 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 518 9 1 10 2.4 CCS(=O)(=O)C[C@@H](O)COc1ccc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
58093416 127595 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 432 4 0 6 3.8 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
CHEMBL3665375 127595 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 432 4 0 6 3.8 CN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
44414310 137940 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 439 5 0 5 5.2 CCc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
CHEMBL377479 137940 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human MCH1RBinding affinity to human MCH1R
ChEMBL 439 5 0 5 5.2 CCc1ccc(-c2ccc3c(=O)c(-c4ccc(N5CCC(N(C)C)C5)nc4)coc3c2)cc1 10.1016/j.bmcl.2006.05.075
11785262 69036 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@@H]2C3)c1 10.1021/jm049035q
CHEMBL193164 69036 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@@H]2C3)c1 10.1021/jm049035q
49869633 127568 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNCC2 nan
CHEMBL3665349 127568 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 399 4 1 5 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc31)CCNCC2 nan
66874268 127637 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)nc31)CNCCC2 nan
CHEMBL3665416 127637 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 418 4 1 6 3.5 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cc5)cc4=O)nc31)CNCCC2 nan
11648753 140197 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 484 7 1 3 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccccc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL381810 140197 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 484 7 1 3 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccccc4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
44424259 141856 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 649 8 2 6 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL388972 141856 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 649 8 2 6 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cc(Cl)nc(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN5CC[C@H](O)C5)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
11648753 140197 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 484 7 1 3 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccccc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL381810 140197 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 484 7 1 3 5.1 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccccc4)C[C@H]23)CC1 10.1021/jm050886n
11168186 67671 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm049035q
CHEMBL191393 67671 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm049035q
11168186 67671 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2006.12.080
CHEMBL191393 67671 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1016/j.bmcl.2006.12.080
11489130 167650 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
CHEMBL433596 167650 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(C(F)(F)F)c(F)c3)cc2)c1 10.1021/jm0503852
44430479 170284 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 659 7 0 8 5.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)c2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2007.02.012
CHEMBL445407 170284 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 659 7 0 8 5.9 CN(C(=O)N1CC[C@H](n2cnc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1)[C@H]1CCN(CC(=O)c2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2007.02.012
44424235 85181 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 606 7 1 4 6.1 CS(=O)(=O)N1CCC(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL228289 85181 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 606 7 1 4 6.1 CS(=O)(=O)N1CCC(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
44425822 160705 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 642 9 1 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(NS(C)(=O)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL412007 160705 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 642 9 1 6 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(NS(C)(=O)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44416689 80830 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 470 6 2 5 4.3 O=C(NCc1cccc2cc(CN3CCC(O)CC3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
CHEMBL215873 80830 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 470 6 2 5 4.3 O=C(NCc1cccc2cc(CN3CCC(O)CC3)cnc12)c1ccc(-c2ccc(F)cc2)nc1 10.1016/j.bmcl.2006.07.006
