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
CHEMBL218994 207648 0 None 1 2 Rat 10.0 pEC50 = 10 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1165734 206775 0 None - 1 Rat 10.0 pEC50 = 10.0 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1163460 206766 0 None - 1 Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1163463 206767 6 None - 1 Rat 9.8 pEC50 = 9.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL390094 210680 1 None - 1 Rat 9.6 pEC50 = 9.6 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL1163467 206768 0 None - 1 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1165797 206782 0 None - 1 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL1165767 206778 0 None - 1 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None C[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](C)C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
44189349 181203 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1059 18 13 14 -0.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4777970 181203 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1059 18 13 14 -0.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL577772 213990 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL577772 213990 0 None - 1 Rat 9.3 pEC50 = 9.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm900683d
CHEMBL1165735 206776 0 None - 1 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL504097 212393 0 None - 1 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL1163473 206770 0 None - 1 Rat 9.1 pEC50 = 9.1 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
162650062 179500 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 944 14 11 12 0.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4748168 179500 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 944 14 11 12 0.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL437430 211960 0 None -3 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1016/j.bmc.2009.07.058
145965592 163853 0 None 33 2 Rat 9.0 pEC50 = 9.0 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 163853 0 None 33 2 Rat 9.0 pEC50 = 9.0 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145973990 164122 0 None 181 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164122 0 None 181 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL524855 213836 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H]2Cc3ccccc3CN2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL510618 213799 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
162646037 178924 0 None 1737 6 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4741230 178924 0 None 1737 6 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL1165796 206781 0 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL1165793 206779 0 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm901294u
CHEMBL1165794 206780 1 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL2372899 208549 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)N)[C@@H](C)O)C(=O)O 10.1021/jm0111043
CHEMBL385616 210601 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H](N)CCC(=O)O)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(=O)O 10.1021/jm0111043
CHEMBL53181 213921 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
CHEMBL2372897 208548 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
145967082 163538 0 None 416 2 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 163538 0 None 416 2 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162663320 181425 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1072 19 13 14 -0.4 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4780734 181425 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1072 19 13 14 -0.4 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
162648628 179265 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 897 24 13 11 -0.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4745321 179265 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 897 24 13 11 -0.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL593663 214027 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmc.2009.07.058
162644923 178839 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 911 25 12 11 -0.1 COc1ccc(C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](CS)C(N)=O)cc1 10.1021/acs.jmedchem.6b00164
CHEMBL4740325 178839 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 911 25 12 11 -0.1 COc1ccc(C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](CS)C(N)=O)cc1 10.1021/acs.jmedchem.6b00164
145978068 163173 0 None 1 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163173 0 None 1 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145973104 164166 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164166 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL406590 210858 0 None - 1 Human 6.0 pEC50 = 6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
CHEMBL505358 212411 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2cccc3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
162655718 180105 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 884 23 13 11 0.1 C[C@@H](O)[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4755542 180105 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 884 23 13 11 0.1 C[C@@H](O)[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
24953411 13954 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197619 13954 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL578654 13954 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
162668637 182055 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4788762 182055 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
24952710 13939 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197510 13939 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL574732 13939 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
24953059 13936 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197507 13936 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL574726 13936 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
162660425 180706 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1044 29 14 13 -0.1 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4762329 180706 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1044 29 14 13 -0.1 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
145977223 163427 0 None 1 2 Rat 7.0 pEC50 = 7.0 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163427 0 None 1 2 Rat 7.0 pEC50 = 7.0 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
2151 242 6 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1016/j.bmc.2010.04.041
9797568 242 6 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1016/j.bmc.2010.04.041
CHEMBL192359 242 6 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1016/j.bmc.2010.04.041
15983447 85206 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 412 8 1 2 5.1 CN(C)CCC(NC(=O)CCc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228413 85206 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 412 8 1 2 5.1 CN(C)CCC(NC(=O)CCc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
15983564 85225 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 378 7 1 2 4.4 Cc1ccc(C(CCN(C)C)NC(=O)Cc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228525 85225 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 378 7 1 2 4.4 Cc1ccc(C(CCN(C)C)NC(=O)Cc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
10407901 10728 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 387 6 0 4 5.0 CN(C)CCC1(c2ccc(Oc3ccccc3)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1172234 10728 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 387 6 0 4 5.0 CN(C)CCC1(c2ccc(Oc3ccccc3)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
49799325 14253 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 379 4 0 3 5.1 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccc3ccccc3c2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1173106 14253 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 379 4 0 3 5.1 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccc3ccccc3c2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200251 14253 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 379 4 0 3 5.1 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccc3ccccc3c2C(=O)O1 10.1016/j.bmc.2010.04.041
145967082 163538 0 None -416 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 163538 0 None -416 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145977223 163427 0 None 1 2 Rat 6.9 pEC50 = 6.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163427 0 None 1 2 Rat 6.9 pEC50 = 6.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
46897997 14236 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 5 0 3 3.8 COc1cccc2c1CC(CCN(C)C)(c1ccc(Cl)cc1)N(C)C2=O 10.1016/j.bmc.2010.04.041
CHEMBL1172407 14236 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 5 0 3 3.8 COc1cccc2c1CC(CCN(C)C)(c1ccc(Cl)cc1)N(C)C2=O 10.1016/j.bmc.2010.04.041
CHEMBL1200175 14236 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 5 0 3 3.8 COc1cccc2c1CC(CCN(C)C)(c1ccc(Cl)cc1)N(C)C2=O 10.1016/j.bmc.2010.04.041
145965592 163853 0 None 33 2 Rat 7.9 pEC50 = 7.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 163853 0 None 33 2 Rat 7.9 pEC50 = 7.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL607810 214046 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1016/j.bmc.2009.07.058
145977587 163123 0 None 14 2 Rat 7.9 pEC50 = 7.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163123 0 None 14 2 Rat 7.9 pEC50 = 7.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24954831 13934 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197503 13934 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL574527 13934 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
145977223 163427 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163427 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145977223 163427 0 None 1 2 Rat 6.9 pEC50 = 6.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-9M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-9M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163427 0 None 1 2 Rat 6.9 pEC50 = 6.9 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-9M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-9M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145965592 163853 0 None -33 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 163853 0 None -33 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24953055 13923 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197455 13923 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572883 13923 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
11983241 85214 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 410 7 1 2 5.2 CN(C)CCC(NC(=O)/C=C/c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228470 85214 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 410 7 1 2 5.2 CN(C)CCC(NC(=O)/C=C/c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL607811 214047 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmc.2009.07.058
145977587 163123 0 None 14 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163123 0 None 14 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372905 208555 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
11325792 139624 8 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 357 4 0 3 4.5 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)cc1)C2 10.1016/j.bmc.2010.04.041
CHEMBL380346 139624 8 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 357 4 0 3 4.5 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)cc1)C2 10.1016/j.bmc.2010.04.041
15983822 85405 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 426 7 1 2 5.7 CN(C)CCC(NC(=O)/C=C/c1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL229713 85405 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 426 7 1 2 5.7 CN(C)CCC(NC(=O)/C=C/c1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
162666444 181680 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 744 20 10 9 0.7 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4783832 181680 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 744 20 10 9 0.7 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
49799029 14256 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 371 5 0 3 4.9 CN(C)CCC1(c2cccc(-c3ccccc3)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1173147 14256 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 371 5 0 3 4.9 CN(C)CCC1(c2cccc(-c3ccccc3)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200258 14256 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 371 5 0 3 4.9 CN(C)CCC1(c2cccc(-c3ccccc3)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
15983820 161186 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 390 9 1 3 4.6 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL413787 161186 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 390 9 1 3 4.6 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2006.09.015
162664787 181622 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 895 24 13 11 -1.0 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4783104 181622 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 895 24 13 11 -1.0 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104471 209307 5 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
44409467 74391 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL203080 74391 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572699 74391 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
49799289 14266 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 5.0 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc3ccccc3c1)C2 10.1016/j.bmc.2010.04.041
CHEMBL1173399 14266 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 5.0 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc3ccccc3c1)C2 10.1016/j.bmc.2010.04.041
CHEMBL1200283 14266 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 5.0 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc3ccccc3c1)C2 10.1016/j.bmc.2010.04.041
145966260 163823 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 163823 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372904 208554 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
145977223 163427 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163427 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162671682 182297 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 942 25 13 13 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4792095 182297 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 942 25 13 13 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
15983443 136797 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.7 COc1ccc(CC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL375275 136797 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.7 COc1ccc(CC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
15983686 137545 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 322 7 1 2 3.8 Cc1ccc(C(CCN(C)C)NC(=O)/C=C/c2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL376582 137545 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 322 7 1 2 3.8 Cc1ccc(C(CCN(C)C)NC(=O)/C=C/c2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
162649626 179477 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1072 31 15 14 -1.8 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4747883 179477 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1072 31 15 14 -1.8 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
145977223 163427 0 None 1 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163427 0 None 1 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-7M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL608099 214050 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.07.058
15983445 85205 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 344 8 1 2 4.1 CN(C)CCC(NC(=O)CCc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228412 85205 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 344 8 1 2 4.1 CN(C)CCC(NC(=O)CCc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
145973990 164122 0 None 181 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164122 0 None 181 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
49798987 14240 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 5 0 4 4.2 COc1ccc2c(c1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1172604 14240 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 5 0 4 4.2 COc1ccc2c(c1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1200193 14240 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 5 0 4 4.2 COc1ccc2c(c1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
15983693 168816 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 346 7 1 2 4.2 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL442230 168816 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 346 7 1 2 4.2 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
162669582 182137 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 641 17 8 7 1.3 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4789784 182137 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 641 17 8 7 1.3 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00164
145973104 164166 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164166 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
11524599 76359 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 330 7 1 2 3.7 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL206596 76359 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 330 7 1 2 3.7 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
145978068 163173 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163173 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372903 208553 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
49799280 14260 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 1 3 3.6 CNCCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1173239 14260 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 1 3 3.6 CNCCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200268 14260 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 1 3 3.6 CNCCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
24954830 13917 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197440 13917 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572398 13917 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmc.2009.04.062
15983690 85475 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 352 8 1 3 3.8 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229924 85475 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 352 8 1 3 3.8 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL1163471 206769 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL298803 209149 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/jm0111043
CHEMBL427632 211600 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](N)[C@@H](C)O)C(=O)O 10.1021/jm0111043
CHEMBL408106 210944 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
CHEMBL426020 211585 0 None - 1 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL2372896 208547 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](C)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
145967082 163538 0 None 416 2 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 163538 0 None 416 2 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL608098 214049 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.07.058
162662463 181441 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 744 20 10 9 0.7 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4780893 181441 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 744 20 10 9 0.7 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00164
24795079 13924 4 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197471 13924 4 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL573392 13924 4 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
46897998 14225 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 370 5 0 2 4.6 CC(C)N1C(=O)c2ccccc2CC1(CCN(C)C)c1ccc(Cl)cc1 10.1016/j.bmc.2010.04.041
CHEMBL1172180 14225 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 370 5 0 2 4.6 CC(C)N1C(=O)c2ccccc2CC1(CCN(C)C)c1ccc(Cl)cc1 10.1016/j.bmc.2010.04.041
CHEMBL1200148 14225 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 370 5 0 2 4.6 CC(C)N1C(=O)c2ccccc2CC1(CCN(C)C)c1ccc(Cl)cc1 10.1016/j.bmc.2010.04.041
46897996 14234 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 342 4 0 2 3.8 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)N1C 10.1016/j.bmc.2010.04.041
CHEMBL1172224 14234 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 342 4 0 2 3.8 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)N1C 10.1016/j.bmc.2010.04.041
CHEMBL1200156 14234 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 342 4 0 2 3.8 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)N1C 10.1016/j.bmc.2010.04.041
15983570 85431 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 392 8 1 2 4.8 Cc1ccc(C(CCN(C)C)NC(=O)CCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229868 85431 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 392 8 1 2 4.8 Cc1ccc(C(CCN(C)C)NC(=O)CCc2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
162670598 182330 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4792481 182330 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL2372895 208546 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
49799327 14257 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 390 9 0 4 4.4 C=CCN(CC=C)c1cccc(C2(CCN(C)C)Cc3ccccc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1173170 14257 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 390 9 0 4 4.4 C=CCN(CC=C)c1cccc(C2(CCN(C)C)Cc3ccccc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1200259 14257 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 390 9 0 4 4.4 C=CCN(CC=C)c1cccc(C2(CCN(C)C)Cc3ccccc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
162677235 182903 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4799581 182903 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
2151 242 6 None -2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm901294u
9797568 242 6 None -2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm901294u
CHEMBL192359 242 6 None -2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm901294u
CHEMBL1163477 206772 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
46897995 14233 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 4 0 2 5.4 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc3ccccc3c1)OC2 10.1016/j.bmc.2010.04.041
CHEMBL1172223 14233 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 4 0 2 5.4 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc3ccccc3c1)OC2 10.1016/j.bmc.2010.04.041
CHEMBL1200155 14233 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 4 0 2 5.4 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc3ccccc3c1)OC2 10.1016/j.bmc.2010.04.041
145966260 163823 0 None -2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 163823 0 None -2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24955192 13933 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL1197496 13933 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL574305 13933 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
145977223 163427 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163427 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
49799291 14267 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 353 5 0 4 3.9 COc1cccc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1173400 14267 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 353 5 0 4 3.9 COc1cccc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1200284 14267 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 353 5 0 4 3.9 COc1cccc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
162653594 179946 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1095 31 15 14 -0.7 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4753729 179946 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1095 31 15 14 -0.7 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
49799368 14245 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2cccc(Br)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1172764 14245 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2cccc(Br)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200219 14245 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2cccc(Br)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
15983449 85213 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 374 9 1 3 4.1 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228461 85213 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 374 9 1 3 4.1 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
10213684 3860 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
2152 3860 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
CHEMBL414256 3860 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None None 10.1021/jm0111043
CHEMBL2372907 208556 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None C[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
145977587 163123 0 None 14 2 Rat 8.5 pEC50 = 8.5 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163123 0 None 14 2 Rat 8.5 pEC50 = 8.5 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372902 208552 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@@H](N)CCC(=O)O)C(=O)O 10.1021/jm0111043
CHEMBL1627325 207058 0 None -102 8 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in CHO cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilizationAntagonist activity at human recombinant urotensin 2 receptor expressed in CHO cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization
ChEMBL None None None CSCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(C)(C)C)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)O)[C@@H](C)O 10.1021/jm900604g
162657061 180308 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4757669 180308 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL216349 207571 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1)C(=O)O 10.1021/jm0111043
CHEMBL3104471 209307 5 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
10996495 179322 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 845 11 10 11 0.7 NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/acs.jmedchem.6b00164
CHEMBL4746051 179322 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 845 11 10 11 0.7 NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/acs.jmedchem.6b00164
CHEMBL385962 210613 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
162649156 179238 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1045 17 13 14 -0.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4745061 179238 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1045 17 13 14 -0.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
2151 242 6 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm049110x
9797568 242 6 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm049110x
CHEMBL192359 242 6 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm049110x
24952707 13915 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197438 13915 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572391 13915 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
15983691 85379 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 320 5 1 2 3.2 Cc1ccc(C(CCN(C)C)NC(=O)C#Cc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229659 85379 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 320 5 1 2 3.2 Cc1ccc(C(CCN(C)C)NC(=O)C#Cc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL1163475 206771 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
145973104 164166 0 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164166 0 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
45481596 13948 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 8 1 2 5.8 CN(C)CCCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197565 13948 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 8 1 2 5.8 CN(C)CCCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL576746 13948 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 8 1 2 5.8 CN(C)CCCC(NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
11696838 76788 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL207823 76788 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573857 76788 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
145966260 163823 0 None 2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 163823 0 None 2 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162659637 180701 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1058 30 14 13 -0.0 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4762272 180701 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1058 30 14 13 -0.0 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
162644289 181199 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 977 25 14 13 -1.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c(S(=O)(=O)O)c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4777923 181199 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 977 25 14 13 -1.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c(S(=O)(=O)O)c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
145973990 164122 0 None -181 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164122 0 None -181 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24953056 13943 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197533 13943 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL575629 13943 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 402 8 1 3 5.1 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(C)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
145965592 163853 0 None -33 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 163853 0 None -33 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24953060 13918 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197441 13918 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL572423 13918 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
145977223 163427 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-10M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-10M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163427 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-10M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in URP-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 3 x 10'-10M pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.16 +/- 0.08 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145977587 163123 0 None -14 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163123 0 None -14 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145967082 163538 0 None -416 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 163538 0 None -416 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145978068 163173 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163173 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24952352 13929 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197480 13929 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573575 13929 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1cccc(-c2ccc3ccccc3c2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1163479 206773 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
15983818 85404 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 428 8 1 2 5.6 CN(C)CCC(NC(=O)CCc1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL229710 85404 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 428 8 1 2 5.6 CN(C)CCC(NC(=O)CCc1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
145973990 164122 0 None -181 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164122 0 None -181 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
15983826 85406 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 388 8 1 3 4.7 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229714 85406 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 388 8 1 3 4.7 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2006.09.015
24953414 13931 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 330 7 1 2 4.2 CN(C)CCCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197484 13931 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 330 7 1 2 4.2 CN(C)CCCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573836 13931 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 330 7 1 2 4.2 CN(C)CCCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
49799486 14273 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 344 4 0 2 4.0 C[N+](C)(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1173689 14273 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 344 4 0 2 4.0 C[N+](C)(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200298 14273 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 344 4 0 2 4.0 C[N+](C)(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
15983560 85215 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 340 5 1 2 3.5 CN(C)CCC(NC(=O)C#Cc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228471 85215 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 340 5 1 2 3.5 CN(C)CCC(NC(=O)C#Cc1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL593662 214026 9 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in CHO cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilizationAntagonist activity at human recombinant urotensin 2 receptor expressed in CHO cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900604g
162651887 179681 0 None 112 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4750625 179681 0 None 112 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
162645261 179095 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1091 18 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4743591 179095 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1091 18 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
10474282 68755 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 369 7 0 3 5.1 CCN(CC)CCC1C(c2ccccc2)=NN(C)C1c1ccc(Cl)cc1 10.1021/jm049110x
CHEMBL192389 68755 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 369 7 0 3 5.1 CCN(CC)CCC1C(c2ccccc2)=NN(C)C1c1ccc(Cl)cc1 10.1021/jm049110x