44417872 141242 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 340 6 1 4 2.7 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL386163 141242 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 340 6 1 4 2.7 COc1cc(OC)cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c1 10.1016/j.bmcl.2006.07.053
57524846 125880 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 442 4 0 6 3.6 CC(=O)N1Cc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1C nan
CHEMBL3651090 125880 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 442 4 0 6 3.6 CC(=O)N1Cc2c(n(C)c3nc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1C nan
2276336 167106 6 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 408 9 0 7 2.8 COc1ccc(/C=C2/SC(=S)N(CCCC(=O)OCCN(C)C)C2=O)cc1 10.1021/jm070759m
CHEMBL430208 167106 6 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cell membranesDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell membranes
ChEMBL 408 9 0 7 2.8 COc1ccc(/C=C2/SC(=S)N(CCCC(=O)OCCN(C)C)C2=O)cc1 10.1021/jm070759m
44389405 62681 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 635 8 0 5 4.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCS(=O)(=O)N3CCCC3)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178808 62681 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 635 8 0 5 4.1 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCS(=O)(=O)N3CCCC3)C2)C1 10.1016/j.bmcl.2004.12.036
17989439 93148 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 432 9 1 5 5.2 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
CHEMBL246588 93148 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cellsDisplacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
ChEMBL 432 9 1 5 5.2 COc1cc(NC(=O)c2ccc(Oc3ccccc3)cc2)ccc1OCCN1CCCC1 10.1016/j.bmcl.2007.04.012
10007632 79893 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 546 4 1 4 5.9 CC(=O)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL214185 79893 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 546 4 1 4 5.9 CC(=O)N1CCC2(CC1)c1ccc(-c3cccc(C#N)c3)cc1CCN2CC(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
44389440 62163 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 571 5 0 4 4.7 CN1CCC(N2CCC(N(C)C(=O)N3CCC(N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2004.12.036
CHEMBL178147 62163 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 571 5 0 4 4.7 CN1CCC(N2CCC(N(C)C(=O)N3CCC(N(C)C(=O)c4ccc(-c5ccc(C(F)(F)F)cc5)cc4)C3)C2)CC1 10.1016/j.bmcl.2004.12.036
44388201 127284 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 561 7 2 4 5.0 CN(C)S(=O)(=O)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
CHEMBL366445 127284 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 561 7 2 4 5.0 CN(C)S(=O)(=O)N1CCC(CNC(=O)Nc2cc(Cl)cc(Cl)c2)(c2ccc(-c3cccnc3)cc2)CC1 10.1016/j.bmcl.2005.05.085
44417061 96571 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 553 6 1 4 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(Cc2nc4cc(Cl)c(F)cc4[nH]2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL266840 96571 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 553 6 1 4 7.1 N#Cc1cccc(-c2ccc3c(c2)CCN(Cc2nc4cc(Cl)c(F)cc4[nH]2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44425830 85588 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 520 7 0 5 5.4 COc1cccc(N2C(=O)N(CC3CC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230625 85588 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 520 7 0 5 5.4 COc1cccc(N2C(=O)N(CC3CC3)C3(CCN(Cc4ccc(-c5cccc(C#N)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
16756520 92728 0 None 9 2 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 474 9 1 3 6.4 O=C(Cc1ccccc1)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
CHEMBL244372 92728 0 None 9 2 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]T-226296 from rat recombinant MCH1 receptorDisplacement of [3H]T-226296 from rat recombinant MCH1 receptor
ChEMBL 474 9 1 3 6.4 O=C(Cc1ccccc1)Nc1cccc(C2CCN(CCCC(=O)c3ccc(Cl)cc3)CC2)c1 10.1021/jm060383x
44424267 85348 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 461 6 1 3 6.4 Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
CHEMBL229408 85348 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 461 6 1 3 6.4 Cc1ccc(C2=CCC(N(CCN3CCCC3)C(=O)Nc3ccc(F)c(Cl)c3)CC2)s1 10.1016/j.bmc.2007.05.068
44417836 82048 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.6 COc1cc(OC)cc(C(=O)NC2(C)CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL217653 82048 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 418 6 1 4 4.6 COc1cc(OC)cc(C(=O)NC2(C)CCN(Cc3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