49798794 14204 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 355 6 0 3 4.5 C=CCN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1170888 14204 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 355 6 0 3 4.5 C=CCN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200021 14204 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 355 6 0 3 4.5 C=CCN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
15983562 85216 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 310 7 1 2 3.3 Cc1ccc(C(CCN(C)C)NC(=O)Cc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228472 85216 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 310 7 1 2 3.3 Cc1ccc(C(CCN(C)C)NC(=O)Cc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
16126405 136641 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 342 7 1 2 4.2 CN(C)CCC(NC(=O)/C=C/c1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL374817 136641 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 342 7 1 2 4.2 CN(C)CCC(NC(=O)/C=C/c1ccccc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
24953410 13919 4 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197442 13919 4 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL572439 13919 4 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
24952350 13964 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197698 13964 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL582835 13964 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
15983688 85474 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 390 7 1 2 4.8 Cc1ccc(C(CCN(C)C)NC(=O)/C=C/c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229923 85474 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 390 7 1 2 4.8 Cc1ccc(C(CCN(C)C)NC(=O)/C=C/c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.ejmech.2006.09.015
45481598 13930 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197481 13930 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL573640 13930 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 442 7 1 2 6.6 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
16126557 85414 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 356 5 1 2 4.0 CN(C)CCC(NC(=O)C#Cc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL229764 85414 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 356 5 1 2 4.0 CN(C)CCC(NC(=O)C#Cc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
15983568 137543 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 324 8 1 2 3.7 Cc1ccc(C(CCN(C)C)NC(=O)CCc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL376581 137543 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 324 8 1 2 3.7 Cc1ccc(C(CCN(C)C)NC(=O)CCc2ccccc2)cc1 10.1016/j.ejmech.2006.09.015
145965592 163853 0 None -33 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213538 163853 0 None -33 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145973104 164166 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164166 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL437430 211960 0 None 3 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL452403 212219 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
145973990 164122 0 None 181 2 Rat 8.3 pEC50 = 8.3 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164122 0 None 181 2 Rat 8.3 pEC50 = 8.3 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL2372901 208551 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
162666856 181882 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 909 25 13 11 -0.9 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4786585 181882 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 909 25 13 11 -0.9 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
10340786 70957 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 397 7 1 2 5.2 CCN(CC)CCC1=C(c2ccccc2)NC(=O)N(C)C1c1ccc(Cl)cc1 10.1021/jm049110x
CHEMBL195746 70957 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 397 7 1 2 5.2 CCN(CC)CCC1=C(c2ccccc2)NC(=O)N(C)C1c1ccc(Cl)cc1 10.1021/jm049110x
46897993 14259 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 0 2 4.3 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2CO1 10.1016/j.bmc.2010.04.041
CHEMBL1173172 14259 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 0 2 4.3 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2CO1 10.1016/j.bmc.2010.04.041
CHEMBL1200261 14259 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 315 4 0 2 4.3 CN(C)CCC1(c2ccc(Cl)cc2)Cc2ccccc2CO1 10.1016/j.bmc.2010.04.041
44409548 76961 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL208362 76961 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL573837 76961 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
46897999 14224 2 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 391 4 0 3 5.2 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2010.04.041
CHEMBL1171808 14224 2 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 391 4 0 3 5.2 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2010.04.041
CHEMBL1200120 14224 2 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 391 4 0 3 5.2 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2010.04.041
15983558 141489 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 372 8 1 3 4.2 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL387661 141489 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 372 8 1 3 4.2 COc1ccc(/C=C/C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2006.09.015
24953412 13955 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197628 13955 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL578853 13955 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 458 7 1 2 7.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc3ccccc3c2)cc1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
49799329 14258 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 383 6 0 5 3.9 COc1cc(OC)cc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1173171 14258 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 383 6 0 5 3.9 COc1cc(OC)cc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL1200260 14258 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 383 6 0 5 3.9 COc1cc(OC)cc(C2(CCN(C)C)Cc3cc(C)c(C)cc3C(=O)O2)c1 10.1016/j.bmc.2010.04.041
CHEMBL412753 211266 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Mobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptorMobilization of intracellular calcium in CHO cells transiently transfected with human Urotensin 2 receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)O 10.1021/jm0111043
145977587 163123 0 None -14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163123 0 None -14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
24953058 13945 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL1197539 13945 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
CHEMBL575819 13945 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 408 7 1 2 5.9 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc2ccccc2c1 10.1016/j.bmc.2009.04.062
15983684 85473 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 354 9 1 3 3.7 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL229922 85473 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 354 9 1 3 3.7 COc1ccc(CCC(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
24952349 13927 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197478 13927 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573570 13927 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(C)CCC(NC(=O)c1cccc(-c2ccccc2)c1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
24952351 13937 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197508 13937 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL574730 13937 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
15983695 144072 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 414 7 1 2 5.2 CN(C)CCC(NC(=O)Cc1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL390792 144072 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 414 7 1 2 5.2 CN(C)CCC(NC(=O)Cc1ccc(C(F)(F)F)cc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
15983824 141492 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 358 7 1 2 4.7 CN(C)CCC(NC(=O)/C=C/c1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL387694 141492 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 358 7 1 2 4.7 CN(C)CCC(NC(=O)/C=C/c1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
15983566 85226 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 340 8 1 3 3.4 COc1ccc(CC(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228526 85226 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 340 8 1 3 3.4 COc1ccc(CC(=O)NC(CCN(C)C)c2ccc(C)cc2)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL501794 212364 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL1165764 206777 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)N)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
145967082 163538 0 None 416 2 Rat 8.2 pEC50 = 8.2 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 163538 0 None 416 2 Rat 8.2 pEC50 = 8.2 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL3104471 209307 5 None 1 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contractionAgonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL607809 214045 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1016/j.bmc.2009.07.058
162666100 181677 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4783820 181677 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
145977223 163427 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163427 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
15983816 85403 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 360 8 1 2 4.6 CN(C)CCC(NC(=O)CCc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
CHEMBL229709 85403 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 360 8 1 2 4.6 CN(C)CCC(NC(=O)CCc1ccccc1)c1ccc2ccccc2c1 10.1016/j.ejmech.2006.09.015
145973990 164122 0 None -181 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4216988 164122 0 None -181 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
44400855 134749 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 448 7 0 3 7.7 CCN(CC)CCC1C(c2ccccc2)=Nc2ccccc2SC1c1ccc(Cl)cc1 10.1021/jm049110x
CHEMBL372689 134749 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity for human Urotensin 2 receptorAgonist activity for human Urotensin 2 receptor
ChEMBL 448 7 0 3 7.7 CCN(CC)CCC1C(c2ccccc2)=Nc2ccccc2SC1c1ccc(Cl)cc1 10.1021/jm049110x
45482441 13928 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197479 13928 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573574 13928 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 438 8 1 3 5.9 COc1ccc(-c2cccc(C(=O)NC(CCN(C)C)c3ccc4ccccc4c3)c2)cc1 10.1016/j.bmc.2009.04.062
24952709 13938 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197509 13938 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL574731 13938 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 406 7 1 2 5.7 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccc(Cl)cc3)c2)cc1 10.1016/j.bmc.2009.04.062
24953413 13949 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 356 6 1 2 4.7 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL1197568 13949 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 356 6 1 2 4.7 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL576922 13949 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 356 6 1 2 4.7 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
162658232 180396 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 923 26 13 11 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4758767 180396 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 923 26 13 11 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/acs.jmedchem.6b00164
45481583 13921 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 432 7 1 2 6.4 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197444 13921 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 432 7 1 2 6.4 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572467 13921 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 432 7 1 2 6.4 O=C(NC(CCN1CCCCC1)c1ccc(Cl)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2009.04.062
145967082 163538 0 None -416 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4209654 163538 0 None -416 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
49799366 14244 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 363 4 0 3 4.6 CN(C)CCC1(c2ccc(Cl)c(Cl)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1172763 14244 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 363 4 0 3 4.6 CN(C)CCC1(c2ccc(Cl)c(Cl)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200218 14244 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 363 4 0 3 4.6 CN(C)CCC1(c2ccc(Cl)c(Cl)c2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
46897994 14269 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 343 4 0 2 4.9 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2 10.1016/j.bmc.2010.04.041
CHEMBL1173492 14269 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 343 4 0 2 4.9 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2 10.1016/j.bmc.2010.04.041
CHEMBL1200286 14269 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 343 4 0 2 4.9 Cc1cc2c(cc1C)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2 10.1016/j.bmc.2010.04.041
145978068 163173 0 None -1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163173 0 None -1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145977223 163427 0 None 1 2 Rat 8.1 pEC50 = 8.1 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163427 0 None 1 2 Rat 8.1 pEC50 = 8.1 Functional
Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)Antagonist activity at UT receptor in Sprague-Dawley rat thoracic aortic ring assessed as reduction in urotensin-2-induced contraction by measuring pEC50 for human urotensin-2-induced contraction at 1 x 10'-8M uM pre-incubated for 30 mins before urotensin-2 stimulation (Rvb = 8.59 +/- 0.12 No_unit)
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL508811 213356 0 None - 1 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
49799023 14252 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 424 9 0 4 5.1 C=CCN(CC=C)c1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1173081 14252 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 424 9 0 4 5.1 C=CCN(CC=C)c1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1200246 14252 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 424 9 0 4 5.1 C=CCN(CC=C)c1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
24952706 13926 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197477 13926 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL573569 13926 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 8 1 3 5.4 COc1ccc(-c2ccc(C(=O)NC(CCN(C)C)c3ccc(Cl)cc3)cc2)cc1 10.1016/j.bmc.2009.04.062
162660720 180594 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 908 24 12 11 0.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4761055 180594 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 908 24 12 11 0.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
24955189 13920 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL1197443 13920 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL572454 13920 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 376 8 1 3 4.3 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc2ccccc2c1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL608097 214048 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.bmc.2009.07.058
24952353 13922 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197454 13922 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572882 13922 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 426 7 1 2 6.1 CN(C)CCC(NC(=O)c1ccc(-c2ccc(Cl)cc2)cc1)c1ccc(Cl)cc1 10.1016/j.bmc.2009.04.062
145966260 163823 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 163823 0 None -2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing beta-arrestin1-polycistronic BRET biosensor assessed as induction of beta-arrestin1 recruitment measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
11663047 1609 14 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1016/j.bmc.2009.04.062
3501 1609 14 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1016/j.bmc.2009.04.062
CHEMBL204989 1609 14 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1016/j.bmc.2009.04.062
162656670 180326 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 953 25 12 13 0.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4757895 180326 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 953 25 12 13 0.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL593612 214025 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assayAgonist activity at human GPR14 expressed in HEK293 cells by calcium mobilization assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1016/j.bmc.2009.07.058
24952708 13916 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197439 13916 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL572392 13916 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 372 7 1 2 5.1 Cc1ccc(C(CCN(C)C)NC(=O)c2cccc(-c3ccccc3)c2)cc1 10.1016/j.bmc.2009.04.062
24953057 13944 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 7 1 2 6.2 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL1197534 13944 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 7 1 2 6.2 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
CHEMBL575630 13944 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 422 7 1 2 6.2 Cc1ccc(C(CCN(C)C)NC(=O)c2ccc(-c3ccc4ccccc4c3)cc2)cc1 10.1016/j.bmc.2009.04.062
24955187 76350 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL206552 76350 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
CHEMBL574304 76350 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1016/j.bmc.2009.04.062
15983441 85204 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 398 7 1 2 4.7 CN(C)CCC(NC(=O)Cc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
CHEMBL228411 85204 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assayAgonist activity at human urotensin-2 receptor transfected in NIH3T3 cells after 5 days by R-SAT assay
ChEMBL 398 7 1 2 4.7 CN(C)CCC(NC(=O)Cc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1016/j.ejmech.2006.09.015
145977587 163123 0 None -14 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4204786 163123 0 None -14 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL509604 213790 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contractionAgonist activity at UT2 receptor in Albino rat aorta assessed as induction of aortic contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
162668785 182106 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1071 31 14 13 -0.3 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CCC(N)=O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4789420 182106 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 1071 31 14 13 -0.3 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CCC(N)=O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104471 209307 5 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at human UT receptor expressed in HEK293 cells co-expressing G12-polycistronic BRET biosensor assessed as induction of G12 activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162662050 181255 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 881 24 13 11 -1.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4778562 181255 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assayAgonist activity at human U-IIR expressed in HEK293-A cells by Fluo4-AM dye based intracellular calcium mobilization assay
ChEMBL 881 24 13 11 -1.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.6b00164
49798989 14241 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2ccc(Br)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1172605 14241 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2ccc(Br)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
CHEMBL1200194 14241 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 373 4 0 3 4.0 CN(C)CCC1(c2ccc(Br)cc2)Cc2ccccc2C(=O)O1 10.1016/j.bmc.2010.04.041
49799137 14278 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 5 0 4 3.9 COc1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1173725 14278 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 5 0 4 3.9 COc1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
CHEMBL1200304 14278 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assayAgonist activity against human urotensin 2 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity after 5 days by R-SAT assay
ChEMBL 359 5 0 4 3.9 COc1ccc2c(c1)CC(CCN(C)C)(c1ccc(Cl)cc1)OC2=O 10.1016/j.bmc.2010.04.041
25126427 2101 6 None 7 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
9437 2101 6 None 7 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
CHEMBL567713 2101 6 None 7 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
45487747 195199 0 None 501 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566056 195199 0 None 501 2 Rat 9.0 pIC50 = 9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
23728637 151178 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 625 8 1 7 4.2 CC(C)(C)OC(=O)N1CCN(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL396443 151178 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 625 8 1 7 4.2 CC(C)(C)OC(=O)N1CCN(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
142747296 170788 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 547 6 1 5 5.7 O=C(c1ccc(-c2ccccc2C(F)(F)F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4461733 170788 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 547 6 1 5 5.7 O=C(c1ccc(-c2ccccc2C(F)(F)F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
24804161 91303 0 None - 1 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 624 8 1 6 5.7 CC(C)(C)OC(=O)N1CCC(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL240916 91303 0 None - 1 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 624 8 1 6 5.7 CC(C)(C)OC(=O)N1CCC(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
10119117 87892 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 526 9 1 6 4.2 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348523 87892 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 526 9 1 6 4.2 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
23627613 195252 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 507 7 0 6 4.1 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5c(F)cccc5F)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566364 195252 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 507 7 0 6 4.1 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5c(F)cccc5F)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596967 195084 0 None 3 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565388 195084 0 None 3 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627666 195439 0 None 4 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567759 195439 0 None 4 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596966 195622 0 None 69 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568764 195622 0 None 69 2 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
142747294 170490 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4457118 170490 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
155543279 172714 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2cccc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4525919 172714 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2cccc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747247 173472 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2cccc(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4543925 173472 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2cccc(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
45486911 195495 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 628 10 1 8 5.8 COc1ccc(C(CCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568089 195495 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 628 10 1 8 5.8 COc1ccc(C(CCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45486917 195748 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 620 12 1 8 4.3 COc1ccc([C@@H](CCCNS(C)(=O)=O)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569689 195748 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 620 12 1 8 4.3 COc1ccc([C@@H](CCCNS(C)(=O)=O)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71717140 87886 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 380 6 1 4 4.4 COc1cccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)c1 10.1016/j.bmcl.2013.01.105
CHEMBL2348517 87886 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 380 6 1 4 4.4 COc1cccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)c1 10.1016/j.bmcl.2013.01.105
142747243 174153 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)cc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4560366 174153 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)cc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747265 175030 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 523 8 1 6 5.1 CCOc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4580364 175030 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 523 8 1 6 5.1 CCOc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
44596867 195285 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 674 12 1 9 5.4 COc1ccc(C(CCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566565 195285 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 674 12 1 9 5.4 COc1ccc(C(CCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45486909 195459 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 614 9 1 8 5.4 COc1ccc(C(CNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567866 195459 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 614 9 1 8 5.4 COc1ccc(C(CNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71580034 87893 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348524 87893 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
25127070 196873 0 None -93 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578204 196873 0 None -93 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
24803165 88352 0 None - 1 Rat 4.9 pIC50 = 4.9 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 497 8 0 4 4.1 CN(CCc1ccccc1)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL236396 88352 0 None - 1 Rat 4.9 pIC50 = 4.9 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 497 8 0 4 4.1 CN(CCc1ccccc1)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
142747268 171026 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2ccc(-c3ccccc3)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4465326 171026 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2ccc(-c3ccccc3)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
25127070 196873 0 None 93 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578204 196873 0 None 93 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
155552384 173561 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL4546405 173561 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
142747256 175093 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 537 8 1 6 5.5 CC(C)Oc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4581735 175093 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 537 8 1 6 5.5 CC(C)Oc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
23627556 196790 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL577518 196790 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596965 195153 0 None -6 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565806 195153 0 None -6 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25124736 196874 0 None -8 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578205 196874 0 None -8 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
71579840 87880 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 442 9 1 5 4.7 COc1cc(Br)c(CNc2ccc(Cl)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348510 87880 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 442 9 1 5 4.7 COc1cc(Br)c(CNc2ccc(Cl)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
71579747 87876 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348506 87876 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
44597068 195085 0 None 15 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565395 195085 0 None 15 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44206680 195316 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm900683d
CHEMBL566894 195316 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm900683d
21023902 3466 25 None 3 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
2165 3466 25 None 3 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
CHEMBL522770 3466 25 None 3 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
44597069 195798 0 None 5 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL569923 195798 0 None 5 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25126424 195337 0 None -19 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL567075 195337 0 None -19 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
71716535 87887 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3c(Br)ccc4c3OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348518 87887 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3c(Br)ccc4c3OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
71579748 87877 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348507 87877 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747285 173565 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 493 6 1 5 5.0 Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4546510 173565 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 493 6 1 5 5.0 Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
23627554 195219 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 471 7 0 6 3.8 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566187 195219 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 471 7 0 6 3.8 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627555 196070 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL571683 196070 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596964 195266 0 None -31 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566433 195266 0 None -31 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
16656749 195436 0 None -43 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567736 195436 0 None -43 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596870 195478 0 None 13 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567949 195478 0 None 13 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25128051 196005 0 None 21 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 0 8 4.3 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571216 196005 0 None 21 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 0 8 4.3 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C)CC3)C2=O)cc1OC 10.1021/jm900683d
25124736 196874 0 None 8 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578205 196874 0 None 8 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
142747253 170527 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 539 8 1 7 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1OC 10.1016/j.bmcl.2018.12.058
CHEMBL4457752 170527 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 539 8 1 7 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1OC 10.1016/j.bmcl.2018.12.058
10173280 2934 45 None 2 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPRAntagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPR
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
3516 2934 45 None 2 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPRAntagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPR
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
CHEMBL567303 2934 45 None 2 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPRAntagonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 10000 nM by FLIPR
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
2164 3457 13 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
9846574 3457 13 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
CHEMBL366221 3457 13 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
45486918 195562 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 722 13 1 9 6.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2ccc(Cl)s2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568388 195562 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 722 13 1 9 6.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2ccc(Cl)s2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627492 195172 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 513 8 0 6 5.3 CCC(c1ccc(OC)c(OC)c1)N1C(=O)c2cccc(N3CCN([C@H](C)c4ccccc4)CC3)c2C1=O 10.1021/jm900683d
CHEMBL565937 195172 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 513 8 0 6 5.3 CCC(c1ccc(OC)c(OC)c1)N1C(=O)c2cccc(N3CCN([C@H](C)c4ccccc4)CC3)c2C1=O 10.1021/jm900683d
71717139 87883 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 428 5 1 3 5.2 CN1CC[C@H](Oc2cc(NCc3ccccc3Br)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348514 87883 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 428 5 1 3 5.2 CN1CC[C@H](Oc2cc(NCc3ccccc3Br)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
24803990 91349 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 525 8 2 6 2.6 O=C(NCCN1CCNCC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL241128 91349 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 525 8 2 6 2.6 O=C(NCCN1CCNCC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
23627612 196125 0 None -22 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL572138 196125 0 None -22 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71719581 87881 0 None 19 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348511 87881 0 None 19 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
25127071 196872 0 None 251 2 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578203 196872 0 None 251 2 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