45279491 123045 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618322 123045 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3nc(-c4ccc(Cl)cc4)cc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
44416173 140885 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 629 6 1 3 9.2 O=C(CN1CCc2cc(-c3cc(Cl)ccc3Cl)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
CHEMBL384116 140885 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 629 6 1 3 9.2 O=C(CN1CCc2cc(-c3cc(Cl)ccc3Cl)ccc2C1C1CCN(C2CCCC2)CC1)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2006.06.055
45278657 123046 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
CHEMBL3618323 123046 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 382 4 0 7 3.2 COc1ccc(-n2cnn3cc(-c4ccc(Cl)cc4)nc3c2=O)cc1OC 10.1016/j.bmcl.2015.09.018
44425802 142630 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 550 7 0 5 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL389608 142630 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 550 7 0 5 5.9 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccnc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44417842 81723 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 398 4 1 2 4.7 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(F)c(F)c(F)c1 10.1016/j.bmcl.2006.07.053
CHEMBL216828 81723 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 398 4 1 2 4.7 O=C(NC1CCN(Cc2ccc3ccccc3c2)CC1)c1cc(F)c(F)c(F)c1 10.1016/j.bmcl.2006.07.053
44480332 65130 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 419 5 0 4 4.5 Cn1cc(C2CN(CCF)C2)c2ccc(-n3ccc(-c4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmcl.2011.07.020
CHEMBL1830048 65130 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [125I]-S36057 from rat MCH1 receptorDisplacement of [125I]-S36057 from rat MCH1 receptor
ChEMBL 419 5 0 4 4.5 Cn1cc(C2CN(CCF)C2)c2ccc(-n3ccc(-c4ccc(F)cc4)cc3=O)cc21 10.1016/j.bmcl.2011.07.020
11752339 69041 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
CHEMBL193260 69041 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)CC2C3)c1 10.1016/j.bmc.2007.05.068
10239907 138193 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 571 8 1 4 5.9 CC(C)CN1CCN(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL378019 138193 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 571 8 1 4 5.9 CC(C)CN1CCN(CCN(C(=O)Nc2ccc(F)c(C(F)(F)F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)C[C@H]23)CC1 10.1021/jm050886n
45279233 123071 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 489 6 1 9 3.1 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618348 123071 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 489 6 1 9 3.1 COc1cc(-n2cnn3cc(-c4ncc(Cl)cn4)cc3c2=O)ccc1OCC1(O)CC(F)(F)C1 10.1016/j.bmcl.2015.09.018
57524673 125867 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 CC1Cc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)CN1 nan
CHEMBL3651077 125867 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 CC1Cc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)CN1 nan
45279872 123066 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 437 4 1 8 2.8 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618343 123066 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from human MCHR1 expressed in HEK293 cells by scintillation counting analysis
ChEMBL 437 4 1 8 2.8 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
66873409 127621 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 452 4 1 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CNCCC2 nan
CHEMBL3665400 127621 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 452 4 1 6 4.1 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5F)cc4=O)nc31)CNCCC2 nan
11785261 67228 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm049035q
CHEMBL190068 67228 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Inhibition constant for human Melanin concentrating hormone receptor 1Inhibition constant for human Melanin concentrating hormone receptor 1
ChEMBL 496 6 2 4 4.8 N#Cc1cccc([C@]23CC[C@@H](N(CCN4CC[C@@H](O)C4)C(=O)Nc4ccc(F)c(Cl)c4)C[C@H]2C3)c1 10.1021/jm049035q
10297428 61639 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 446 8 2 3 5.7 CN(C)CCC(CNC(=O)Nc1ccc(Cl)cc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
CHEMBL177426 61639 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibitory constant towards Human melanin-concentrating hormone receptorInhibitory constant towards Human melanin-concentrating hormone receptor
ChEMBL 446 8 2 3 5.7 CN(C)CCC(CNC(=O)Nc1ccc(Cl)cc1)c1ccc(-c2cccc(C#N)c2)cc1 10.1016/j.bmcl.2005.05.039