44596965 195153 0 None 6 2 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565806 195153 0 None 6 2 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627305 195747 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 642 11 1 8 6.2 COc1ccc(C(CCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569688 195747 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 642 11 1 8 6.2 COc1ccc(C(CCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627251 197231 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 542 10 1 7 4.7 COc1ccc(C(CCCN)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL584545 197231 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 542 10 1 7 4.7 COc1ccc(C(CCCN)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71579743 87872 0 None -43 3 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348502 87872 0 None -43 3 Rat 5.7 pIC50 = 5.7 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
71720175 87890 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 356 5 1 4 4.5 CN1CC[C@H](Oc2cc(NCc3cccs3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348521 87890 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 356 5 1 4 4.5 CN1CC[C@H](Oc2cc(NCc3cccs3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
24804323 90375 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 643 9 2 5 5.3 O=C(NCC1CCN(C(=O)NCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL239199 90375 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 643 9 2 5 5.3 O=C(NCC1CCN(C(=O)NCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44597068 195085 0 None -15 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565395 195085 0 None -15 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596870 195478 0 None -13 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567949 195478 0 None -13 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45487731 196876 0 None 2 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578207 196876 0 None 2 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
142747289 170014 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 479 6 1 5 4.7 O=C(c1ccc(-c2ccccc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4450638 170014 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 479 6 1 5 4.7 O=C(c1ccc(-c2ccccc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747303 170810 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 547 6 1 5 6.0 O=C(c1ccc(-c2ccc(Cl)c(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4462068 170810 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 547 6 1 5 6.0 O=C(c1ccc(-c2ccc(Cl)c(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
23627722 195518 0 None -8 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568165 195518 0 None -8 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
24803168 89448 0 None - 1 Rat 4.6 pIC50 = 4.6 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 407 5 0 4 2.5 CN(C)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL237877 89448 0 None - 1 Rat 4.6 pIC50 = 4.6 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 407 5 0 4 2.5 CN(C)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
23627249 195548 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568316 195548 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
24804816 145848 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 576 7 1 6 4.7 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2ccccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL392166 145848 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 576 7 1 6 4.7 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2ccccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
142747251 171914 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)cc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4483058 171914 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)cc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747252 172868 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)ccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4529337 172868 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)ccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
44597398 195113 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565580 195113 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
155512483 169087 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
CHEMBL4437489 169087 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
23627722 195518 0 None 8 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568165 195518 0 None 8 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25125422 195601 0 None 17 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL568637 195601 0 None 17 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
16656749 195436 0 None 43 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567736 195436 0 None 43 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45486908 195207 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 514 8 1 7 3.9 COc1ccc(C(CN)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566144 195207 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 514 8 1 7 3.9 COc1ccc(C(CN)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71718372 87885 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 380 6 1 4 4.4 COc1ccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1 10.1016/j.bmcl.2013.01.105
CHEMBL2348516 87885 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 380 6 1 4 4.4 COc1ccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1 10.1016/j.bmcl.2013.01.105
142747255 170865 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 507 7 1 5 5.3 CCc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4463082 170865 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 507 7 1 5 5.3 CCc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
10173280 2934 45 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
3516 2934 45 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
CHEMBL567303 2934 45 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
44597071 196875 0 None -52 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578206 196875 0 None -52 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
142747273 171501 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 533 6 1 5 5.1 O=C(c1ccc(-c2cc(F)c(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4472265 171501 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 533 6 1 5 5.1 O=C(c1ccc(-c2cc(F)c(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
24804324 89450 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 608 8 1 5 5.4 CC(C)(C)CC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL237879 89450 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 608 8 1 5 5.4 CC(C)(C)CC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
21023902 3466 25 None -3 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
2165 3466 25 None -3 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
CHEMBL522770 3466 25 None -3 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
25128051 196005 0 None -21 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 0 8 4.3 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571216 196005 0 None -21 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 11 0 8 4.3 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C)CC3)C2=O)cc1OC 10.1021/jm900683d
71580134 87897 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348528 87897 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
44596967 195084 0 None -3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565388 195084 0 None -3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
142747298 172674 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccc(Cl)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4524693 172674 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccc(Cl)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
44597070 195088 0 None 10 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL565416 195088 0 None 10 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
10173280 2934 45 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysisAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysis
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1016/j.bmcl.2013.01.105
3516 2934 45 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysisAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysis
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1016/j.bmcl.2013.01.105
CHEMBL567303 2934 45 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysisAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysis
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1016/j.bmcl.2013.01.105
71719581 87881 0 None -19 3 Rat 5.4 pIC50 = 5.4 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348511 87881 0 None -19 3 Rat 5.4 pIC50 = 5.4 Functional
Antagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at rat urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
24893978 993 5 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
8872 993 5 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
CHEMBL495075 993 5 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
25127072 196051 0 None 128 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571537 196051 0 None 128 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
45487748 196063 0 None 15 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571625 196063 0 None 15 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44596964 195266 0 None 31 2 Rat 8.3 pIC50 = 8.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566433 195266 0 None 31 2 Rat 8.3 pIC50 = 8.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44596869 195253 0 None 12 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566366 195253 0 None 12 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
24804326 144805 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 644 9 1 6 5.7 O=C(NCC1CCN(C(=O)OCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL391354 144805 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 644 9 1 6 5.7 O=C(NCC1CCN(C(=O)OCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44597070 195088 0 None -10 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL565416 195088 0 None -10 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
11272107 87871 37 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 504 7 1 6 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348501 87871 37 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 504 7 1 6 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
24803167 89449 0 None - 1 Rat 4.4 pIC50 = 4.4 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 469 7 1 4 3.8 O=C1COc2ccccc2N1CCN1CCC(C(=O)NCc2ccccc2)(c2ccccc2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL237878 89449 0 None - 1 Rat 4.4 pIC50 = 4.4 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 469 7 1 4 3.8 O=C1COc2ccccc2N1CCN1CCC(C(=O)NCc2ccccc2)(c2ccccc2)CC1 10.1016/j.bmcl.2007.09.092
23627430 195208 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566145 195208 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627666 195439 0 None -4 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567759 195439 0 None -4 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
142747254 169928 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2cccc(-c3ccccc3)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4449461 169928 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2cccc(-c3ccccc3)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
71579743 87872 0 None -102 3 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348502 87872 0 None -102 3 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747238 174951 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccccc2Cl)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4578409 174951 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccccc2Cl)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
45487747 195199 0 None -501 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566056 195199 0 None -501 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44596869 195253 0 None -12 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566366 195253 0 None -12 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
25127071 196872 0 None -251 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578203 196872 0 None -251 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
25067560 187378 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of intercellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of intercellular calcium mobilization by FLIPR assay
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497171 187378 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of intercellular calcium mobilization by FLIPR assayAntagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of intercellular calcium mobilization by FLIPR assay
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
45487731 196876 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578207 196876 0 None -2 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25127072 196051 0 None -128 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571537 196051 0 None -128 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
24804325 144809 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 614 8 1 5 5.2 O=C(NCC1CCN(C(=O)c2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL391355 144809 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 614 8 1 5 5.2 O=C(NCC1CCN(C(=O)c2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44435044 90439 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 664 10 1 6 4.9 O=C(NCC1CCN(S(=O)(=O)Cc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL239250 90439 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 664 10 1 6 4.9 O=C(NCC1CCN(S(=O)(=O)Cc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
25125422 195601 0 None -17 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL568637 195601 0 None -17 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
71718978 87889 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 440 8 1 6 4.4 COc1cc(OC)c(OC)cc1CNc1ccc(C(F)(F)F)c(O[C@H]2CCN(C)C2)c1 10.1016/j.bmcl.2013.01.105
CHEMBL2348520 87889 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 440 8 1 6 4.4 COc1cc(OC)c(OC)cc1CNc1ccc(C(F)(F)F)c(O[C@H]2CCN(C)C2)c1 10.1016/j.bmcl.2013.01.105
71580033 87894 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348525 87894 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
25125764 195505 0 None -9 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL568123 195505 0 None -9 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25125764 195505 0 None 9 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL568123 195505 0 None 9 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44597071 196875 0 None 52 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578206 196875 0 None 52 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
71579743 87872 0 None 43 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348502 87872 0 None 43 3 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
24804491 89510 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 610 7 1 6 5.3 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL238066 89510 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 610 7 1 6 5.3 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
71719582 87891 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 390 5 1 4 5.1 CN1CC[C@H](Oc2cc(NCc3ccc(Cl)s3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348522 87891 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 390 5 1 4 5.1 CN1CC[C@H](Oc2cc(NCc3ccc(Cl)s3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
71579843 87882 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 382 7 1 3 4.7 CN(C)CCOc1cc(NCc2ccccc2Br)ccc1Cl 10.1016/j.bmcl.2013.01.105
CHEMBL2348513 87882 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 382 7 1 3 4.7 CN(C)CCOc1cc(NCc2ccccc2Br)ccc1Cl 10.1016/j.bmcl.2013.01.105
45487748 196063 0 None -15 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571625 196063 0 None -15 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
10120078 67285 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL190533 67285 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448692 94444 3 None -208 2 Human 6.2 pIC50 = 6.2 Functional
Inhibition of human recombinant urotensin 2 receptor-mediated calcium mobilization expressed in HEK293 cells by FLIPR assayInhibition of human recombinant urotensin 2 receptor-mediated calcium mobilization expressed in HEK293 cells by FLIPR assay
ChEMBL 383 5 0 3 3.9 CN(CC(=O)N1CCCCC1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL254154 94444 3 None -208 2 Human 6.2 pIC50 = 6.2 Functional
Inhibition of human recombinant urotensin 2 receptor-mediated calcium mobilization expressed in HEK293 cells by FLIPR assayInhibition of human recombinant urotensin 2 receptor-mediated calcium mobilization expressed in HEK293 cells by FLIPR assay
ChEMBL 383 5 0 3 3.9 CN(CC(=O)N1CCCCC1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
71719581 87881 0 None -31 3 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348511 87881 0 None -31 3 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assayAntagonist activity at mouse urotensin2 receptor assessed as inhibition of urotensin2-stimulated Ca2+ mobilization by cell-based assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
45486916 195557 0 None - 1 Rat 4.2 pIC50 = 4.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 656 12 1 8 6.6 COc1ccc([C@@H](CCCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568358 195557 0 None - 1 Rat 4.2 pIC50 = 4.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 656 12 1 8 6.6 COc1ccc([C@@H](CCCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44597398 195113 0 None 3 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565580 195113 0 None 3 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25126424 195337 0 None 19 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL567075 195337 0 None 19 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25125075 196050 0 None 12 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 0 8 4.7 CCN1CCN(c2cccc3c2CN([C@H](CCCN(C)S(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571535 196050 0 None 12 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 0 8 4.7 CCN1CCN(c2cccc3c2CN([C@H](CCCN(C)S(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
142747291 169322 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2cccc([N+](=O)[O-])c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4440805 169322 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2cccc([N+](=O)[O-])c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747279 173926 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2ccc([N+](=O)[O-])cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4555094 173926 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2ccc([N+](=O)[O-])cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
23627557 195259 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc(C(C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566389 195259 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 499 7 0 6 4.9 COc1ccc(C(C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
24802993 88806 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 441 5 0 4 3.2 CN(C)C(=O)C1(c2ccc(Cl)cc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL236800 88806 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 441 5 0 4 3.2 CN(C)C(=O)C1(c2ccc(Cl)cc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
71579744 87873 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348503 87873 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
45486910 195690 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 660 11 1 9 5.0 COc1ccc(C(CNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569238 195690 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 660 11 1 9 5.0 COc1ccc(C(CNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596966 195622 0 None -69 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568764 195622 0 None -69 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
71579935 87884 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 372 7 1 3 4.9 CN(C)CCOc1cc(NCc2ccccc2C(F)(F)F)ccc1Cl 10.1016/j.bmcl.2013.01.105
CHEMBL2348515 87884 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 372 7 1 3 4.9 CN(C)CCOc1cc(NCc2ccccc2C(F)(F)F)ccc1Cl 10.1016/j.bmcl.2013.01.105
25126427 2101 6 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
9437 2101 6 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
CHEMBL567713 2101 6 None -7 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
21023902 3466 25 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
2165 3466 25 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
CHEMBL522770 3466 25 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
142747275 169068 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 509 7 1 6 4.7 COc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
CHEMBL4437224 169068 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 509 7 1 6 4.7 COc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
142747242 169957 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4449808 169957 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747271 174383 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 509 7 1 6 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL4565990 174383 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 509 7 1 6 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
23627249 195548 0 None 3 2 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568316 195548 0 None 3 2 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44597069 195798 0 None -5 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL569923 195798 0 None -5 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
23627612 196125 0 None 22 2 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL572138 196125 0 None 22 2 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25125075 196050 0 None -12 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 0 8 4.7 CCN1CCN(c2cccc3c2CN([C@H](CCCN(C)S(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571535 196050 0 None -12 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assayAntagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 612 12 0 8 4.7 CCN1CCN(c2cccc3c2CN([C@H](CCCN(C)S(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
148470142 169099 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4437619 169099 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
142747258 173232 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccc(F)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4538387 173232 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccc(F)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747281 175368 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cccc(F)c2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4588098 175368 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assayAntagonist activity at human UT2 receptor expressed in HEK293-aeq cells assessed as inhibition of U2-induced intracellular calcium mobilization preincubated for 15 mins followed by U2 addition by luminescence assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cccc(F)c2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
44435003 145820 0 None - 1 Rat 5.0 pIC50 = 5.0 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 511 9 0 4 4.5 CN(CCCc1ccccc1)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL392142 145820 0 None - 1 Rat 5.0 pIC50 = 5.0 Functional
Antagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR methodAntagonist activity at rat UT receptor transfected in CHOK1 cells assessed as calcium mobilization by FLIPR method
ChEMBL 511 9 0 4 4.5 CN(CCCc1ccccc1)C(=O)C1(c2ccccc2)CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
71720174 87888 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3cc4c(cc3Br)OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348519 87888 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assayAntagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3cc4c(cc3Br)OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
25067045 154958 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human urotensin 2 receptorAntagonist activity at human urotensin 2 receptor
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL404177 154958 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human urotensin 2 receptorAntagonist activity at human urotensin 2 receptor
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL387916 210656 0 None - 0 Rat 8.0 pKd = 8 Functional
Antagonist activity at rat UT receptorAntagonist activity at rat UT receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
25067560 187378 0 None - 1 Human 7.0 pKd = 7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497171 187378 0 None - 1 Human 7.0 pKd = 7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580475 192607 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL523566 192607 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580515 187425 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497561 187425 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
44580519 187291 0 None - 0 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
CHEMBL496516 187291 0 None - 0 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
12704866 187744 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL500880 187744 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human urotensin 2 receptor by FLIPR assayAntagonist activity at human urotensin 2 receptor by FLIPR assay
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL389653 210674 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity at rat UT receptorAntagonist activity at rat UT receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL223905 207691 10 None - 0 Rat 8.3 pKd = 8.3 Functional
Antagonist activity at rat UT receptorAntagonist activity at rat UT receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL389654 210675 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Antagonist activity at rat UT receptorAntagonist activity at rat UT receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL218698 207643 0 None - 0 Rat 6.1 pKd = 6.1 Functional
Antagonist potency against human urotensin-2-induced contraction of rat aortic ringAntagonist potency against human urotensin-2-induced contraction of rat aortic ring
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
2164 3457 13 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
9846574 3457 13 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
CHEMBL366221 3457 13 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
44206682 10363 0 None - 0 Rat 7.5 pKi = 7.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 449 5 0 5 4.7 CCN1CCN(c2cccc3c2[C@H]2CCCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
CHEMBL1165145 10363 0 None - 0 Rat 7.5 pKi = 7.5 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 449 5 0 5 4.7 CCN1CCN(c2cccc3c2[C@H]2CCCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
44206680 195316 0 None - 1 Human 6.4 pKi = 6.4 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
CHEMBL566894 195316 0 None - 1 Human 6.4 pKi = 6.4 Functional
Agonist activity at human urotensin 2 expressed in CHO cells by FLIPRAgonist activity at human urotensin 2 expressed in CHO cells by FLIPR
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
44206680 195316 0 None - 1 Rat 8.2 pKi = 8.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
CHEMBL566894 195316 0 None - 1 Rat 8.2 pKi = 8.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
46907359 10349 0 None - 0 Rat 6.2 pKi = 6.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 1000 nM by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 1000 nM by FLIPR
ChEMBL 536 12 2 6 4.4 CC(C)[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1021/jm901294u
CHEMBL1164523 10349 0 None - 0 Rat 6.2 pKi = 6.2 Functional
Agonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 1000 nM by FLIPRAgonist activity at rat urotensin 2 receptor expressed in CHO cells assessed as calcium mobilization at 1000 nM by FLIPR
ChEMBL 536 12 2 6 4.4 CC(C)[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1021/jm901294u
11663047 1609 14 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 17112638
11663047 1609 14 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 19481466
3501 1609 14 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 17112638
3501 1609 14 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 19481466
CHEMBL204989 1609 14 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 17112638
CHEMBL204989 1609 14 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 19481466
9441 3881 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 27791374
9436 103 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12943190
2163 3383 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 446 6 3 3 5.4 NC(=N)c1cccc(c1)Cn1c(cc2c1cccc2C)C(=O)NCc1cccc2c1cccc2 11960491
9803617 3383 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 446 6 3 3 5.4 NC(=N)c1cccc(c1)Cn1c(cc2c1cccc2C)C(=O)NCc1cccc2c1cccc2 11960491
CHEMBL93758 3383 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 446 6 3 3 5.4 NC(=N)c1cccc(c1)Cn1c(cc2c1cccc2C)C(=O)NCc1cccc2c1cccc2 11960491
10173280 2934 45 None -2 2 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 15146030
3516 2934 45 None -2 2 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 15146030
CHEMBL567303 2934 45 None -2 2 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 15146030
10886 3593 0 None - 1 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 549 10 2 5 6.2 CN(CCCOc1cc(ccc1Cl)c1nc(ccc1c1ccccc1C)C(=O)NC1(CCCCC1)C(=O)O)C 32332113
66720777 3593 0 None - 1 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 549 10 2 5 6.2 CN(CCCOc1cc(ccc1Cl)c1nc(ccc1c1ccccc1C)C(=O)NC1(CCCCC1)C(=O)O)C 32332113
66720778 3593 0 None - 1 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 549 10 2 5 6.2 CN(CCCOc1cc(ccc1Cl)c1nc(ccc1c1ccccc1C)C(=O)NC1(CCCCC1)C(=O)O)C 32332113
11438 1453 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 0 7 2.1 O=C(N1CCN(C[C@@H]1CN1CCCC1)S(=O)(=O)CCN1CCN(CC1)C(=O)C)COc1cc(Cl)c(cc1Cl)Cl 30608334
46862051 1453 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 0 7 2.1 O=C(N1CCN(C[C@@H]1CN1CCCC1)S(=O)(=O)CCN1CCN(CC1)C(=O)C)COc1cc(Cl)c(cc1Cl)Cl 30608334
11995575 3886 0 None - 1 Human 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14550283
2156 3886 0 None - 1 Human 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14550283
CHEMBL437110 3886 0 None - 1 Human 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14550283


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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
CHEMBL3315148 209616 0 None - 1 Rat 10.9 pEC50 = 10.9 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315144 209612 0 None - 1 Rat 10.7 pEC50 = 10.7 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2nc3ccccc3s2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315139 209607 9 None - 1 Rat 9.4 pEC50 = 9.4 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315152 209620 0 None - 1 Rat 9.2 pEC50 = 9.2 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315140 209608 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315146 209614 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL437430 211960 0 None - 1 Rat 9.1 pEC50 = 9.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL437430 211960 0 None - 1 Rat 9.0 pEC50 = 9 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3315150 209618 0 None - 1 Rat 9.0 pEC50 = 9.0 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
137628790 160437 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4068478 160437 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116168 160437 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177635 120681 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577311 120681 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177635 120681 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577311 120681 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
127051713 140484 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1125 19 12 15 0.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN(C)C)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823939 140484 0 None - 0 Rat 8.8 pEC50 = 8.8 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1125 19 12 15 0.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN(C)C)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL218994 207648 0 None - 1 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137630764 160545 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4077689 160545 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117037 160545 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137630919 160573 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4062799 160573 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117229 160573 0 None - 0 Rat 8.0 pEC50 = 8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177633 120679 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577309 120679 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137629788 160621 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4099974 160621 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117629 160621 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177633 120679 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577309 120679 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137629655 160607 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 160607 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 160607 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137629876 160633 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 160633 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 160633 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137629789 160622 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4095707 160622 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117630 160622 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137629655 160607 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 160607 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 160607 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