57524673 125867 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 CC1Cc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)CN1 nan
CHEMBL3651077 125867 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 400 4 1 6 3.3 CC1Cc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)nc3n2C)CN1 nan
50903068 131295 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693994 131295 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL4115702 211131 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL None None None None nan
10415704 80719 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 7 1 4 7.2 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL215728 80719 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 572 7 1 4 7.2 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(CC3CC3)CC2)c1 10.1016/j.bmcl.2006.06.055
11613829 76087 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 562 8 1 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(S(C)(=O)=O)cc4)C[C@H]23)CC1 10.1021/jm050886n
CHEMBL205979 76087 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 562 8 1 5 4.5 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4ccc(S(C)(=O)=O)cc4)C[C@H]23)CC1 10.1021/jm050886n
49869351 127557 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 5 0 5 5.1 CC(C)N1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
CHEMBL3665338 127557 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 441 5 0 5 5.1 CC(C)N1CCCc2c(c3ccc(-n4ccc(OCc5ccccc5)cc4=O)cc3n2C)C1 nan
58093338 127598 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 446 5 0 6 4.2 CCN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
CHEMBL3665378 127598 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 446 5 0 6 4.2 CCN1CCCc2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc3n2C)C1 nan
44424209 137050 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@H](C)CO 10.1016/j.bmc.2007.05.068
CHEMBL375520 137050 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 526 9 2 4 5.8 CC(C)N(CCN(C(=O)Nc1ccc(F)c(Cl)c1)[C@@H]1CC[C@]2(c3cccc(C#N)c3)CC2C1)[C@H](C)CO 10.1016/j.bmc.2007.05.068
25057911 18949 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 444 8 0 7 3.5 CO[C@H]1CCN(CCn2ncc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2010.09.039
CHEMBL1289516 18949 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 444 8 0 7 3.5 CO[C@H]1CCN(CCn2ncc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 10.1016/j.bmcl.2010.09.039
49869070 127540 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 0 5 4.3 CCN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
CHEMBL3665321 127540 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 427 5 0 5 4.3 CCN1CCc2c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc23)CC1 nan
58093402 127634 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)nc31)CCNCC2 nan
CHEMBL3665413 127634 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 434 4 1 6 3.6 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(Cl)cc5)cc4=O)nc31)CCNCC2 nan
11511671 140664 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
CHEMBL382841 140664 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to MCHR1Binding affinity to MCHR1
ChEMBL 499 7 2 4 4.7 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(N)c4)C[C@H]23)CC1 10.1016/j.bmcl.2006.05.069
45279872 123066 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 437 4 1 8 2.8 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
CHEMBL3618343 123066 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysisDisplacement of [125I][Phe13,Tyr19]-MCH from rat MCHR1 by scintillation counting analysis
ChEMBL 437 4 1 8 2.8 COc1cc(-n2cnn3cc(-c4ccc(Cl)cn4)cc3c2=O)ccc1N1CC[C@@H](O)C1 10.1016/j.bmcl.2015.09.018
11168186 67671 0 None -2 2 Mouse 8.0 pKi = 8.0 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm049035q
CHEMBL191393 67671 0 None -2 2 Mouse 8.0 pKi = 8.0 Binding
Inhibition constant for mouse Melanin concentrating hormone receptor 1Inhibition constant for mouse Melanin concentrating hormone receptor 1
ChEMBL 512 6 2 4 5.5 N#Cc1cccc(-c2ccc(N(CCN3CC[C@@H](O)C3)C(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc2)c1 10.1021/jm049035q
66886732 127632 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 1 5 3.5 Cn1c2c(c3ccc(-n4ccc(CCc5ccccc5)nc4=O)cc31)CNCCC2 nan
CHEMBL3665411 127632 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 1 5 3.5 Cn1c2c(c3ccc(-n4ccc(CCc5ccccc5)nc4=O)cc31)CNCCC2 nan
58092272 129242 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCC1C2 nan
CHEMBL3675282 129242 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138).
ChEMBL 444 4 0 6 4.0 Cn1c2c(c3ccc(-n4ccc(OCc5ccc(F)cn5)cc4=O)cc31)CN1CCCC1C2 nan
50901931 131300 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 4 0 5 4.6 CN1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3694005 131300 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 425 4 0 5 4.6 CN1C2CCC1c1c(n(C)c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
11758499 157260 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 614 6 1 4 8.5 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL408332 157260 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 614 6 1 4 8.5 N#Cc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44424234 141960 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 6 1 4 4.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cccc(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL389058 141960 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 524 6 1 4 4.7 CS(=O)(=O)N1CCC(CN(C(=O)Nc2cccc(F)c2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
24857597 19052 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 424 5 0 6 4.7 O=c1c2cc(-c3ccccc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
CHEMBL1290266 19052 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]4-(benzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 424 5 0 6 4.7 O=c1c2cc(-c3ccccc3)oc2ccn1-c1ccc2c(cnn2CCN2CCCC2)c1 10.1016/j.bmcl.2010.09.039
9985634 79332 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
CHEMBL211746 79332 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cellsDisplacement of [125I-Tyr13]MCH from human MCHR1 expressed in HEK293 cells
ChEMBL 578 8 1 3 5.9 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)[C@H]1CCN(C(=O)N2CC[C@@H](NCCCc3ccccc3)C2)C1 10.1016/j.bmcl.2006.06.045
49870456 127601 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 5 0 4 4.0 CCN1CCCc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc3n2C)C1 nan
CHEMBL3665381 127601 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 448 5 0 4 4.0 CCN1CCCc2c(c3ccc(N4CCN(CCc5ccc(F)cc5)CC4=O)cc3n2C)C1 nan
50903068 131295 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
CHEMBL3693994 131295 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 397 4 2 4 4.2 O=c1cc(OCc2ccccc2)ccn1-c1ccc2c3c([nH]c2c1)CC1CCC3N1 nan
49870048 127626 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 1 5 3.2 Cn1c2c(c3ccc(-n4ccc(CCc5ccccc5)nc4=O)cc31)CCNCC2 nan
CHEMBL3665405 127626 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 nM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 398 4 1 5 3.2 Cn1c2c(c3ccc(-n4ccc(CCc5ccccc5)nc4=O)cc31)CCNCC2 nan
44424254 85332 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 562 7 2 4 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
CHEMBL229290 85332 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 562 7 2 4 5.0 CS(=O)(=O)N1CCC(CN(C(=O)Nc2ccc(F)c(Cl)c2)[C@@H]2CC[C@]3(c4cccc(CN)c4)CC3C2)CC1 10.1016/j.bmc.2007.05.068
44397227 66816 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1cccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c1 10.1016/j.bmcl.2005.05.015
CHEMBL187660 66816 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurementsBinding affinity towards the human MCH-R1 receptor by displacing [125I]Tyr13]-MCH radioligand in HEK293 cells, Data is average of 3 or more independent measurements
ChEMBL 456 5 0 5 3.3 COc1cccc(-c2ccc(C(=O)N(C)[C@H]3CCN(C(=O)N(C)[C@@H]4CCN(C)C4)C3)s2)c1 10.1016/j.bmcl.2005.05.015
44416929 140895 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 486 5 0 6 6.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1Cc1cccc2cc(CN3CCCC3)cnc12 10.1016/j.bmcl.2006.07.006
CHEMBL384156 140895 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to MCHR1 by radioligand binding assayBinding affinity to MCHR1 by radioligand binding assay
ChEMBL 486 5 0 6 6.0 O=c1c2sc(-c3ccc(Cl)cc3)cc2ncn1Cc1cccc2cc(CN3CCCC3)cnc12 10.1016/j.bmcl.2006.07.006
44425824 54516 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 591 8 0 5 6.7 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(C(C)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL161261 54516 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 591 8 0 5 6.7 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5cccc(C(C)=O)c5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
44424200 85436 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 469 6 2 5 3.8 N#Cc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
CHEMBL229876 85436 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 469 6 2 5 3.8 N#Cc1cccc(NC(=O)N(CCN2CC[C@@H](O)C2)[C@@H]2CC[C@]3(c4cccc(C#N)c4)CC3C2)c1 10.1016/j.bmc.2007.05.068
44424201 142522 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 469 8 1 2 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3ccccc3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