44409478 75569 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 7 1 2 4.3 CCc1ccccc1C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205157 75569 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 7 1 2 4.3 CCc1ccccc1C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
155519842 169796 0 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4447811 169796 0 None - 1 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
15983315 76977 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 409 6 0 3 5.3 Cc1cc(Br)ccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL208436 76977 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 409 6 0 3 5.3 Cc1cc(Br)ccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
11640431 140815 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 423 8 2 3 5.9 CN(C)CCC(NC(=O)Nc1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL383698 140815 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 423 8 2 3 5.9 CN(C)CCC(NC(=O)Nc1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
137629655 160607 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 160607 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 160607 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
122177625 120671 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577301 120671 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137631060 160596 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076985 160596 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117349 160596 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177625 120671 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577301 120671 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177627 120673 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577303 120673 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177627 120673 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577303 120673 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
2151 242 6 None - 1 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm051121i
9797568 242 6 None - 1 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm051121i
CHEMBL192359 242 6 None - 1 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm051121i
11626617 76992 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 362 7 1 4 4.6 COc1cccc(NC(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL208536 76992 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 362 7 1 4 4.6 COc1cccc(NC(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
15983313 97795 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 365 6 0 3 5.2 Cc1c(Cl)cccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL274508 97795 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 365 6 0 3 5.2 Cc1c(Cl)cccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
15983200 76990 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 0 3 4.8 Cc1cccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL208512 76990 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 0 3 4.8 Cc1cccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL3104463 209303 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11684574 165472 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 399 6 2 2 5.2 CN(C)CCC(NC(=O)Nc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL425592 165472 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 399 6 2 2 5.2 CN(C)CCC(NC(=O)Nc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104463 209303 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
137631155 160643 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 160643 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 160643 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137629655 160607 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 160607 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 160607 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137629651 160602 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4084476 160602 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117427 160602 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
122177624 120670 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577300 120670 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177624 120670 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577300 120670 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3315149 209617 0 None - 1 Rat 7.9 pEC50 = 7.9 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N1)C(=O)O 10.1021/jm500218x
15983196 193913 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 7 0 3 4.8 CCc1ccccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL555609 193913 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 7 0 3 4.8 CCc1ccccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
137631008 160583 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4081970 160583 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117292 160583 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
127050201 140395 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1134 19 12 15 1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3822808 140395 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1134 19 12 15 1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
155544020 172733 0 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4526244 172733 0 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137629875 160632 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4074175 160632 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117691 160632 0 None - 0 Rat 7.9 pEC50 = 7.9 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
11325792 139624 8 None - 0 Human 6.9 pEC50 = 6.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 357 4 0 3 4.5 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)cc1)C2 10.1021/jm051121i
CHEMBL380346 139624 8 None - 0 Human 6.9 pEC50 = 6.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 357 4 0 3 4.5 Cc1cc2c(cc1C)C(=O)OC(CCN(C)C)(c1ccc(Cl)cc1)C2 10.1021/jm051121i
11559579 74401 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 2 3 4.2 COc1cccc(NC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL203106 74401 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 2 3 4.2 COc1cccc(NC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
11631605 74690 1 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 7 1 3 3.8 COc1ccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL203531 74690 1 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 7 1 3 3.8 COc1ccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11546868 75592 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 359 7 1 3 3.8 CN(C)CCC(NC(=O)c1ccc(N(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205254 75592 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 359 7 1 3 3.8 CN(C)CCC(NC(=O)c1ccc(N(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
15983325 138164 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 370 6 0 4 4.7 CN(C)CCC(OC(=O)c1cc2ccccc2n1C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL377946 138164 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 370 6 0 4 4.7 CN(C)CCC(OC(=O)c1cc2ccccc2n1C)c1ccc(Cl)cc1 10.1021/jm051121i
137631155 160643 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 160643 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 160643 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
11552098 74644 1 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 316 6 1 2 3.8 CN(C)CCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203337 74644 1 None - 0 Human 5.9 pEC50 = 5.9 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 316 6 1 2 3.8 CN(C)CCC(NC(=O)c1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
11625650 76396 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 407 7 2 2 5.8 CN(C)CCC(NC(=O)Nc1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206811 76396 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 407 7 2 2 5.8 CN(C)CCC(NC(=O)Nc1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
44409467 74391 1 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203080 74391 1 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL572699 74391 1 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
137629875 160632 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4074175 160632 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117691 160632 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 2 4 6.1 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
127049894 140417 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc3ccccc3c2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823122 140417 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc3ccccc3c2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
137628890 160415 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4064003 160415 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4115991 160415 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
44409534 75191 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 370 6 0 4 4.7 CN(C)CCC(OC(=O)c1cn(C)c2ccccc12)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL204516 75191 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 370 6 0 4 4.7 CN(C)CCC(OC(=O)c1cn(C)c2ccccc12)c1ccc(Cl)cc1 10.1021/jm051121i
11546571 75614 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1ccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c(C)c1 10.1021/jm051121i
CHEMBL205430 75614 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1ccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c(C)c1 10.1021/jm051121i
CHEMBL3104461 209301 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
137631155 160643 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 160643 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 160643 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137630919 160573 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4062799 160573 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117229 160573 0 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 502 8 2 4 6.3 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL3104461 209301 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11674961 139805 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 362 7 1 4 4.6 COc1ccc(NC(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL380745 139805 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 362 7 1 4 4.6 COc1ccc(NC(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11508921 76806 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 331 6 0 3 4.5 Cc1ccccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL207882 76806 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 331 6 0 3 4.5 Cc1ccccc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
11569119 75912 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 385 6 0 3 5.2 CN(C)CCC(OC(=O)c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205859 75912 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 385 6 0 3 5.2 CN(C)CCC(OC(=O)c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
11566781 76259 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 364 6 1 2 4.7 Cc1c(Cl)cccc1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206371 76259 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 364 6 1 2 4.7 Cc1c(Cl)cccc1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
137631154 160642 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 160642 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 160642 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
11510666 140173 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 358 6 1 2 4.7 Cc1cc(C)c(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1C 10.1021/jm051121i
CHEMBL381756 140173 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 358 6 1 2 4.7 Cc1cc(C)c(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1C 10.1021/jm051121i
CHEMBL3315143 209611 0 None - 1 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N1)C(=O)O 10.1021/jm500218x
121335724 158386 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 1 uM preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 1 uM preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b01525
CHEMBL4095859 158386 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 1 uM preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 1 uM preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b01525
155560750 174499 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568539 174499 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3104460 209300 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11591072 138171 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 388 6 1 3 5.9 CN(C)CCC(OC(=O)Nc1ccc(C(C)(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL377973 138171 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 388 6 1 3 5.9 CN(C)CCC(OC(=O)Nc1ccc(C(C)(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
15983317 75108 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 0 3 4.8 Cc1ccc(C)c(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL204227 75108 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 0 3 4.8 Cc1ccc(C)c(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
122177634 120680 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 120680 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177634 120680 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 120680 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137629651 160602 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4084476 160602 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117427 160602 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 476 7 2 4 5.8 NCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137641820 160667 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4087993 160667 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117996 160667 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
11531958 140754 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 424 8 1 4 6.4 CN(C)CCC(OC(=O)Nc1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL383326 140754 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 424 8 1 4 6.4 CN(C)CCC(OC(=O)Nc1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
11524599 76359 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 330 7 1 2 3.7 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206596 76359 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 330 7 1 2 3.7 CN(C)CCC(NC(=O)Cc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
15983311 138348 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 0 4 4.5 COc1cccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL378235 138348 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 0 4 4.5 COc1cccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
137629876 160633 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 160633 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 160633 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced G12 activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 6.75 +/- 0.19 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
155532198 171164 0 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4467241 171164 0 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
2151 242 6 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Potency against rat Urotensin 2 receptorPotency against rat Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
9797568 242 6 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Potency against rat Urotensin 2 receptorPotency against rat Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
CHEMBL192359 242 6 None - 1 Rat 6.7 pEC50 = 6.7 Binding
Potency against rat Urotensin 2 receptorPotency against rat Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
11532525 75685 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 2 3 4.2 COc1ccc(NC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL205735 75685 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 361 7 2 3 4.2 COc1ccc(NC(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11573773 140520 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 7 2 2 3.8 CN(C)CCC(NC(=O)NCc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL382477 140520 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 7 2 2 3.8 CN(C)CCC(NC(=O)NCc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
127052350 140454 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1097 18 13 15 -0.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823569 140454 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1097 18 13 15 -0.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
122177625 120671 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577301 120671 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3315147 209615 0 None - 1 Rat 8.6 pEC50 = 8.6 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
155537097 171680 0 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4474481 171680 0 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3104471 209307 5 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
122177625 120671 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577301 120671 0 None - 0 Rat 8.6 pEC50 = 8.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104465 209305 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11697064 76369 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 367 6 0 3 5.3 CN(C)CCC(OC(=O)c1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206661 76369 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 367 6 0 3 5.3 CN(C)CCC(OC(=O)c1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104465 209305 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
122177629 120675 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577305 120675 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177629 120675 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577305 120675 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104464 209304 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11559558 75659 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 6 1 4 3.5 CN(C)CCC(NC(=O)c1ccc2c(c1)OCO2)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205628 75659 1 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 6 1 4 3.5 CN(C)CCC(NC(=O)c1ccc2c(c1)OCO2)c1ccc(Cl)cc1 10.1021/jm051121i
11495815 76360 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 7 1 3 4.3 CN(C)CCC(OC(=O)NCc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206597 76360 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 7 1 3 4.3 CN(C)CCC(OC(=O)NCc1ccccc1)c1ccc(Cl)cc1 10.1021/jm051121i
11595438 77293 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 347 7 0 4 4.2 COc1ccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL208886 77293 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 347 7 0 4 4.2 COc1ccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
137631155 160643 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 160643 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 160643 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL3104464 209304 0 None - 0 Rat 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
155532198 171164 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4467241 171164 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137631154 160642 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 160642 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 160642 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
11681737 75610 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 2 2 4.5 Cc1ccccc1NC(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205390 75610 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 345 6 2 2 4.5 Cc1ccccc1NC(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
15983323 76379 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 367 6 0 3 5.3 CN(C)CCC(OC(=O)c1cccc2ccccc12)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206719 76379 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 367 6 0 3 5.3 CN(C)CCC(OC(=O)c1cccc2ccccc12)c1ccc(Cl)cc1 10.1021/jm051121i
122177624 120670 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577300 120670 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177624 120670 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577300 120670 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 522 9 4 5 4.6 NCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155537097 171680 0 None - 1 Rat 7.6 pEC50 = 7.6 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4474481 171680 0 None - 1 Rat 7.6 pEC50 = 7.6 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
121335724 158386 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 1 uM preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 1 uM preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b01525
CHEMBL4095859 158386 0 None - 0 Rat 7.6 pEC50 = 7.6 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 1 uM preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 1 uM preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b01525
CHEMBL3104462 209302 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11526048 74336 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 400 6 1 3 5.6 CN(C)CCC(OC(=O)Nc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203051 74336 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 400 6 1 3 5.6 CN(C)CCC(OC(=O)Nc1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104462 209302 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
2151 242 6 None - 1 Human 6.6 pEC50 = 6.6 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
9797568 242 6 None - 1 Human 6.6 pEC50 = 6.6 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
CHEMBL192359 242 6 None - 1 Human 6.6 pEC50 = 6.6 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
15983321 75167 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 337 6 0 4 4.6 Cc1ccsc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL204368 75167 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 337 6 0 4 4.6 Cc1ccsc1C(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104467 209306 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3ccccc3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11627432 74688 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 408 7 1 3 6.2 CN(C)CCC(OC(=O)Nc1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203528 74688 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 408 7 1 3 6.2 CN(C)CCC(OC(=O)Nc1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
11501947 75663 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 387 6 2 2 5.5 CN(C)CCC(NC(=O)Nc1ccc(C(C)(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205681 75663 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 387 6 2 2 5.5 CN(C)CCC(NC(=O)Nc1ccc(C(C)(C)C)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
15983198 140743 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 331 6 0 3 4.5 Cc1ccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL383258 140743 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 331 6 0 3 4.5 Cc1ccc(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11648503 76349 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 381 6 2 2 5.3 CN(C)CCC(NC(=O)Nc1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL206551 76349 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 381 6 2 2 5.3 CN(C)CCC(NC(=O)Nc1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
11609885 140491 1 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1ccc(C)c(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL382401 140491 1 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1ccc(C)c(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1 10.1021/jm051121i
CHEMBL593662 214026 9 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL593662 214026 9 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137630539 160516 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4060368 160516 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116751 160516 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL593662 214026 9 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
137629890 160453 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4069649 160453 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116283 160453 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137631008 160583 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4081970 160583 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117292 160583 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 516 9 1 4 6.6 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137629876 160633 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 160633 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 160633 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137631154 160642 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 160642 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 160642 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
135747623 174483 0 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568153 174483 0 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137641820 160667 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4087993 160667 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117996 160667 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 518 10 2 4 6.6 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177634 120680 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 120680 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177634 120680 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 120680 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 4 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137630539 160516 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4060368 160516 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116751 160516 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
127048901 140404 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1058 18 12 15 -0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccccc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3822950 140404 0 None - 0 Rat 8.5 pEC50 = 8.5 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1058 18 12 15 -0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccccc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL218994 207648 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
135747623 174483 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568153 174483 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137630689 160540 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4092221 160540 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116960 160540 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177631 120677 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577307 120677 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177631 120677 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577307 120677 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137628790 160437 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4068478 160437 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116168 160437 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 545 9 1 5 7.1 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137631060 160596 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076985 160596 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117349 160596 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.5 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137629952 160462 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4103468 160462 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116345 160462 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137630764 160545 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4077689 160545 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117037 160545 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 478 8 2 4 5.7 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
127051713 140484 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1125 19 12 15 0.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN(C)C)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823939 140484 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1125 19 12 15 0.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN(C)C)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3315141 209609 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm500218x
137630124 160489 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4085539 160489 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116532 160489 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137629876 160633 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 160633 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 160633 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137630474 160510 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4065552 160510 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116679 160510 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
2151 242 6 None - 1 Human 6.5 pEC50 = 6.5 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
9797568 242 6 None - 1 Human 6.5 pEC50 = 6.5 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
CHEMBL192359 242 6 None - 1 Human 6.5 pEC50 = 6.5 Binding
Potency against human Urotensin 2 receptorPotency against human Urotensin 2 receptor
ChEMBL 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 10.1021/jm025551+
11696838 76788 1 None - 0 Human 7.5 pEC50 = 7.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL207823 76788 1 None - 0 Human 7.5 pEC50 = 7.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL573857 76788 1 None - 0 Human 7.5 pEC50 = 7.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(C)CC[C@H](NC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3315145 209613 0 None - 1 Rat 7.5 pEC50 = 7.5 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2nc3ccccc3s2)C(=O)N1)C(=O)O 10.1021/jm500218x
11537255 74077 1 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 330 6 1 2 4.1 Cc1ccccc1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL202725 74077 1 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 330 6 1 2 4.1 Cc1ccccc1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
11582902 75582 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1cccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL205201 75582 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 344 6 1 2 4.4 Cc1cccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
137629876 160633 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 160633 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 160633 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced G12 activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 6.31 +/- 0.17 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL3104460 209300 0 None - 0 Rat 6.4 pEC50 = 6.4 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11604535 75630 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 6 1 3 4.9 Cc1ccccc1NC(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205488 75630 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 346 6 1 3 4.9 Cc1ccccc1NC(=O)OC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
122177629 120675 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577305 120675 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137628942 160425 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4090653 160425 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116059 160425 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137630802 160552 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4087877 160552 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117095 160552 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
137631155 160643 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 160643 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 160643 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137631061 160597 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4096184 160597 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117350 160597 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137631061 160597 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4096184 160597 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117350 160597 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
122177630 120676 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577306 120676 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177630 120676 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577306 120676 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137629655 160607 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 160607 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 160607 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
155567837 175453 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4590360 175453 0 None - 1 Rat 8.4 pEC50 = 8.4 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137629789 160622 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4095707 160622 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117630 160622 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 504 9 2 4 6.2 NCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177634 120680 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 120680 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177634 120680 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577310 120680 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 1 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177632 120678 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577308 120678 0 None - 0 Rat 8.4 pEC50 = 8.4 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177632 120678 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577308 120678 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155524087 170316 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4454498 170316 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
122177629 120675 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577305 120675 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137628889 160414 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4070119 160414 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4115990 160414 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
127048901 140404 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1058 18 12 15 -0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccccc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3822950 140404 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1058 18 12 15 -0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccccc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
122177631 120677 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577307 120677 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177631 120677 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577307 120677 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155536007 171550 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4472928 171550 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137628942 160425 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4090653 160425 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4116059 160425 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 559 10 1 5 7.4 CNCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177636 120682 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577312 120682 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104644 209313 0 None - 0 Rat 7.4 pEC50 = 7.4 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104644 209313 0 None - 0 Rat 7.4 pEC50 = 7.4 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
44409477 76779 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 366 6 1 2 4.9 CN(C)CC[C@H](NC(=O)c1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL207783 76779 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 366 6 1 2 4.9 CN(C)CC[C@H](NC(=O)c1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
11496131 139796 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 7 1 3 4.1 COc1cccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
CHEMBL380704 139796 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 7 1 3 4.1 COc1cccc(C(=O)NC(CCN(C)C)c2ccc(Cl)cc2)c1C 10.1021/jm051121i
15983319 76404 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 359 6 0 3 5.1 Cc1cc(C)c(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1C 10.1021/jm051121i
CHEMBL206832 76404 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 359 6 0 3 5.1 Cc1cc(C)c(C(=O)OC(CCN(C)C)c2ccc(Cl)cc2)cc1C 10.1021/jm051121i
122177636 120682 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577312 120682 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3315142 209610 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at UT receptor in rat aorta assessed as contractionAgonist activity at UT receptor in rat aorta assessed as contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N1)C(=O)O 10.1021/jm500218x
137629655 160607 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4066696 160607 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117503 160607 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 492 9 2 4 6.1 NCCCCN1N=C(CCc2ccc(O)cc2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137629952 160462 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4103468 160462 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116345 160462 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 532 11 1 4 6.9 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137630124 160489 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4085539 160489 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116532 160489 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 506 10 1 4 6.4 COc1ccc(CCC2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137629788 160621 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4099974 160621 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117629 160621 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 490 8 1 4 6.1 COc1ccc(/C=C/C2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137629877 160634 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4077479 160634 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117693 160634 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
127051389 140449 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2cccc3ccccc23)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823484 140449 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2cccc3ccccc23)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
155529504 170856 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4462940 170856 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
155524087 170316 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4454498 170316 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL218994 207648 0 None - 1 Rat 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137629877 160634 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4077479 160634 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117693 160634 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 533 9 1 5 7.0 NCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
122177628 120674 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577304 120674 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177628 120674 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577304 120674 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155537736 171770 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4475783 171770 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assayAgonist activity at urotensin 2 receptor (unknown origin) expressed in HEK293 cells co-expressing Gq-polycistronic BRET biosensor assessed as induction of Gq activation measured for 5 mins by luminescence detection based BRET assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
122177632 120678 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577308 120678 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177632 120678 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577308 120678 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 498 8 5 5 3.9 NCCC[C@@H]1N[C@H](c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155537736 171770 0 None - 1 Rat 8.2 pEC50 = 8.2 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4475783 171770 0 None - 1 Rat 8.2 pEC50 = 8.2 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137628889 160414 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4070119 160414 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4115990 160414 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
44409548 76961 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL208362 76961 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL573837 76961 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL3104639 209310 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
11525327 140553 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 364 6 1 2 4.7 Cc1cccc(Cl)c1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL382688 140553 0 None - 0 Human 5.3 pEC50 = 5.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 364 6 1 2 4.7 Cc1cccc(Cl)c1C(=O)NC(CCN(C)C)c1ccc(Cl)cc1 10.1021/jm051121i
11653844 75029 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 382 6 1 3 5.7 CN(C)CCC(OC(=O)Nc1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203937 75029 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 382 6 1 3 5.7 CN(C)CCC(OC(=O)Nc1ccc2ccccc2c1)c1ccc(Cl)cc1 10.1021/jm051121i
11524788 76146 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 393 7 0 3 5.9 CN(C)CCC(OC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL205991 76146 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 393 7 0 3 5.9 CN(C)CCC(OC(=O)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104637 209308 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
155560750 174499 0 None - 1 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568539 174499 0 None - 1 Rat 6.3 pEC50 = 6.3 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3104637 209308 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
137628890 160415 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4064003 160415 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4115991 160415 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in human urotensin-2-mediated aortic ring contraction by measuring urotensin-2 pEC50 at 10'-5M preincubated for 15 mins followed by urotensin-2 addition (Rvb = 8.61 +/- 0.05 No_unit)
ChEMBL 573 11 1 5 7.7 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
137629876 160633 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4076150 160633 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117692 160633 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 519 8 1 5 6.6 NCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2ccc3ccccc3c2)C1=O 10.1021/acs.jmedchem.7b01525
137630474 160510 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4065552 160510 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116679 160510 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 492 9 1 4 6.0 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137631154 160642 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 160642 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 160642 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177627 120673 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577303 120673 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177627 120673 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577303 120673 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 15 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 536 10 4 5 5.0 NCCCC[C@@H]1N=C(c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137630802 160552 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4087877 160552 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117095 160552 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 547 10 1 5 7.2 CNCCCCN1N=C(CCc2nc3ccccc3s2)c2ccccc2N(Cc2cccc3ccccc23)C1=O 10.1021/acs.jmedchem.7b01525
122177626 120672 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577302 120672 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177626 120672 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577302 120672 0 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
11496252 138162 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 366 7 1 3 3.6 Cc1ccc(S(=O)(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
CHEMBL377938 138162 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 366 7 1 3 3.6 Cc1ccc(S(=O)(=O)NC(CCN(C)C)c2ccc(Cl)cc2)cc1 10.1021/jm051121i
11567714 74786 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 408 8 1 3 5.6 CN(C)CCC(NC(=O)c1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL203626 74786 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 408 8 1 3 5.6 CN(C)CCC(NC(=O)c1ccc(Oc2ccccc2)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL3104471 209307 5 None - 1 Rat 8.2 pEC50 = 8.2 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
137631154 160642 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 160642 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 160642 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in URP-induced Gq activation by measuring URP pEC50 at 10'-5 M preincubated for 30 mins followed by URP addition by BRET assay (Rvb = 8.28 +/- 0.08 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL3104471 209307 5 None - 1 Rat 8.1 pEC50 = 8.1 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
137629890 160453 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4069649 160453 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116283 160453 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 518 10 1 4 6.5 COc1ccc(CCC2=NN(CCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177628 120674 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577304 120674 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177628 120674 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577304 120674 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 8 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 510 9 4 5 4.5 NCCCC[C@@H]1N=C(c2cccc3ccccc23)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
127051389 140449 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2cccc3ccccc23)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823484 140449 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2cccc3ccccc23)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
11663047 1609 14 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1021/jm051121i
3501 1609 14 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1021/jm051121i
CHEMBL204989 1609 14 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 392 7 1 2 5.4 CN(CCC(c1ccc(cc1)Cl)NC(=O)c1ccc(cc1)c1ccccc1)C 10.1021/jm051121i
11589093 75548 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 384 6 1 2 4.8 CN(C)CCC(NC(=O)c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
CHEMBL204988 75548 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 384 6 1 2 4.8 CN(C)CCC(NC(=O)c1ccc(C(F)(F)F)cc1)c1ccc(Cl)cc1 10.1021/jm051121i
122177630 120676 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577306 120676 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104471 209307 5 None - 1 Rat 8.1 pEC50 = 8.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
122177630 120676 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577306 120676 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 11 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 524 9 5 5 4.5 NCCC[C@@H]1N[C@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177636 120682 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577312 120682 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177636 120682 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577312 120682 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
137631154 160642 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4071437 160642 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4117761 160642 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)Allosteric modulation of human urotensin-2 receptor expressed in HEK293 cells assessed as change in human urotensin-2-induced Gq activation by measuring urotensin-2 pEC50 at 10'-5 M preincubated for 30 mins followed by urotensin-2 addition by BRET assay (Rvb = 7.88 +/- 0.07 No_unit)
ChEMBL 530 10 1 4 7.0 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
137630689 160540 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4092221 160540 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
CHEMBL4116960 160540 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 504 9 1 4 6.4 COc1ccc(/C=C/C2=NN(CCCCN)C(=O)N(Cc3ccc4ccccc4c3)c3ccccc32)cc1 10.1021/acs.jmedchem.7b01525
122177635 120681 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577311 120681 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 13 nM)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177633 120679 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577309 120679 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177635 120681 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577311 120681 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as urotensin-2 related peptide pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by urotensin-2 related peptide addition (Rvb = 7.89 +/- 0.08 no unit)
ChEMBL 512 9 5 5 4.3 NCCCC[C@@H]1N[C@@H](c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177633 120679 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577309 120679 0 None - 0 Rat 8.1 pEC50 = 8.1 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 14 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 538 10 5 5 4.9 NCCCC[C@@H]1N[C@@H](c2ccc(-c3ccccc3)cc2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3104638 209309 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
155544020 172733 0 None - 1 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4526244 172733 0 None - 1 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3104467 209306 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3ccccc3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104638 209309 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
24955187 76350 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL206552 76350 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL574304 76350 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Activity against human urotensin-2 receptor expressed in NIH3T3 cellsActivity against human urotensin-2 receptor expressed in NIH3T3 cells
ChEMBL 360 8 1 3 3.8 CO[C@@H](C(=O)N[C@@H](CCN(C)C)c1ccc(Cl)cc1)c1ccccc1 10.1021/jm051121i
CHEMBL3104639 209310 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstrictionAgonist activity at urotensin-2 receptor in Sprague-Dawley rat aortic rings assessed as KCl-induced vasoconstriction
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
127052350 140454 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1097 18 13 15 -0.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823569 140454 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1097 18 13 15 -0.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NN(CCCCN)S(=O)(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
137631155 160643 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4100932 160643 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
CHEMBL4117762 160643 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)Allosteric modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aorta assessed as change in URP-mediated aortic ring contraction by measuring URP pEC50 at 10'-5M preincubated for 15 mins followed by URP addition (Rvb = 8.09 +/- 0.03 No_unit)
ChEMBL 516 9 2 4 6.7 NCCCCN1N=C(/C=C/c2ccc(O)cc2)c2ccccc2N(Cc2ccc(-c3ccccc3)cc2)C1=O 10.1021/acs.jmedchem.7b01525
122177626 120672 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577302 120672 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 pEC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 8.71 +/- 0.08 no unit)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
122177626 120672 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
CHEMBL3577302 120672 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)Modulation of urotensin-2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as human urotensin-2 EC50 for induction of aortic ring contraction at 10 uM preincubated for 15 mins followed by human urotensin-2 addition (Rvb = 1.9 nM)
ChEMBL 496 8 4 5 4.1 NCCC[C@@H]1N=C(c2ccc3ccccc3c2)c2[nH]c(C(=O)O)cc2N(CCc2ccc(O)cc2)C1=O 10.1021/acs.jmedchem.5b00162
155529504 170856 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4462940 170856 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
127049894 140417 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc3ccccc3c2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3823122 140417 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for URP -induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1108 18 12 15 0.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc3ccccc3c2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
127050201 140395 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1134 19 12 15 1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
CHEMBL3822808 140395 0 None - 0 Rat 8.0 pEC50 = 8.0 Binding
Antagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KClAntagonist activity at UT2 receptor in Sprague-Dawley rat thoracic aorta ring assessed as pEC50 for hU2-induced aortic contractions at 10'-5M relative to KCl
ChEMBL 1134 19 12 15 1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)NN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.6b00108
155520913 169958 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4449844 169958 0 None - 1 Rat 8.0 pEC50 = 8.0 Binding
Agonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contractionAgonist activity at urotensin 2 receptor in Sprague-Dawley rat thoracic aortic ring assessed as induction of contraction relative to KCl-induced contraction
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44189349 181203 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1059 18 13 14 -0.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4777970 181203 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1059 18 13 14 -0.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104464 209304 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
134134886 143925 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 595 6 2 5 6.2 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(C(F)(F)F)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3906682 143925 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 595 6 2 5 6.2 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(C(F)(F)F)ccc2s1 10.1016/j.bmcl.2016.08.049
134155324 150391 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 557 7 2 6 5.2 COc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3957806 150391 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 557 7 2 6 5.2 COc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
156012877 176857 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1054 17 11 14 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3cccnc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4638745 176857 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1054 17 11 14 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3cccnc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
162657061 180308 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4757669 180308 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104471 209307 5 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
156017817 177245 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1077 16 11 13 1.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4643905 177245 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1077 16 11 13 1.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL3104471 209307 5 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
155552384 173561 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL4546405 173561 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
134156076 150752 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 472 6 2 5 3.4 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccccn1 10.1016/j.bmcl.2016.08.049
CHEMBL3960613 150752 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 472 6 2 5 3.4 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccccn1 10.1016/j.bmcl.2016.08.049
71579840 87880 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 442 9 1 5 4.7 COc1cc(Br)c(CNc2ccc(Cl)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348510 87880 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 442 9 1 5 4.7 COc1cc(Br)c(CNc2ccc(Cl)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
86291695 115745 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1csc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358677 115745 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1csc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc12 10.1016/j.bmcl.2014.09.089
71579744 87873 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348503 87873 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL437430 211960 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
86292101 115753 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 428 6 3 5 3.6 O=C(NCCN1CCC(O)(Cc2ccc(F)cc2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358687 115753 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 428 6 3 5 3.6 O=C(NCCN1CCC(O)(Cc2ccc(F)cc2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL437430 211960 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
134152840 152966 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 477 6 2 5 4.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cccs1 10.1016/j.bmcl.2016.08.049
CHEMBL3979822 152966 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 477 6 2 5 4.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cccs1 10.1016/j.bmcl.2016.08.049
10119117 87892 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 526 9 1 6 4.2 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348523 87892 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 526 9 1 6 4.2 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN(C)C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
156016806 177140 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1129 18 11 13 3.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccc(-c4ccccc4)cc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4642313 177140 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1129 18 11 13 3.8 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccc(-c4ccccc4)cc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
71579748 87877 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348507 87877 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747255 170865 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 507 7 1 5 5.3 CCc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4463082 170865 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 507 7 1 5 5.3 CCc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
123185525 142896 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 617 7 2 5 7.2 Cc1ccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)cc1 10.1016/j.bmcl.2016.08.049
CHEMBL3898238 142896 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 617 7 2 5 7.2 Cc1ccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)cc1 10.1016/j.bmcl.2016.08.049
134133034 143994 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 637 7 2 5 7.5 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccc(Cl)cc3)cc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3907266 143994 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 637 7 2 5 7.5 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccc(Cl)cc3)cc2s1 10.1016/j.bmcl.2016.08.049
86291907 115749 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cccc(CC2(O)CCN(CCNC(=O)Nc3ccnc4ccsc34)CC2)c1 10.1016/j.bmcl.2014.09.089
CHEMBL3358683 115749 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cccc(CC2(O)CCN(CCNC(=O)Nc3ccnc4ccsc34)CC2)c1 10.1016/j.bmcl.2014.09.089
142747275 169068 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 509 7 1 6 4.7 COc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
CHEMBL4437224 169068 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 509 7 1 6 4.7 COc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
142747296 170788 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 547 6 1 5 5.7 O=C(c1ccc(-c2ccccc2C(F)(F)F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4461733 170788 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 547 6 1 5 5.7 O=C(c1ccc(-c2ccccc2C(F)(F)F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747256 175093 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 537 8 1 6 5.5 CC(C)Oc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4581735 175093 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 537 8 1 6 5.5 CC(C)Oc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
142747281 175368 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cccc(F)c2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4588098 175368 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cccc(F)c2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
156013999 176612 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1054 17 11 14 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccncc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4635150 176612 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1054 17 11 14 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccncc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
162648628 179265 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 897 24 13 11 -0.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4745321 179265 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 897 24 13 11 -0.4 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
2164 3457 13 None -1 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
9846574 3457 13 None -1 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL366221 3457 13 None -1 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assayInhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL3104637 209308 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
71580034 87893 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348524 87893 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 7 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(O[C@@H]3CCCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
86305736 115736 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 407 6 3 5 2.8 Cn1ccc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc21 10.1016/j.bmcl.2014.09.089
CHEMBL3358667 115736 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 407 6 3 5 2.8 Cn1ccc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc21 10.1016/j.bmcl.2014.09.089
162671682 182297 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 942 25 13 13 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4792095 182297 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 942 25 13 13 -0.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104637 209308 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
142747285 173565 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 493 6 1 5 5.0 Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4546510 173565 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 493 6 1 5 5.0 Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
142747265 175030 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 523 8 1 6 5.1 CCOc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4580364 175030 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 523 8 1 6 5.1 CCOc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
71719582 87891 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 390 5 1 4 5.1 CN1CC[C@H](Oc2cc(NCc3ccc(Cl)s3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348522 87891 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 390 5 1 4 5.1 CN1CC[C@H](Oc2cc(NCc3ccc(Cl)s3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
134156326 153738 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 555 7 2 5 5.8 CCc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3986509 153738 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 555 7 2 5 5.8 CCc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3104640 209311 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104640 209311 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104471 209307 5 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
86291908 115750 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1ccc(CC2(O)CCN(CCNC(=O)Nc3ccnc4ccsc34)CC2)cc1 10.1016/j.bmcl.2014.09.089
CHEMBL3358684 115750 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1ccc(CC2(O)CCN(CCNC(=O)Nc3ccnc4ccsc34)CC2)cc1 10.1016/j.bmcl.2014.09.089
162646037 178924 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4741230 178924 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
156014461 176606 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1103 16 11 13 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4635039 176606 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1103 16 11 13 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
142747247 173472 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2cccc(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4543925 173472 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2cccc(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
86291906 115748 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1ccccc1CC1(O)CCN(CCNC(=O)Nc2ccnc3ccsc23)CC1 10.1016/j.bmcl.2014.09.089
CHEMBL3358682 115748 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1ccccc1CC1(O)CCN(CCNC(=O)Nc2ccnc3ccsc23)CC1 10.1016/j.bmcl.2014.09.089
86291904 115751 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2ccccc2Br)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358685 115751 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2ccccc2Br)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3104465 209305 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104465 209305 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCc3ccccc3[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
71580135 87898 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348529 87898 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
118723010 115739 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 408 6 3 6 2.2 Cn1cnc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc21 10.1016/j.bmcl.2014.09.089
CHEMBL3358670 115739 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 408 6 3 6 2.2 Cn1cnc2c(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)ccnc21 10.1016/j.bmcl.2014.09.089
71719581 87881 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348511 87881 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 488 7 1 5 5.2 COc1cc(Br)c(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
118723009 115738 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 422 6 3 6 2.5 Cc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2cnn(C)c2n1 10.1016/j.bmcl.2014.09.089
CHEMBL3358669 115738 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 422 6 3 6 2.5 Cc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2cnn(C)c2n1 10.1016/j.bmcl.2014.09.089
11272107 87871 37 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 504 7 1 6 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348501 87871 37 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 504 7 1 6 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
71579747 87876 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348506 87876 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(CNc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747254 169928 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2cccc(-c3ccccc3)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4449461 169928 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2cccc(-c3ccccc3)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747252 172868 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)ccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4529337 172868 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)ccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