CHEMBL389518 142522 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from MCHR1 expressed in CHO cellsDisplacement of [125I]MCH from MCHR1 expressed in CHO cells
ChEMBL 469 8 1 2 6.4 CC(C)N(CCN(C(=O)Nc1ccc(F)c(F)c1)[C@@H]1CC[C@]2(c3ccccc3)CC2C1)C(C)C 10.1016/j.bmc.2007.05.068
11496824 81160 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 488 7 1 4 4.5 COc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
CHEMBL216286 81160 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 488 7 1 4 4.5 COc1ccc2c(c1)CC(N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(Cl)c1)CC2 10.1016/j.bmcl.2006.12.080
44416275 80804 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 560 5 1 4 6.3 CC(=O)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
CHEMBL215850 80804 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 560 5 1 4 6.3 CC(=O)N1CCC(C2c3ccc(-c4cccc(C#N)c4)cc3CCN2CC(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1016/j.bmcl.2006.06.055
44417891 79927 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(C(F)(F)F)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
CHEMBL214323 79927 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at MCHR1 by flash plate radioligand binding assayBinding affinity at MCHR1 by flash plate radioligand binding assay
ChEMBL 487 8 0 3 4.8 CCN(CC)Cc1ccc2c(c1)CC[C@H](N1CCN(CCc3cccc(C(F)(F)F)c3)CC1=O)C2 10.1016/j.bmc.2006.12.028
44425814 85644 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 549 7 0 4 6.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccccc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
CHEMBL230940 85644 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cellsDisplacement of [125I-Tyr13] from human MCH-R1 expressed in HEK 293 cells
ChEMBL 549 7 0 4 6.5 COc1cccc(N2C(=O)N(Cc3ccccc3F)C3(CCN(Cc4ccc(-c5ccccc5)cc4)CC3)C2=O)c1 10.1016/j.bmcl.2007.01.104
45272985 194034 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.1 Cc1ccccc1CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
CHEMBL557071 194034 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity to MCH1 receptorBinding affinity to MCH1 receptor
ChEMBL 456 7 1 4 5.1 Cc1ccccc1CNC(=O)c1ccc(CC2CCN(Cc3ccc4c(c3)OCO4)CC2)cc1 10.1016/j.ejmech.2009.01.031
57524761 125872 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 5 0 6 4.0 CC(C)N1CCn2c(nc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 nan
CHEMBL3651082 125872 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH-1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro-3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 414 5 0 6 4.0 CC(C)N1CCn2c(nc3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc32)C1 nan
44437526 90986 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240341 90986 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437526 90986 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240341 90986 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
44416223 138717 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 591 7 1 4 7.9 COc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
CHEMBL379004 138717 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human MCHR1Binding affinity to human MCHR1
ChEMBL 591 7 1 4 7.9 COc1cccc(-c2ccc3c(c2)CCN(CC(=O)Nc2cc(Cl)cc(Cl)c2)C3C2CCN(C3CCCC3)CC2)c1 10.1016/j.bmcl.2006.06.055
44437526 90986 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL240341 90986 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2007.02.049
44437526 90986 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL240341 90986 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 555 11 1 4 6.8 CC(=O)OCC(C)(C)NC(=O)N(CCC1CCN(Cc2ccc(C)cc2)CC1)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2010.09.014
44389390 62602 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 518 6 1 4 3.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCO)C2)C1 10.1016/j.bmcl.2004.12.036
CHEMBL178496 62602 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cellsDisplacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells
ChEMBL 518 6 1 4 3.6 CN(C(=O)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1)C1CCN(C(=O)N(C)C2CCN(CCO)C2)C1 10.1016/j.bmcl.2004.12.036
11642491 81156 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 551 8 2 5 3.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(NS(C)(=O)=O)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
CHEMBL216267 81156 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranesInhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
ChEMBL 551 8 2 5 3.9 CN1CCN(CCCN(C(=O)Nc2ccc(F)c(Cl)c2)C2CCc3ccc(NS(C)(=O)=O)cc3C2)CC1 10.1016/j.bmcl.2006.12.080
44437553 90700 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239871 90700 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
44437553 90700 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239871 90700 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
44437553 90700 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
CHEMBL239871 90700 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP from human MCH1 receptor expressed in HEK cellsDisplacement of [3H]SNAP from human MCH1 receptor expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2007.02.049
44437553 90700 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
CHEMBL239871 90700 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cellsDisplacement of [3H]SNAP-7941 from human MCHR1 expressed in HEK cells
ChEMBL 531 10 2 3 6.4 Cc1ccc(CN2CCC(CCN(Cc3ccc(-c4ccc(F)cc4)cc3)C(=O)NC(C)(C)CO)CC2)cc1 10.1016/j.bmc.2010.09.014
50902011 131304 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 4 1 4 4.5 CC(=O)N1C2CCC1c1c([nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
CHEMBL3694009 131304 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 439 4 1 4 4.5 CC(=O)N1C2CCC1c1c([nH]c3cc(-n4ccc(OCc5ccccc5)cc4=O)ccc13)C2 nan
44409689 76401 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 597 7 1 5 4.5 CS(=O)(=O)c1ccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1021/jm050886n
CHEMBL206825 76401 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]MCH from human MCHR1 expressed in CHO cellDisplacement of [125I]MCH from human MCHR1 expressed in CHO cell
ChEMBL 597 7 1 5 4.5 CS(=O)(=O)c1ccc([C@]23CC[C@@H](N(CC4CCN(S(C)(=O)=O)CC4)C(=O)Nc4ccc(F)c(Cl)c4)[C@H]2C3)cc1 10.1021/jm050886n
44389590 62166 0 None - 1 Human 7.0 pKi = 7.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 548 7 2 5 6.1 Cn1c(CN2CCC(CNC(=O)Nc3ccccc3F)(c3ccc(-c4cccnc4)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2005.05.085
CHEMBL178182 62166 0 None - 1 Human 7.0 pKi = 7.0 Binding
Ability to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cellsAbility to displace [125I]-MCH()0.5 nM from human MCH1R(2.5 uM) expressed in CHO cells
ChEMBL 548 7 2 5 6.1 Cn1c(CN2CCC(CNC(=O)Nc3ccccc3F)(c3ccc(-c4cccnc4)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2005.05.085
11306487 66824 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 1 4 6.7 COc1cccc(NC(=O)N(c2ccc(-c3cccc(C#N)c3)cc2)C2CCN(C3CCCC3)CC2)c1 10.1021/jm0503852
CHEMBL187719 66824 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of human melanin concentrating hormone receptor 1Inhibition of human melanin concentrating hormone receptor 1
ChEMBL 494 6 1 4 6.7 COc1cccc(NC(=O)N(c2ccc(-c3cccc(C#N)c3)cc2)C2CCN(C3CCCC3)CC2)c1 10.1021/jm0503852
11202371 84642 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 362 5 1 2 3.9 O=C(Cc1ccccc1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
CHEMBL224519 84642 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 362 5 1 2 3.9 O=C(Cc1ccccc1)NC1CCN(Cc2ccc(Cl)c(Cl)c2)C1 10.1021/jm040084c
11192042 136812 0 None - 1 Rat 5.0 pKi = 5.0 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 432 6 1 3 5.5 O=C(Cc1csc2ccccc12)NC[C@H]1CCCN1Cc1ccc(Cl)c(Cl)c1 10.1021/jm040084c
CHEMBL375291 136812 0 None - 1 Rat 5.0 pKi = 5.0 Binding
Binding affinity to rat MCH1 receptorBinding affinity to rat MCH1 receptor
ChEMBL 432 6 1 3 5.5 O=C(Cc1csc2ccccc12)NC[C@H]1CCCN1Cc1ccc(Cl)c(Cl)c1 10.1021/jm040084c
50902015 124094 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 449 4 1 5 3.5 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)nc31)C1CCC(C2)N1 nan
CHEMBL3640816 124094 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.Binding Assay: Evaluation of the affinity of compounds for the human MCH-1 receptor was accomplished using 4-(3,4,5-tritritiumbenzyloxy)-1-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-5-yl)pyridin-2(1H)-one and membranes prepared from stable CHO-K1 cells expressing the human MCH1 receptor obtained from Euroscreen (Batch 1138). Cell membrane homogenates (8.92 μg protein) were incubated for 60 min at 25° C. with 1.4 μM of the [3H]-labeled compound in the absence or presence of the test compound in 50 mM Tris-HCl buffer, pH 7.4. Nonspecific binding was determined in the presence of 50 μM 1-(5-(4-cyanophenyl)bicyclo[3.1.0]hexan-2-yl)-3-(4-fluoro 3-(trifluoromethyl)phenyl)-1-(3-(4-methylpiperazin-1-yl)propyl)urea. Following incubation, the samples were filtered rapidly under vacuum through Skatron 11731 filters, pre-soaked in 0.5% polyethylenimine, and washed with ice-cold 50 mM Tris-HCl buffer, pH 7.4, (wash setting 9,9,0) using a Skatron cell harvester.