71579745 87874 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 487 7 0 5 4.5 COc1cc(Br)c([S+]([O-])Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348504 87874 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 487 7 0 5 4.5 COc1cc(Br)c([S+]([O-])Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
134151496 152679 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 552 6 2 6 5.1 N#Cc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3977330 152679 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 552 6 2 6 5.1 N#Cc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
142747291 169322 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2cccc([N+](=O)[O-])c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4440805 169322 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2cccc([N+](=O)[O-])c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
86291696 115746 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2sccc2n1 10.1016/j.bmcl.2014.09.089
CHEMBL3358679 115746 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2sccc2n1 10.1016/j.bmcl.2014.09.089
145966260 163823 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4213101 163823 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1116 16 12 13 2.3 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(C#Cc3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
142747243 174153 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)cc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4560366 174153 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)cc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747271 174383 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 509 7 1 6 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL4565990 174383 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 509 7 1 6 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1 10.1016/j.bmcl.2018.12.058
CHEMBL3104463 209303 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
71720175 87890 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 356 5 1 4 4.5 CN1CC[C@H](Oc2cc(NCc3cccs3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348521 87890 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 356 5 1 4 4.5 CN1CC[C@H](Oc2cc(NCc3cccs3)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL3104643 209312 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(c2ccccc2)c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104643 209312 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(c2ccccc2)c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104462 209302 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104463 209303 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104462 209302 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](c2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
156016802 177136 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4642307 177136 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1053 17 11 13 2.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
10173280 2934 45 None -3 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
3516 2934 45 None -3 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
CHEMBL567303 2934 45 None -3 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
145978068 163173 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4205274 163173 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1186 18 13 14 1.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
162659637 180701 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1058 30 14 13 -0.0 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4762272 180701 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1058 30 14 13 -0.0 CC(C)[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(N)=O 10.1021/acs.jmedchem.6b00164
162660720 180594 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 908 24 12 11 0.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4761055 180594 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 908 24 12 11 0.2 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
71579839 87879 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(NCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348509 87879 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 454 7 1 5 4.8 COc1cc(Br)c(NCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
142747279 173926 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2ccc([N+](=O)[O-])cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4555094 173926 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 524 7 1 7 4.6 O=C(c1ccc(-c2ccc([N+](=O)[O-])cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
134148271 149396 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 603 7 2 5 6.9 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(-c3ccccc3)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3949719 149396 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 603 7 2 5 6.9 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(-c3ccccc3)ccc2s1 10.1016/j.bmcl.2016.08.049
86291694 115744 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2c(Br)csc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358676 115744 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2c(Br)csc12 10.1016/j.bmcl.2014.09.089
142747238 174951 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccccc2Cl)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4578409 174951 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccccc2Cl)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747253 170527 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 539 8 1 7 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1OC 10.1016/j.bmcl.2018.12.058
CHEMBL4457752 170527 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 539 8 1 7 4.7 COc1ccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)cc1OC 10.1016/j.bmcl.2018.12.058
71579743 87872 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348502 87872 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 503 7 0 6 4.2 COc1cc(Br)c(S(=O)(=O)Cc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
134153111 152017 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 462 6 2 6 3.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccno1 10.1016/j.bmcl.2016.08.049
CHEMBL3971737 152017 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 462 6 2 6 3.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccno1 10.1016/j.bmcl.2016.08.049
71579843 87882 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 382 7 1 3 4.7 CN(C)CCOc1cc(NCc2ccccc2Br)ccc1Cl 10.1016/j.bmcl.2013.01.105
CHEMBL2348513 87882 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 382 7 1 3 4.7 CN(C)CCOc1cc(NCc2ccccc2Br)ccc1Cl 10.1016/j.bmcl.2013.01.105
86292104 115741 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 410 6 3 5 3.5 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358672 115741 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 410 6 3 5 3.5 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
156010342 176489 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1059 17 11 14 2.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccsc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4633010 176489 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1059 17 11 14 2.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(-c3ccsc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL3104459 209299 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104459 209299 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
142747273 171501 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 533 6 1 5 5.1 O=C(c1ccc(-c2cc(F)c(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4472265 171501 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 533 6 1 5 5.1 O=C(c1ccc(-c2cc(F)c(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
142747303 170810 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 547 6 1 5 6.0 O=C(c1ccc(-c2ccc(Cl)c(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4462068 170810 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 547 6 1 5 6.0 O=C(c1ccc(-c2ccc(Cl)c(Cl)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
86291905 115752 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2cccc(Br)c2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358686 115752 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 488 6 3 5 4.3 O=C(NCCN1CCC(O)(Cc2cccc(Br)c2)CC1)Nc1ccnc2ccsc12 10.1016/j.bmcl.2014.09.089
155512483 169087 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
CHEMBL4437489 169087 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1cccc(-c2ccc(C(=O)N3CCN(Cc4ccc(OC5CCNCC5)c(Cl)c4)CC3)o2)c1 10.1016/j.bmcl.2018.12.058
162656670 180326 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 953 25 12 13 0.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4757895 180326 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 953 25 12 13 0.1 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.6b00164
71579746 87875 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 471 7 0 5 5.5 COc1cc(Br)c(SCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348505 87875 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 471 7 0 5 5.5 COc1cc(Br)c(SCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
71720174 87888 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3cc4c(cc3Br)OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348519 87888 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3cc4c(cc3Br)OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
118723011 115740 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 394 6 3 5 3.0 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2ccoc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358671 115740 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 394 6 3 5 3.0 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2ccoc12 10.1016/j.bmcl.2014.09.089
CHEMBL3104638 209309 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104638 209309 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cccc3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
148470142 169099 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
CHEMBL4437619 169099 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 504 6 1 6 4.6 N#Cc1ccccc1-c1ccc(C(=O)N2CCN(Cc3ccc(OC4CCNCC4)c(Cl)c3)CC2)o1 10.1016/j.bmcl.2018.12.058
142747289 170014 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 479 6 1 5 4.7 O=C(c1ccc(-c2ccccc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4450638 170014 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 479 6 1 5 4.7 O=C(c1ccc(-c2ccccc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
162670598 182330 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4792481 182330 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 879 24 12 10 0.0 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
162677235 182903 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4799581 182903 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
123794584 151748 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1ccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)cc1 10.1016/j.bmcl.2016.08.049
CHEMBL3969435 151748 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1ccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)cc1 10.1016/j.bmcl.2016.08.049
134152171 152668 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 572 7 2 7 5.1 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc([N+](=O)[O-])ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3977271 152668 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 572 7 2 7 5.1 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc([N+](=O)[O-])ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3104471 209307 5 None - 1 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
145977223 163427 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4208184 163427 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1092 17 12 13 2.6 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
145973104 164166 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
CHEMBL4217514 164166 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-countingDisplacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
ChEMBL 1142 16 12 13 1.5 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b00789
134133573 142705 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 561 6 2 5 5.8 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(Cl)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3896625 142705 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 561 6 2 5 5.8 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(Cl)ccc2s1 10.1016/j.bmcl.2016.08.049
71579935 87884 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 372 7 1 3 4.9 CN(C)CCOc1cc(NCc2ccccc2C(F)(F)F)ccc1Cl 10.1016/j.bmcl.2013.01.105
CHEMBL2348515 87884 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 372 7 1 3 4.9 CN(C)CCOc1cc(NCc2ccccc2C(F)(F)F)ccc1Cl 10.1016/j.bmcl.2013.01.105
71718978 87889 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 440 8 1 6 4.4 COc1cc(OC)c(OC)cc1CNc1ccc(C(F)(F)F)c(O[C@H]2CCN(C)C2)c1 10.1016/j.bmcl.2013.01.105
CHEMBL2348520 87889 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 440 8 1 6 4.4 COc1cc(OC)c(OC)cc1CNc1ccc(C(F)(F)F)c(O[C@H]2CCN(C)C2)c1 10.1016/j.bmcl.2013.01.105
134141359 146251 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 545 6 2 5 5.3 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(F)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3924660 146251 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 545 6 2 5 5.3 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(F)ccc2s1 10.1016/j.bmcl.2016.08.049
134142270 145080 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1ccccc1-c1ccc2cc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)sc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3915656 145080 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1ccccc1-c1ccc2cc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)sc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3104639 209310 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104639 209310 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(I)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
142747294 170490 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4457118 170490 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2ccc(F)c(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
21023902 3466 25 None 2 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
2165 3466 25 None 2 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
CHEMBL522770 3466 25 None 2 3 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1016/j.bmcl.2013.01.105
142747268 171026 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2ccc(-c3ccccc3)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4465326 171026 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 555 7 1 5 6.4 O=C(c1ccc(-c2ccc(-c3ccccc3)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL3104461 209301 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
86291697 115747 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 438 7 3 5 4.1 CCc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2sccc2n1 10.1016/j.bmcl.2014.09.089
CHEMBL3358680 115747 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 438 7 3 5 4.1 CCc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2sccc2n1 10.1016/j.bmcl.2014.09.089
CHEMBL3104461 209301 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
162651887 179681 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4750625 179681 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
86305831 115737 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 407 6 3 5 2.8 Cn1ccc2nccc(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)c21 10.1016/j.bmcl.2014.09.089
CHEMBL3358668 115737 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 407 6 3 5 2.8 Cn1ccc2nccc(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)c21 10.1016/j.bmcl.2014.09.089
142747251 171914 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)cc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4483058 171914 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 515 6 1 5 5.0 O=C(c1ccc(-c2cc(F)cc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
134140417 145734 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 473 6 2 6 2.8 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cnccn1 10.1016/j.bmcl.2016.08.049
CHEMBL3920751 145734 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 473 6 2 6 2.8 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cnccn1 10.1016/j.bmcl.2016.08.049
71716535 87887 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3c(Br)ccc4c3OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348518 87887 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 472 5 1 5 4.9 CN1CC[C@H](Oc2cc(NCc3c(Br)ccc4c3OCO4)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
71580035 87895 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 568 9 1 7 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN3CCOCC3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348526 87895 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 568 9 1 7 4.0 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN3CCOCC3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
134141963 146452 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 527 6 2 5 5.2 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3926450 146452 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 527 6 2 5 5.2 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2016.08.049
142747298 172674 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccc(Cl)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4524693 172674 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 513 6 1 5 5.3 O=C(c1ccc(-c2ccc(Cl)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
71579838 87878 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 455 7 0 5 4.8 COc1cc(Br)c(OCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348508 87878 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 455 7 0 5 4.8 COc1cc(Br)c(OCc2ccc(Cl)c(O[C@@H]3CCN(C)C3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
10303115 10312 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 560 9 2 5 6.2 COc1cc2c(cc1OC)C(CCc1cc(F)ccc1F)N(CCNC(=O)Nc1cc(C)nc3ccccc13)CC2 10.1021/jm901294u
CHEMBL1163360 10312 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 560 9 2 5 6.2 COc1cc2c(cc1OC)C(CCc1cc(F)ccc1F)N(CCNC(=O)Nc1cc(C)nc3ccccc13)CC2 10.1021/jm901294u
142747258 173232 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccc(F)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4538387 173232 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccc(F)cc2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
71717140 87886 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 380 6 1 4 4.4 COc1cccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)c1 10.1016/j.bmcl.2013.01.105
CHEMBL2348517 87886 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 380 6 1 4 4.4 COc1cccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)c1 10.1016/j.bmcl.2013.01.105
156012366 176823 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1083 19 11 14 2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(OCc3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
CHEMBL4638346 176823 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting methodAntagonist activity at human UT receptor expressed in HEK293 cells using Na [125I] incubated for 2 hrs by gamma counting method
ChEMBL 1083 19 11 14 2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(OCc3ccccc3)cc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acsmedchemlett.0c00223
71718372 87885 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 380 6 1 4 4.4 COc1ccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1 10.1016/j.bmcl.2013.01.105
CHEMBL2348516 87885 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 380 6 1 4 4.4 COc1ccc(CNc2ccc(C(F)(F)F)c(O[C@H]3CCN(C)C3)c2)cc1 10.1016/j.bmcl.2013.01.105
134151328 151688 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 541 6 2 5 5.5 Cc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3968841 151688 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 541 6 2 5 5.5 Cc1ccc2sc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)cc2c1 10.1016/j.bmcl.2016.08.049
123922871 152740 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 621 7 2 5 7.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccc(F)cc3)cc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3977836 152740 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 621 7 2 5 7.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccc(F)cc3)cc2s1 10.1016/j.bmcl.2016.08.049
134146007 148425 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 461 6 2 5 3.6 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccco1 10.1016/j.bmcl.2016.08.049
CHEMBL3942137 148425 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 461 6 2 5 3.6 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccco1 10.1016/j.bmcl.2016.08.049
86294592 115743 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cc2nccc(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)c2s1 10.1016/j.bmcl.2014.09.089
CHEMBL3358674 115743 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 424 6 3 5 3.8 Cc1cc2nccc(NC(=O)NCCN3CCC(O)(Cc4ccccc4)CC3)c2s1 10.1016/j.bmcl.2014.09.089
162668637 182055 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4788762 182055 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 890 24 11 10 0.7 CCC(NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL3104644 209313 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
123264706 142817 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 552 6 2 6 5.1 N#Cc1ccc2cc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)sc2c1 10.1016/j.bmcl.2016.08.049
CHEMBL3897677 142817 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 552 6 2 6 5.1 N#Cc1ccc2cc(C(=O)NC3CCN(Cc4ccc(OC5CCNCC5)c(Br)c4)CC3)sc2c1 10.1016/j.bmcl.2016.08.049
71580134 87897 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348528 87897 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 552 8 1 6 4.8 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OC[C@H]3CCCN3C)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL3104460 209300 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104460 209300 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H]2Cc3c([nH]c4ccccc34)CN(C2=O)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
71717139 87883 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 428 5 1 3 5.2 CN1CC[C@H](Oc2cc(NCc3ccccc3Br)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
CHEMBL2348514 87883 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 428 5 1 3 5.2 CN1CC[C@H](Oc2cc(NCc3ccccc3Br)ccc2C(F)(F)F)C1 10.1016/j.bmcl.2013.01.105
71580133 87896 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 581 9 1 7 3.9 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN3CCN(C)CC3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
CHEMBL2348527 87896 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assayDisplacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay
ChEMBL 581 9 1 7 3.9 COc1cc(Br)c(S(=O)(=O)Nc2ccc(C(F)(F)F)c(OCCN3CCN(C)CC3)c2)cc1OC 10.1016/j.bmcl.2013.01.105
134142581 145084 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 605 6 2 5 6.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(Br)ccc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3915670 145084 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 605 6 2 5 6.0 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2cc(Br)ccc2s1 10.1016/j.bmcl.2016.08.049
134156353 153816 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1cccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)c1 10.1016/j.bmcl.2016.08.049
CHEMBL3987058 153816 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 633 8 2 6 6.9 COc1cccc(-c2ccc3cc(C(=O)NC4CCN(Cc5ccc(OC6CCNCC6)c(Br)c5)CC4)sc3c2)c1 10.1016/j.bmcl.2016.08.049
CHEMBL3104467 209306 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3ccccc3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
CHEMBL3104467 209306 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3ccccc3C[C@@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
162644923 178839 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 911 25 12 11 -0.1 COc1ccc(C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](CS)C(N)=O)cc1 10.1021/acs.jmedchem.6b00164
CHEMBL4740325 178839 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr9]-U-II from human U-IIR expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 911 25 12 11 -0.1 COc1ccc(C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CC(N)=O)C(=O)N[C@@H](CS)C(N)=O)cc1 10.1021/acs.jmedchem.6b00164
155543279 172714 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2cccc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4525919 172714 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2cccc(F)c2)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL3104644 209313 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysisDisplacement of [125I]-Urotensin-2 from human GPR14 expressed in CHO cells after 90 mins by gamma counting analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N2Cc3[nH]c4ccccc4c3C[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm401153j
134151441 152843 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 603 7 2 5 6.9 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccccc3)cc2s1 10.1016/j.bmcl.2016.08.049
CHEMBL3978782 152843 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 603 7 2 5 6.9 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cc2ccc(-c3ccccc3)cc2s1 10.1016/j.bmcl.2016.08.049
142747242 169957 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
CHEMBL4449808 169957 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assayDisplacement of Eu-labelled UT2 from recombinant human UT2 receptor expressed in HEK293 cell membranes preincubated for 10 mins followed by Eu-labelled UT2 addition and measured after 90 mins by TRF assay
ChEMBL 497 6 1 5 4.8 O=C(c1ccc(-c2ccccc2F)o1)N1CCN(Cc2ccc(OC3CCNCC3)c(Cl)c2)CC1 10.1016/j.bmcl.2018.12.058
118723012 115742 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 410 6 3 5 3.5 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2sccc12 10.1016/j.bmcl.2014.09.089
CHEMBL3358673 115742 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assayDisplacement of europium-labeled urotensin-II from human urotensin-2 receptor expressed in HEK293 cells by TRF assay
ChEMBL 410 6 3 5 3.5 O=C(NCCN1CCC(O)(Cc2ccccc2)CC1)Nc1ccnc2sccc12 10.1016/j.bmcl.2014.09.089
134138102 147312 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 478 6 2 6 3.4 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cscn1 10.1016/j.bmcl.2016.08.049
CHEMBL3933152 147312 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assayDisplacement of europium-labeled urotensin-2 from human recombinant urotensin-2 receptor expressed in HEK293 cell membranes after 90 mins by filtration based time resolved fluorometric assay
ChEMBL 478 6 2 6 3.4 O=C(NC1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)CC1)c1cscn1 10.1016/j.bmcl.2016.08.049
CHEMBL1165797 206782 0 None - 1 Rat 10.7 pKi = 10.7 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL577772 213990 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL577772 213990 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Displacement of [125I]urotensin 2 from rat urotensin 2 receptor expressed in CHOK1 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from rat urotensin 2 receptor expressed in CHOK1 cells by scintillation proximity assay
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm900683d
CHEMBL1163463 206767 6 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm901294u
CHEMBL390094 210680 1 None - 1 Human 9.7 pKi = 9.7 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm025549i
CHEMBL390094 210680 1 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0309912
CHEMBL390094 210680 1 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL390094 210680 1 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL3315139 209607 9 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL426020 211585 0 None - 1 Human 9.6 pKi = 9.6 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm025549i
CHEMBL426020 211585 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0309912
CHEMBL426020 211585 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL426020 211585 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL218994 207648 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL504097 212393 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44561239 173124 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 563 10 1 5 5.4 CN(C(=O)CN(CC#N)c1ccc(Cl)c(Cl)c1)C(CN1CCCC1)c1ccc(-c2cccc(C(N)=O)c2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL453587 173124 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 563 10 1 5 5.4 CN(C(=O)CN(CC#N)c1ccc(Cl)c(Cl)c1)C(CN1CCCC1)c1ccc(-c2cccc(C(N)=O)c2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL3315142 209610 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N1)C(=O)O 10.1021/jm500218x
44449106 94657 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 501 5 0 4 4.6 O=C1COc2cc(Cl)c(Cl)cc2N1CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL255509 94657 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 501 5 0 4 4.6 O=C1COc2cc(Cl)c(Cl)cc2N1CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
44449079 95006 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 5 0 4 3.9 Cc1cc2c(cc1C)N(CC(=O)N1CCCC(c3ccccc3)C1CN1CCCC1)C(=O)CO2 10.1016/j.bmcl.2008.05.027
CHEMBL257171 95006 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 5 0 4 3.9 Cc1cc2c(cc1C)N(CC(=O)N1CCCC(c3ccccc3)C1CN1CCCC1)C(=O)CO2 10.1016/j.bmcl.2008.05.027
44449053 94959 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 498 5 0 5 4.6 O=C(Cn1c(=O)cnc2cc(Cl)c(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL256989 94959 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 498 5 0 5 4.6 O=C(Cn1c(=O)cnc2cc(Cl)c(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL3315141 209609 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315148 209616 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL437430 211960 0 None - 1 Human 9.1 pKi = 9.1 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm025549i
CHEMBL437430 211960 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0309912
CHEMBL437430 211960 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL437430 211960 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL509604 213790 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL593662 214026 9 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL510618 213799 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL2371933 208400 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
44449004 95061 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 458 5 0 5 3.9 Cc1cc2ncc(=O)n(CC(=O)N3CCCC(c4ccccc4)C3CN3CCCC3)c2cc1C 10.1016/j.bmcl.2008.05.027
CHEMBL257415 95061 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 458 5 0 5 3.9 Cc1cc2ncc(=O)n(CC(=O)N3CCCC(c4ccccc4)C3CN3CCCC3)c2cc1C 10.1016/j.bmcl.2008.05.027
CHEMBL3315147 209615 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL385281 210589 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0602110
44448876 94647 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 469 5 0 5 4.6 O=C(Cn1c(=O)sc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL255462 94647 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 469 5 0 5 4.6 O=C(Cn1c(=O)sc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL218994 207648 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL3315146 209614 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL2370836 208177 0 None - 1 Human 8.9 pKi = 8.9 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(C)(C)SSC1(C)C)C(=O)O 10.1021/jm025549i
CHEMBL2370836 208177 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(C)(C)SSC1(C)C)C(=O)O 10.1021/jm0309912
CHEMBL224616 207694 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL388060 210657 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL374468 210444 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CN[C@@H](CC(=O)O)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](C(=O)O)C(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0602110
CHEMBL448403 212196 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
155536007 171550 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4472928 171550 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
135747623 174483 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568153 174483 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL3315144 209612 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2nc3ccccc3s2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315152 209620 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315150 209618 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL3315140 209608 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O 10.1021/jm500218x
44580517 187426 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 2 4.7 c1ccc2c(c1)[nH]c1ccnc(NCC3CCCCC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497562 187426 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 2 4.7 c1ccc2c(c1)[nH]c1ccnc(NCC3CCCCC3)c12 10.1016/j.bmcl.2008.08.054
44580475 192607 0 None 39 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL523566 192607 0 None 39 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
25067045 154958 0 None -1 2 Rat 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from rat urotensin 2 receptorDisplacement of [125I]human urotensin 2 from rat urotensin 2 receptor
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL404177 154958 0 None -1 2 Rat 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin 2 from rat urotensin 2 receptorDisplacement of [125I]human urotensin 2 from rat urotensin 2 receptor
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL412179 211217 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(N)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL389654 210675 0 None 5 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