ChEMBL 449 4 1 5 3.5 Cn1c2c(c3ccc(N4CCN(CCc5ccc(Cl)cc5)CC4=O)nc31)C1CCC(C2)N1 nan
44418000 141390 0 None - 1 Human 7.0 pKi = 7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 434 7 1 5 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4cc(OC)ccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
CHEMBL387065 141390 0 None - 1 Human 7.0 pKi = 7 Binding
Binding activity against human MCH-R1Binding activity against human MCH-R1
ChEMBL 434 7 1 5 4.3 COc1cc(OC)cc(C(=O)NC2CCN(Cc3ccc4cc(OC)ccc4c3)CC2)c1 10.1016/j.bmcl.2006.07.053
25206298 19072 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 432 6 0 6 4.1 COc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)c(F)c1 10.1016/j.bmcl.2010.09.037
CHEMBL1290379 19072 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cellsDisplacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells
ChEMBL 432 6 0 6 4.1 COc1ccc(-c2ccn(-c3ccc4c(cnn4CCN4CCCC4)c3)c(=O)c2)c(F)c1 10.1016/j.bmcl.2010.09.037
11520239 3562 4 None 2 4 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
1313 3562 4 None 2 4 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
CHEMBL185271 3562 4 None 2 4 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 613 10 3 7 4.0 COCC1=C(C(=O)OC)[C@@H](N(C(=O)N1)C(=O)NCCCN1CCC(CC1)c1cccc(c1)NC(=O)C)c1ccc(c(c1)F)F 12118247
1311 3378 0 None - 1 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19619599
1295 3374 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
155817404 3374 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1298 2439 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
1298 2439 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
16167454 2439 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
16167454 2439 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
91898993 2439 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
91898993 2439 0 None 1 2 Human 10.1 pKi None 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1294 3373 0 None -1 2 Rat 10.2 pKi None 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1294 3373 0 None 1 2 Human 10.3 pKi None 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1302 3900 0 None - 1 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
155817405 3900 0 None - 1 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
1295 3374 0 None 1 2 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
155817404 3374 0 None 1 2 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1309 3376 0 None - 1 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1308 3375 0 None - 1 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1312 3458 0 None - 1 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 472 9 1 4 5.6 CCNCCOc1ccc(cc1OC)N(C(=O)c1ccc(cc1)c1ccc(cc1)C(F)(F)F)C 16839763
16046160 3458 0 None - 1 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 472 9 1 4 5.6 CCNCCOc1ccc(cc1OC)N(C(=O)c1ccc(cc1)c1ccc(cc1)C(F)(F)F)C 16839763
11238212 507 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 551 8 2 6 5.9 Brc1ccc(c(c1)OC(F)(F)F)CCN[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
1304 507 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 551 8 2 6 5.9 Brc1ccc(c(c1)OC(F)(F)F)CCN[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 15677346
1310 3377 0 None - 1 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1291 751 0 None - 1 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
268 751 0 None - 1 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
11691555 3717 0 None - 1 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 17251014
1319 3717 0 None - 1 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 17251014
CHEMBL384701 3717 0 None - 1 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 483 6 1 4 4.4 N#Cc1ccc2c(c1)CC(CC2)N(C(=O)Nc1ccc(c(c1)Cl)F)CCCN1CCN(CC1)C 17251014
1297 3042 0 None - 1 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
101600353 2425 0 None -1 2 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1301 2425 0 None -1 2 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
134824567 2425 0 None -1 2 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
16207764 2425 0 None -1 2 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
101110542 2426 0 None -1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1293 2426 0 None -1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
101600353 2425 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
101600353 2425 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
1301 2425 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
1301 2425 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
134824567 2425 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
134824567 2425 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
16207764 2425 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10421367
16207764 2425 0 None 1 2 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11375253
101110542 2426 0 None 1 2 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1293 2426 0 None 1 2 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
1298 2439 0 None -1 2 Rat 9.9 pKi None 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
16167454 2439 0 None -1 2 Rat 9.9 pKi None 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073
91898993 2439 0 None -1 2 Rat 9.9 pKi None 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11561073