44568398 182942 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 539 7 2 4 4.9 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL479994 182942 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 539 7 2 4 4.9 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44448290 94914 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.0 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256773 94914 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.0 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2008.03.078
44580679 187408 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1nccc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497368 187408 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1nccc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
44580518 187463 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 287 4 2 2 4.4 c1ccc(CCNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL497765 187463 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 287 4 2 2 4.4 c1ccc(CCNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
44399254 67279 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 509 13 3 5 3.9 CC(C)C[C@H](NC(=O)Nc1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL190501 67279 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 509 13 3 5 3.9 CC(C)C[C@H](NC(=O)Nc1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44580519 187291 0 None -15 2 Cat 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
CHEMBL496516 187291 0 None -15 2 Cat 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
12704866 187744 0 None -63 2 Cat 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL500880 187744 0 None -63 2 Cat 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
44448714 95051 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257365 95051 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44568339 183257 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 539 8 1 4 5.2 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL480776 183257 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 539 8 1 4 5.2 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44534500 193326 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 6 1 4 4.4 Cc1cc(CN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)ccc1OC1CCN(C)C1 10.1016/j.bmcl.2008.06.019
CHEMBL548340 193326 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 6 1 4 4.4 Cc1cc(CN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)ccc1OC1CCN(C)C1 10.1016/j.bmcl.2008.06.019
25127071 196872 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578203 196872 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 626 12 0 8 5.1 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
25124736 196874 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578205 196874 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 574 11 2 7 4.1 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2c(C)n[nH]c2C)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL509042 213478 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
10120078 67285 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL190533 67285 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL1163479 206773 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
46907359 10349 0 None 50 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 536 12 2 6 4.4 CC(C)[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1021/jm901294u
CHEMBL1164523 10349 0 None 50 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 536 12 2 6 4.4 CC(C)[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1021/jm901294u
10190075 188162 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 676 10 3 7 4.5 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL505360 188162 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 676 10 3 7 4.5 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL3315151 209619 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL2370837 208178 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cellsAbility to displace radioligand [125I]Tyr-hU-II from human recombinant Urotensin 2 receptor in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)CC(=O)O)CSSC1(C)C)C(=O)O 10.1021/jm025549i
CHEMBL2372643 208523 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human Urotensin 2 receptor was determinedBinding affinity towards human Urotensin 2 receptor was determined
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)CSSC1(C)C)C(=O)O 10.1021/jm0309912
44580564 187210 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 255 5 2 3 3.2 CCOCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL495907 187210 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 255 5 2 3 3.2 CCOCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580476 187217 0 None 125 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CC(C)CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL495937 187217 0 None 125 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CC(C)CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
12704866 187744 0 None 63 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL500880 187744 0 None 63 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 3 2 2 4.3 c1ccc(CNc2nccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmcl.2008.08.054
CHEMBL387916 210656 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL3315145 209613 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2nc3ccccc3s2)C(=O)N1)C(=O)O 10.1021/jm500218x
44597398 195113 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565580 195113 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44568429 190161 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 575 6 2 5 4.1 O=C(N[C@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL518312 190161 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 575 6 2 5 4.1 O=C(N[C@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
10278166 3459 32 None 2 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat urotensin 2 receptorBinding affinity to rat urotensin 2 receptor
ChEMBL 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 10.1021/jm901294u
3531 3459 32 None 2 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat urotensin 2 receptorBinding affinity to rat urotensin 2 receptor
ChEMBL 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 10.1021/jm901294u
CHEMBL1164033 3459 32 None 2 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat urotensin 2 receptorBinding affinity to rat urotensin 2 receptor
ChEMBL 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 10.1021/jm901294u
10120078 67285 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL190533 67285 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 550 13 2 6 4.8 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399063 68272 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 562 13 2 5 4.9 CC(C)C[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL191793 68272 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 562 13 2 5 4.9 CC(C)C[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44580475 192607 0 None -39 2 Cat 5.9 pKi = 5.9 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL523566 192607 0 None -39 2 Cat 5.9 pKi = 5.9 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCC(C)CNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448653 171157 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 392 4 0 4 3.8 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCOCC1 10.1016/j.bmcl.2008.03.078
CHEMBL446717 171157 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 392 4 0 4 3.8 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCOCC1 10.1016/j.bmcl.2008.03.078
44561196 172931 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)C(CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL453074 172931 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)C(CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
44593421 186110 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)[C@@H](CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL488470 186110 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)[C@@H](CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
23627666 195439 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567759 195439 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 700 13 2 9 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL508811 213356 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44449136 154709 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 519 9 0 5 4.6 COCCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL402813 154709 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 519 9 0 5 4.6 COCCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
44596966 195622 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568764 195622 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 651 12 1 9 5.4 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL415851 211447 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)CC(=O)O)CSSC[C@@H](C(=O)N[C@H](C(=O)O)C(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm0602110
24804491 89510 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 610 7 1 6 5.3 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL238066 89510 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 610 7 1 6 5.3 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
10210584 183466 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 589 6 2 5 4.5 O=C(NC1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482302 183466 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 589 6 2 5 4.5 O=C(NC1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
45486917 195748 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 620 12 1 8 4.3 COc1ccc([C@@H](CCCNS(C)(=O)=O)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569689 195748 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 620 12 1 8 4.3 COc1ccc([C@@H](CCCNS(C)(=O)=O)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44561123 192881 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)C(CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL527199 192881 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)C(CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL1165794 206780 1 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
44597071 196875 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578206 196875 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 637 12 1 8 5.8 COc1ccc([C@@H](CCCNC(=O)c2cnoc2C)N2Cc3c(cccc3N3CCN([C@H](C)c4ccccc4)CC3)C2=O)cc1OC 10.1021/jm900683d
44568399 191975 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 495 7 2 4 4.8 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(Cl)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL521418 191975 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 495 7 2 4 4.8 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(Cl)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44448469 94739 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 432 5 0 3 5.6 Cc1ccc2scc(CC(=O)N3CCC[C@H](c4ccccc4)[C@@H]3CN3CCCC3)c2c1 10.1016/j.bmcl.2008.03.078
CHEMBL255927 94739 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 432 5 0 3 5.6 Cc1ccc2scc(CC(=O)N3CCC[C@H](c4ccccc4)[C@@H]3CN3CCCC3)c2c1 10.1016/j.bmcl.2008.03.078
25067046 154621 3 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL402303 154621 3 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL389653 210674 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL500949 212348 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44596869 195253 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566366 195253 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 584 11 2 9 3.3 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCNCC4)c3C2=O)cc1OC 10.1021/jm900683d
44534506 183461 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 554 8 2 5 4.0 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482258 183461 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 554 8 2 5 4.0 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
155540766 171931 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N(C)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4483461 171931 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N(C)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL425467 211578 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
10230399 122823 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 534 13 2 6 4.3 CC(C)C[C@H](NC(=O)c1cc2ccccc2o1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL361664 122823 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 534 13 2 6 4.3 CC(C)C[C@H](NC(=O)c1cc2ccccc2o1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448314 168179 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 441 6 0 3 5.1 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2008.03.078
CHEMBL437216 168179 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 441 6 0 3 5.1 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2008.03.078
44580476 187217 0 None -125 2 Cat 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CC(C)CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL495937 187217 0 None -125 2 Cat 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CC(C)CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448691 94443 3 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL254153 94443 3 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44448337 94789 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 487 6 0 3 5.2 CC(=O)N(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256159 94789 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 487 6 0 3 5.2 CC(=O)N(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44580436 171852 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 211 2 2 2 3.1 CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL447747 171852 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 211 2 2 2 3.1 CCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448775 94480 2 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL254356 94480 2 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
44561197 172932 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)[C@@H](CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL453075 172932 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)[C@@H](CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
44448775 94480 2 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL254356 94480 2 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
44597068 195085 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565395 195085 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 700 13 1 10 4.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL3315153 209621 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
24804325 144809 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 614 8 1 5 5.2 O=C(NCC1CCN(C(=O)c2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL391355 144809 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 614 8 1 5 5.2 O=C(NCC1CCN(C(=O)c2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
23627554 195219 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 471 7 0 6 3.8 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566187 195219 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 471 7 0 6 3.8 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627556 196790 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL577518 196790 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44448691 94443 3 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL254153 94443 3 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@@H](c2ccccc2)[C@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL1163471 206769 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
25126424 195337 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL567075 195337 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 562 11 1 7 4.8 CCN1CCN(c2cccc3c2CN([C@H](CCCNC(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
25125764 195505 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL568123 195505 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 548 12 1 7 5.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNCc2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44568526 189945 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 626 11 3 6 5.0 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(CCc2ccc(O[C@@H]3CCNC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL517991 189945 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 626 11 3 6 5.0 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(CCc2ccc(O[C@@H]3CCNC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL376223 210486 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL501579 212359 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44580563 192525 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 241 4 2 3 2.8 COCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL522895 192525 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 241 4 2 3 2.8 COCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
2164 3457 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
9846574 3457 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL366221 3457 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
12052419 67673 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 572 13 2 5 4.3 CC(C)C[C@H](NC(=O)c1ccc(Br)cc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL191401 67673 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 572 13 2 5 4.3 CC(C)C[C@H](NC(=O)c1ccc(Br)cc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44580473 187345 0 None -31 2 Cat 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 6 2 2 4.7 CCCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL496920 187345 0 None -31 2 Cat 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 6 2 2 4.7 CCCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448474 94784 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CC[C@H](c2ccccc2)C[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL256140 94784 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CC[C@H](c2ccccc2)C[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448317 94862 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 419 6 0 3 4.6 Cc1ccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)cc1C 10.1016/j.bmcl.2008.03.078
CHEMBL256516 94862 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 419 6 0 3 4.6 Cc1ccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)cc1C 10.1016/j.bmcl.2008.03.078
44448514 154892 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 4.8 C[C@H]1CCCN(C(=O)Cc2csc3ccc(Cl)cc23)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL403833 154892 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 4.8 C[C@H]1CCCN(C(=O)Cc2csc3ccc(Cl)cc23)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44399475 67233 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3cc(Cl)cc(Cl)c3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL190137 67233 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3cc(Cl)cc(Cl)c3)C2)cc1 10.1016/j.bmcl.2005.04.074
44399166 170435 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 495 13 2 6 2.9 CC(C)C[C@H](NC(=O)c1ccncc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL445655 170435 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 495 13 2 6 2.9 CC(C)C[C@H](NC(=O)c1ccncc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448549 95204 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 5.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL258017 95204 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 5.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL375241 210458 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
44449228 95143 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 484 7 0 4 5.2 N#CCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL257767 95143 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 484 7 0 4 5.2 N#CCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
44449107 154654 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 517 5 0 5 3.8 O=C1COc2cc(Cl)c(Cl)cc2N1CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
CHEMBL402520 154654 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 517 5 0 5 3.8 O=C1COc2cc(Cl)c(Cl)cc2N1CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
155544020 172733 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4526244 172733 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL218825 207646 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)C(C)(C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL3315149 209617 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(Cl)c(Cl)c2)C(=O)N1)C(=O)O 10.1021/jm500218x
CHEMBL265166 208884 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)c([N+](=O)[O-])c2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL524855 213836 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H]2Cc3ccccc3CN2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL216712 207585 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0602110
155567837 175453 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4590360 175453 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL266651 208935 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CCC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
44561157 186128 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 495 8 0 3 6.4 CN(CC(=O)N(C)C(CN1CCCC1)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL488642 186128 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 495 8 0 3 6.4 CN(CC(=O)N(C)C(CN1CCCC1)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
155537736 171770 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4475783 171770 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
2164 3457 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
9846574 3457 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
CHEMBL366221 3457 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
CHEMBL1163475 206771 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
23627305 195747 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 642 11 1 8 6.2 COc1ccc(C(CCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569688 195747 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 642 11 1 8 6.2 COc1ccc(C(CCCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
2164 3457 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
9846574 3457 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
CHEMBL366221 3457 13 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2008.06.019
155550733 173702 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N(C)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4549818 173702 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N(C)[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
155524911 170341 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N(C)[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4455086 170341 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N(C)[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL505288 212410 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
155537097 171680 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4474481 171680 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
155560750 174499 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4568539 174499 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL219356 207657 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccc(C(C)(C)C)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0602110
23627555 196070 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL571683 196070 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc([C@@H](C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44534510 182940 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 615 8 1 4 6.8 O=C(N[C@H]1CCN(Cc2ccc(OC3CCN(Cc4ccccc4)CC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL479993 182940 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 615 8 1 4 6.8 O=C(N[C@H]1CCN(Cc2ccc(OC3CCN(Cc4ccccc4)CC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
155519842 169796 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4447811 169796 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
45487731 196876 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL578207 196876 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 582 12 2 8 3.0 CCN1CCN(c2cccc3c2CN([C@H](CCCNS(=O)(=O)c2c[nH]cn2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44448510 95047 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 458 5 0 3 6.4 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](C2CCCCC2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257337 95047 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 458 5 0 3 6.4 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](C2CCCCC2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580519 187291 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
CHEMBL496516 187291 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 3 4.4 c1csc(CNc2nccc3[nH]c4ccccc4c23)c1 10.1016/j.bmcl.2008.08.054
44580437 188480 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 225 3 2 2 3.5 CCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL509831 188480 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 225 3 2 2 3.5 CCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44561156 186126 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)[C@H](CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL488635 186126 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 419 7 0 3 4.7 CN(CC(=O)N(C)[C@H](CN1CCCC1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
2164 3457 13 None -1 3 Rhesus macaque 6.6 pKi = 6.6 Binding
Binding affinity for monkey urotensin-2 receptorBinding affinity for monkey urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
9846574 3457 13 None -1 3 Rhesus macaque 6.6 pKi = 6.6 Binding
Binding affinity for monkey urotensin-2 receptorBinding affinity for monkey urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL366221 3457 13 None -1 3 Rhesus macaque 6.6 pKi = 6.6 Binding
Binding affinity for monkey urotensin-2 receptorBinding affinity for monkey urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
44399168 134650 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 510 13 2 6 3.9 CC(C)C[C@H](NC(=O)Oc1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL372019 134650 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 510 13 2 6 3.9 CC(C)C[C@H](NC(=O)Oc1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448431 95091 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 418 5 0 3 5.3 O=C(Cc1csc2ccccc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257563 95091 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 418 5 0 3 5.3 O=C(Cc1csc2ccccc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44399476 67150 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 425 9 1 6 2.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL189482 67150 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 425 9 1 6 2.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc4c(c3)OCO4)C2)cc1 10.1016/j.bmcl.2005.04.074
44399169 135046 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 381 9 1 4 3.0 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccccc3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL372911 135046 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 381 9 1 4 3.0 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccccc3)C2)cc1 10.1016/j.bmcl.2005.04.074
44399083 159489 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 432 12 2 5 2.3 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL410825 159489 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 432 12 2 5 2.3 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399234 161299 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 421 9 1 5 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3cc4ccccc4o3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL414847 161299 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 421 9 1 5 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3cc4ccccc4o3)C2)cc1 10.1016/j.bmcl.2005.04.074
44580515 187425 0 None -89 2 Cat 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497561 187425 0 None -89 2 Cat 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
44448394 154656 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 430 5 0 2 5.4 O=C(Cc1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL402543 154656 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 430 5 0 2 5.4 O=C(Cc1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580477 188179 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 223 2 2 2 3.3 c1ccc2c(c1)[nH]c1ccnc(NC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL505617 188179 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 223 2 2 2 3.3 c1ccc2c(c1)[nH]c1ccnc(NC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL505358 212411 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2cccc3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
11995575 3886 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None None 10.1021/jm0602110
2156 3886 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None None 10.1021/jm0602110
CHEMBL437110 3886 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None None 10.1021/jm0602110
24804324 89450 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 608 8 1 5 5.4 CC(C)(C)CC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL237879 89450 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 608 8 1 5 5.4 CC(C)(C)CC(=O)N1CCC(CNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
44596867 195285 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 674 12 1 9 5.4 COc1ccc(C(CCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566565 195285 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 674 12 1 9 5.4 COc1ccc(C(CCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
45486910 195690 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 660 11 1 9 5.0 COc1ccc(C(CNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL569238 195690 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 660 11 1 9 5.0 COc1ccc(C(CNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44561240 172036 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 570 8 1 6 4.2 CC(=O)Nc1ccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)CN3C(=O)COc4cc(C)c(C)cc43)cc2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL449192 172036 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 570 8 1 6 4.2 CC(=O)Nc1ccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)CN3C(=O)COc4cc(C)c(C)cc43)cc2)cc1 10.1016/j.bmcl.2008.05.058
44561238 172928 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 582 12 1 5 5.5 COCCN(CC(=O)N(C)C(CN1CCCC1)c1ccc(-c2ccc(C(N)=O)cc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL453067 172928 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 582 12 1 5 5.5 COCCN(CC(=O)N(C)C(CN1CCCC1)c1ccc(-c2ccc(C(N)=O)cc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
44449052 94958 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 514 5 0 6 3.8 O=C(Cn1c(=O)cnc2cc(Cl)c(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
CHEMBL256988 94958 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 514 5 0 6 3.8 O=C(Cn1c(=O)cnc2cc(Cl)c(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
10121972 182462 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 626 10 3 6 5.3 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL479413 182462 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 626 10 3 6 5.3 CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N[C@H]1CCN(Cc2ccc(OC3CCNCC3)c(Br)c2)C1 10.1016/j.bmcl.2008.06.019
2164 3457 13 None 1 3 Rat 8.5 pKi = 8.5 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
9846574 3457 13 None 1 3 Rat 8.5 pKi = 8.5 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
CHEMBL366221 3457 13 None 1 3 Rat 8.5 pKi = 8.5 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1021/jm901294u
155524087 170316 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4454498 170316 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1074 18 12 14 0.7 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
155529504 170856 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4462940 170856 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1C)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL507406 212529 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2cccc3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
25067045 154958 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL404177 154958 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
25067560 187378 0 None 31 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497171 187378 0 None 31 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580472 187379 0 None 100 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 5 2 2 4.3 CCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497172 187379 0 None 100 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 5 2 2 4.3 CCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
24804323 90375 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 643 9 2 5 5.3 O=C(NCC1CCN(C(=O)NCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL239199 90375 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 643 9 2 5 5.3 O=C(NCC1CCN(C(=O)NCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44435044 90439 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 664 10 1 6 4.9 O=C(NCC1CCN(S(=O)(=O)Cc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL239250 90439 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 664 10 1 6 4.9 O=C(NCC1CCN(S(=O)(=O)Cc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
44448513 94689 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 434 7 0 4 5.0 CCCO[C@H]1CCCN(C(=O)Cc2csc3ccc(Cl)cc23)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL255665 94689 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 434 7 0 4 5.0 CCCO[C@H]1CCCN(C(=O)Cc2csc3ccc(Cl)cc23)[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448471 94783 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1C[C@H](c2ccccc2)CC[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL256138 94783 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1C[C@H](c2ccccc2)CC[C@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448338 94790 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 473 7 0 3 5.7 CCN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256160 94790 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 473 7 0 3 5.7 CCN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44580683 187438 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 269 5 2 3 3.9 CCCCNc1ccnc2[nH]c3c(OC)cccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497580 187438 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 269 5 2 3 3.9 CCCCNc1ccnc2[nH]c3c(OC)cccc3c12 10.1016/j.bmcl.2008.08.054
23627492 195172 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 513 8 0 6 5.3 CCC(c1ccc(OC)c(OC)c1)N1C(=O)c2cccc(N3CCN([C@H](C)c4ccccc4)CC3)c2C1=O 10.1021/jm900683d
CHEMBL565937 195172 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 513 8 0 6 5.3 CCC(c1ccc(OC)c(OC)c1)N1C(=O)c2cccc(N3CCN([C@H](C)c4ccccc4)CC3)c2C1=O 10.1021/jm900683d
23627613 195252 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 507 7 0 6 4.1 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5c(F)cccc5F)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566364 195252 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 507 7 0 6 4.1 COc1ccc(CN2C(=O)c3cccc(N4CCN(Cc5c(F)cccc5F)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627557 195259 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc(C(C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566389 195259 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 499 7 0 6 4.9 COc1ccc(C(C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44399163 96314 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL264726 96314 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2005.04.074
44580634 187214 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 241 4 2 3 2.8 COCCNc1ccnc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL495920 187214 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 241 4 2 3 2.8 COCCNc1ccnc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
2164 3457 13 None 1 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat urotensin-2 receptorBinding affinity for rat urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
9846574 3457 13 None 1 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat urotensin-2 receptorBinding affinity for rat urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
CHEMBL366221 3457 13 None 1 3 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat urotensin-2 receptorBinding affinity for rat urotensin-2 receptor
ChEMBL 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2005.04.074
44399453 67469 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 534 13 2 6 4.3 CC(C)C[C@@H](NC(=O)c1cc2ccccc2o1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL190975 67469 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 534 13 2 6 4.3 CC(C)C[C@@H](NC(=O)c1cc2ccccc2o1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448361 160895 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 446 6 0 3 6.0 Cc1ccc2scc(CCC(=O)N3CCC[C@H](c4ccccc4)[C@@H]3CN3CCCC3)c2c1 10.1016/j.bmcl.2008.03.078
CHEMBL412746 160895 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 446 6 0 3 6.0 Cc1ccc2scc(CCC(=O)N3CCC[C@H](c4ccccc4)[C@@H]3CN3CCCC3)c2c1 10.1016/j.bmcl.2008.03.078
44448734 168426 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 391 6 0 3 4.0 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccccc1 10.1016/j.bmcl.2008.03.078
CHEMBL439244 168426 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 391 6 0 3 4.0 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccccc1 10.1016/j.bmcl.2008.03.078
44596965 195153 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565806 195153 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 687 13 1 10 5.0 COc1ccc([C@@H](CCCNS(=O)(=O)c2cnoc2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44399163 96314 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2008.06.019
CHEMBL264726 96314 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2008.06.019
23627251 197231 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 542 10 1 7 4.7 COc1ccc(C(CCCN)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL584545 197231 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 542 10 1 7 4.7 COc1ccc(C(CCCN)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596964 195266 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566433 195266 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 612 12 1 9 4.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cccs2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44568226 183009 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2008.06.019
CHEMBL480170 183009 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 9 1 4 3.8 CN(C)CCCOc1ccc(CN2CC[C@@H](NC(=O)c3ccc(Br)cc3)C2)cc1 10.1016/j.bmcl.2008.06.019
44568368 183460 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 555 8 1 5 4.5 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCOCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482257 183460 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 555 8 1 5 4.5 O=C(N[C@H]1CCN(Cc2ccc(OCCN3CCOCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44568426 191059 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 491 8 2 5 4.2 COc1cc(CCN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)ccc1OC1CCNCC1 10.1016/j.bmcl.2008.06.019
CHEMBL519629 191059 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 491 8 2 5 4.2 COc1cc(CCN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)ccc1OC1CCNCC1 10.1016/j.bmcl.2008.06.019
44568484 183415 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 575 6 2 5 4.1 O=C(N[C@@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL481964 183415 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 575 6 2 5 4.1 O=C(N[C@@H]1CCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44399062 69033 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 552 14 2 7 3.2 CC(C)C[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL193133 69033 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 552 14 2 7 3.2 CC(C)C[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399093 126866 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 500 13 2 6 3.6 CC(C)C[C@H](NC(=O)c1cccs1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL365966 126866 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 500 13 2 6 3.6 CC(C)C[C@H](NC(=O)c1cccs1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399084 133079 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 596 13 2 5 5.1 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)c3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2005.04.074
CHEMBL371361 133079 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 596 13 2 5 5.1 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)c3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2005.04.074
44580472 187379 0 None -100 2 Cat 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 5 2 2 4.3 CCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497172 187379 0 None -100 2 Cat 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 5 2 2 4.3 CCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448736 94397 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 405 6 0 3 4.3 Cc1cccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)c1 10.1016/j.bmcl.2008.03.078
CHEMBL253749 94397 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 405 6 0 3 4.3 Cc1cccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)c1 10.1016/j.bmcl.2008.03.078
44448692 94444 3 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 383 5 0 3 3.9 CN(CC(=O)N1CCCCC1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL254154 94444 3 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 383 5 0 3 3.9 CN(CC(=O)N1CCCCC1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL439551 212089 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
44448732 94368 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 473 7 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL253540 94368 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 473 7 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44580632 187213 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 329 6 1 3 5.5 CCCCNc1nccc2c1c1ccccc1n2Cc1ccccc1 10.1016/j.bmcl.2008.08.054
CHEMBL495919 187213 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 329 6 1 3 5.5 CCCCNc1nccc2c1c1ccccc1n2Cc1ccccc1 10.1016/j.bmcl.2008.08.054
24863522 188310 9 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 607 8 1 7 4.3 CNC(=O)c1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)Cn3c(=O)cnc4cc(Cl)c(Cl)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
CHEMBL507691 188310 9 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 607 8 1 7 4.3 CNC(=O)c1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)Cn3c(=O)cnc4cc(Cl)c(Cl)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
10173280 2934 45 None 3 2 Rhesus macaque 8.4 pKi = 8.4 Binding
Binding affinity to monkey urotensin 2 receptorBinding affinity to monkey urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
3516 2934 45 None 3 2 Rhesus macaque 8.4 pKi = 8.4 Binding
Binding affinity to monkey urotensin 2 receptorBinding affinity to monkey urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
CHEMBL567303 2934 45 None 3 2 Rhesus macaque 8.4 pKi = 8.4 Binding
Binding affinity to monkey urotensin 2 receptorBinding affinity to monkey urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
25126427 2101 6 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
9437 2101 6 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
CHEMBL567713 2101 6 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 10.1021/jm900683d
25125422 195601 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL568637 195601 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 612 12 1 8 4.8 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C(C)C)CC3)C2=O)cc1OC 10.1021/jm900683d
24893978 993 5 None 9 8 Human 8.4 pKi = 8.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
8872 993 5 None 9 8 Human 8.4 pKi = 8.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
CHEMBL495075 993 5 None 9 8 Human 8.4 pKi = 8.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
CHEMBL1165796 206781 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
CHEMBL218994 207648 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44448913 154997 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 469 5 0 6 3.4 O=C(Cn1c(=O)oc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
CHEMBL404289 154997 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 469 5 0 6 3.4 O=C(Cn1c(=O)oc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
11691 1940 4 None -91201 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 390 6 0 2 4.8 Clc1cc(ccc1Cl)CC(=O)N([C@H](CN1CCCC1)c1ccccc1)C 10.1016/j.bmcl.2008.05.058
3082718 1940 4 None -91201 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 390 6 0 2 4.8 Clc1cc(ccc1Cl)CC(=O)N([C@H](CN1CCCC1)c1ccccc1)C 10.1016/j.bmcl.2008.05.058
CHEMBL38576 1940 4 None -91201 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 390 6 0 2 4.8 Clc1cc(ccc1Cl)CC(=O)N([C@H](CN1CCCC1)c1ccccc1)C 10.1016/j.bmcl.2008.05.058
CHEMBL218698 207643 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
10173280 2934 45 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
3516 2934 45 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
CHEMBL567303 2934 45 None -3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm900683d
10119115 190155 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 1 4 4.8 CN1CCC(Oc2ccc(CN3CCC(NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2Br)C1 10.1016/j.bmcl.2008.06.019
CHEMBL518301 190155 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 525 6 1 4 4.8 CN1CCC(Oc2ccc(CN3CCC(NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2Br)C1 10.1016/j.bmcl.2008.06.019
44568428 183008 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 7 2 4 4.2 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)cc2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL480165 183008 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 461 7 2 4 4.2 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)cc2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
24804816 145848 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 576 7 1 6 4.7 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2ccccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL392166 145848 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 576 7 1 6 4.7 CC(C)(C)OC(=O)N1CCC(CNC(=O)c2ccccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
45486909 195459 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 614 9 1 8 5.4 COc1ccc(C(CNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567866 195459 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 614 9 1 8 5.4 COc1ccc(C(CNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25127072 196051 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL571537 196051 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 638 12 0 8 5.2 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CCC4)CC3)C2=O)cc1OC 10.1021/jm900683d
44568370 189236 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 511 6 2 4 4.5 O=C(N[C@H]1CCN(Cc2ccc(O[C@H]3CCNC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL516606 189236 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 511 6 2 4 4.5 O=C(N[C@H]1CCN(Cc2ccc(O[C@H]3CCNC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
16656749 195436 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567736 195436 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 626 12 1 9 4.4 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C(C)C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44534490 193293 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 481 6 1 4 4.7 CN1CCC(Oc2ccc(CN3CC[C@H](NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2Cl)C1 10.1016/j.bmcl.2008.06.019
CHEMBL546011 193293 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 481 6 1 4 4.7 CN1CCC(Oc2ccc(CN3CC[C@H](NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2Cl)C1 10.1016/j.bmcl.2008.06.019
155520913 169958 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4449844 169958 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44597070 195088 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL565416 195088 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 584 11 1 8 4.0 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCNCC3)C2=O)cc1OC 10.1021/jm900683d
23627722 195518 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568165 195518 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
10173280 2934 45 None -3 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
3516 2934 45 None -3 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
CHEMBL567303 2934 45 None -3 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 418 6 3 4 3.7 O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1 10.1021/jm901294u
44561276 173011 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 583 8 0 6 4.9 COc1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)CN3C(=O)COc4cc(Cl)c(Cl)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
CHEMBL453329 173011 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 583 8 0 6 4.9 COc1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)CN3C(=O)COc4cc(Cl)c(Cl)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
44448976 94902 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 474 5 0 6 3.1 Cc1cc2ncc(=O)n(CC(=O)N3CCCC(c4ccccc4)C3CN3CCOCC3)c2cc1C 10.1016/j.bmcl.2008.05.027
CHEMBL256721 94902 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 474 5 0 6 3.1 Cc1cc2ncc(=O)n(CC(=O)N3CCCC(c4ccccc4)C3CN3CCOCC3)c2cc1C 10.1016/j.bmcl.2008.05.027
44448947 95002 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 453 5 0 5 4.1 O=C(Cn1c(=O)oc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL257150 95002 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 453 5 0 5 4.1 O=C(Cn1c(=O)oc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCCC1 10.1016/j.bmcl.2008.05.027
CHEMBL223905 207691 10 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cellsDisplacement of [125I]urotensin 2 from human UT receptor expressed in CHO-K1 cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm058043j
CHEMBL223905 207691 10 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL223905 207691 10 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm500218x
21023902 3466 25 None 2 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to urotensin-2 receptorBinding affinity to urotensin-2 receptor
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm9001346
2165 3466 25 None 2 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to urotensin-2 receptorBinding affinity to urotensin-2 receptor
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm9001346
CHEMBL522770 3466 25 None 2 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to urotensin-2 receptorBinding affinity to urotensin-2 receptor
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm9001346
44568369 183462 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 511 6 2 4 4.5 O=C(N[C@H]1CCN(Cc2ccc(O[C@@H]3CCNC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482259 183462 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 511 6 2 4 4.5 O=C(N[C@H]1CCN(Cc2ccc(O[C@@H]3CCNC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44448339 94827 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 499 8 0 3 6.1 O=C(CN(CC1CC1)c1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL256365 94827 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 499 8 0 3 6.1 O=C(CN(CC1CC1)c1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580631 187212 0 None 12 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 1 3 3.9 CCCCNc1nccc2c1c1ccccc1n2C 10.1016/j.bmcl.2008.08.054
CHEMBL495918 187212 0 None 12 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 1 3 3.9 CCCCNc1nccc2c1c1ccccc1n2C 10.1016/j.bmcl.2008.08.054
44580682 187436 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 4 2 2 4.6 CCCCNc1ccnc2[nH]c3ccc(Cl)cc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497579 187436 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 273 4 2 2 4.6 CCCCNc1ccnc2[nH]c3ccc(Cl)cc3c12 10.1016/j.bmcl.2008.08.054
18613636 183301 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 463 9 1 4 4.7 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2008.06.019
CHEMBL481129 183301 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 463 9 1 4 4.7 CN(C)CCCOc1ccc(CN2CCC(NC(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2008.06.019
12052410 67593 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 533 13 3 5 4.0 CC(C)C[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL191110 67593 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 533 13 3 5 4.0 CC(C)C[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
12052411 68819 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 538 13 2 7 3.3 CC(C)C[C@H](NC(=O)c1ccc2c(c1)OCO2)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL192552 68819 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 538 13 2 7 3.3 CC(C)C[C@H](NC(=O)c1ccc2c(c1)OCO2)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
12052408 125847 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 494 13 2 5 3.6 CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL365053 125847 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 494 13 2 5 3.6 CC(C)C[C@H](NC(=O)c1ccccc1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448656 94573 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 376 4 0 3 4.6 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL254994 94573 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 376 4 0 3 4.6 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448293 94915 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.03.078
CHEMBL256774 94915 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.03.078
155560178 174349 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N(C)[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4565187 174349 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1030 16 11 13 1.2 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N(C)[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
24804326 144805 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 644 9 1 6 5.7 O=C(NCC1CCN(C(=O)OCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL391354 144805 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 644 9 1 6 5.7 O=C(NCC1CCN(C(=O)OCc2ccccc2)CC1)c1cc(Cl)ccc1C1CCN(CCN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2007.09.092
45486911 195495 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 628 10 1 8 5.8 COc1ccc(C(CCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568089 195495 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 628 10 1 8 5.8 COc1ccc(C(CCNC(=O)OC(C)(C)C)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
23627612 196125 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL572138 196125 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 485 7 0 6 4.4 COc1ccc(CN2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
44596870 195478 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL567949 195478 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 598 11 1 9 3.6 COc1ccc([C@@H](CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN(C)CC4)c3C2=O)cc1OC 10.1021/jm900683d
25127070 196873 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
CHEMBL578204 196873 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 624 12 0 8 4.8 COc1ccc([C@@H](CCCN(C)S(=O)(=O)c2cccs2)N2Cc3c(cccc3N3CCN(C4CC4)CC3)C2=O)cc1OC 10.1021/jm900683d
25067046 154621 3 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL402303 154621 3 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
44561237 187652 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 567 8 1 7 3.6 CNC(=O)c1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)Cn3c(=O)cnc4cc(C)c(C)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
CHEMBL499582 187652 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 567 8 1 7 3.6 CNC(=O)c1cccc(-c2ccc(C(CN3CCOCC3)N(C)C(=O)Cn3c(=O)cnc4cc(C)c(C)cc43)cc2)c1 10.1016/j.bmcl.2008.05.058
44448874 94646 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 485 5 0 6 3.8 O=C(Cn1c(=O)sc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
CHEMBL255460 94646 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 485 5 0 6 3.8 O=C(Cn1c(=O)sc2ccc(Cl)cc21)N1CCCC(c2ccccc2)C1CN1CCOCC1 10.1016/j.bmcl.2008.05.027
44449202 95251 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 500 7 0 5 4.4 N#CCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL258251 95251 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 500 7 0 5 4.4 N#CCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL3104471 209307 5 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
25067046 154621 3 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL402303 154621 3 None -1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44580473 187345 0 None 31 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 6 2 2 4.7 CCCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL496920 187345 0 None 31 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 6 2 2 4.7 CCCCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580515 187425 0 None 89 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497561 187425 0 None 89 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 237 3 2 2 3.5 c1ccc2c(c1)[nH]c1ccnc(NCC3CC3)c12 10.1016/j.bmcl.2008.08.054
25067046 154621 3 None 1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from rat urotensin 2 receptorDisplacement of [125I]human urotensin 2 from rat urotensin 2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL402303 154621 3 None 1 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]human urotensin 2 from rat urotensin 2 receptorDisplacement of [125I]human urotensin 2 from rat urotensin 2 receptor
ChEMBL 459 6 0 3 5.3 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL452403 212219 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL3315143 209611 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting methodDisplacement of [125I]urotensin-2 from human recombinant UT receptor expressed in CHO-K1 cells by scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N1)C(=O)O 10.1021/jm500218x
44534504 183256 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 527 9 1 4 5.1 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)cc1Br 10.1016/j.bmcl.2008.06.019
CHEMBL480775 183256 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 527 9 1 4 5.1 CN(C)CCCOc1ccc(CN2CC[C@H](NC(=O)c3ccc(Cl)c(Cl)c3)C2)cc1Br 10.1016/j.bmcl.2008.06.019
CHEMBL1163477 206772 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cellsDisplacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm901294u
45487747 195199 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL566056 195199 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 564 11 1 8 4.9 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(Cl)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44568400 183411 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 479 7 2 4 4.3 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(F)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL481946 183411 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 479 7 2 4 4.3 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c(F)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
44448359 95048 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 445 6 1 3 5.3 O=C(CNc1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257349 95048 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 445 6 1 3 5.3 O=C(CNc1ccc(Cl)c(Cl)c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580681 187435 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCCCNc1ccnc2[nH]c3ccc(C)cc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497578 187435 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.2 CCCCNc1ccnc2[nH]c3ccc(C)cc3c12 10.1016/j.bmcl.2008.08.054
25211348 188161 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 281 5 1 3 5.0 CCCCNc1nccc2c1c1ccccc1n2C(C)C 10.1016/j.bmcl.2008.08.054
CHEMBL505353 188161 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 281 5 1 3 5.0 CCCCNc1nccc2c1c1ccccc1n2C(C)C 10.1016/j.bmcl.2008.08.054
44561195 172635 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 511 8 0 4 5.6 CN(CC(=O)N(C)C(CN1CCOCC1)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
CHEMBL452298 172635 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 511 8 0 4 5.6 CN(CC(=O)N(C)C(CN1CCOCC1)c1ccc(-c2ccccc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.058
44561236 172811 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)[C@H](CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
CHEMBL452808 172811 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human urotensin-2 receptorBinding affinity to human urotensin-2 receptor
ChEMBL 553 7 0 5 4.9 CN(C(=O)CN1C(=O)COc2cc(Cl)c(Cl)cc21)[C@H](CN1CCOCC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2008.05.058
12052412 69023 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 545 13 2 6 4.1 CC(C)C[C@H](NC(=O)c1ccc2ccccc2n1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL193033 69023 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 545 13 2 6 4.1 CC(C)C[C@H](NC(=O)c1ccc2ccccc2n1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44399398 69042 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 429 9 1 4 4.0 Cc1cc(C(=O)N[C@H]2CCN(Cc3ccc(OCCCN(C)C)cc3)C2)ccc1Cl 10.1016/j.bmcl.2005.04.074
CHEMBL193266 69042 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 429 9 1 4 4.0 Cc1cc(C(=O)N[C@H]2CCN(Cc3ccc(OCCCN(C)C)cc3)C2)ccc1Cl 10.1016/j.bmcl.2005.04.074
44399094 121828 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 473 9 1 4 4.1 Cc1cc(C(=O)N[C@H]2CCN(Cc3ccc(OCCCN(C)C)cc3)C2)ccc1Br 10.1016/j.bmcl.2005.04.074
CHEMBL359993 121828 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 473 9 1 4 4.1 Cc1cc(C(=O)N[C@H]2CCN(Cc3ccc(OCCCN(C)C)cc3)C2)ccc1Br 10.1016/j.bmcl.2005.04.074
12052415 134745 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 484 13 2 6 3.1 CC(C)C[C@H](NC(=O)c1ccco1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL372658 134745 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 484 13 2 6 3.1 CC(C)C[C@H](NC(=O)c1ccco1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44580631 187212 0 None -12 2 Cat 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 1 3 3.9 CCCCNc1nccc2c1c1ccccc1n2C 10.1016/j.bmcl.2008.08.054
CHEMBL495918 187212 0 None -12 2 Cat 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 1 3 3.9 CCCCNc1nccc2c1c1ccccc1n2C 10.1016/j.bmcl.2008.08.054
25067560 187378 0 None -31 2 Cat 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL497171 187378 0 None -31 2 Cat 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from cat urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448428 94688 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 479 5 1 2 5.3 O=C(Cc1c[nH]c2ccc(Br)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL255664 94688 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 479 5 1 2 5.3 O=C(Cc1c[nH]c2ccc(Br)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44206680 195316 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
CHEMBL566894 195316 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human urotensin 2 receptorBinding affinity to human urotensin 2 receptor
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm901294u
44206680 195316 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm900683d
CHEMBL566894 195316 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 435 5 0 5 4.3 CCN1CCN(c2cccc3c2[C@H]2CCC[C@H](c4ccc(OC)c(OC)c4)N2C3=O)CC1 10.1021/jm900683d
23728637 151178 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 625 8 1 7 4.2 CC(C)(C)OC(=O)N1CCN(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL396443 151178 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 625 8 1 7 4.2 CC(C)(C)OC(=O)N1CCN(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
44568427 183433 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 506 8 2 6 4.1 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c([N+](=O)[O-])c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL482114 183433 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 506 8 2 6 4.1 O=C(N[C@H]1CCN(CCc2ccc(OC3CCNCC3)c([N+](=O)[O-])c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL593662 214026 9 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44448472 154919 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 496 5 0 3 6.1 O=C(Cc1csc2ccc(Br)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL403947 154919 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 496 5 0 3 6.1 O=C(Cc1csc2ccc(Br)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
25067045 154958 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL404177 154958 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 452 5 0 3 6.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
45486908 195207 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 514 8 1 7 3.9 COc1ccc(C(CN)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL566144 195207 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 514 8 1 7 3.9 COc1ccc(C(CN)N2C(=O)c3cccc(N4CCN([C@@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
10232516 191939 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 603 6 2 5 4.9 O=C(NC1CCCCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL521117 191939 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 603 6 2 5 4.9 O=C(NC1CCCCN(S(=O)(=O)c2ccc(OC3CCNCC3)c(Br)c2)C1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.06.019
CHEMBL428990 211731 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(C(=O)O)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
23627249 195548 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL568316 195548 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 688 13 1 9 5.7 COc1ccc(C(CCCNS(=O)(=O)c2cccs2)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
24804161 91303 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 624 8 1 6 5.7 CC(C)(C)OC(=O)N1CCC(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
CHEMBL240916 91303 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrsDisplacement of [125I]U2 from human UT receptor in RMS13 cells after 2.5 hrs
ChEMBL 624 8 1 6 5.7 CC(C)(C)OC(=O)N1CCC(CCNC(=O)c2cc(Cl)ccc2C2CCN(CCN3C(=O)COc4ccccc43)CC2)CC1 10.1016/j.bmcl.2007.09.092
44448772 154706 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 475 6 0 4 4.5 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL402805 154706 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 475 6 0 4 4.5 CN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCOCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
44448315 94815 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256299 94815 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.03.078
44448316 94816 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 523 7 0 4 4.6 CS(=O)(=O)N(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
CHEMBL256300 94816 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 523 7 0 4 4.6 CS(=O)(=O)N(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.03.078
44448429 154622 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 412 5 0 2 5.3 O=C(Cc1cccc2ccccc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL402304 154622 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 412 5 0 2 5.3 O=C(Cc1cccc2ccccc12)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44580633 187037 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1ccnc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL494934 187037 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 239 4 2 2 3.9 CCCCNc1ccnc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580565 192790 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 3 2 3 3.3 c1ccc2c(c1)[nH]c1ccnc(NCC3CCCO3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL525759 192790 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 267 3 2 3 3.3 c1ccc2c(c1)[nH]c1ccnc(NCC3CCCO3)c12 10.1016/j.bmcl.2008.08.054
12052413 67158 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 548 12 2 5 4.5 CC(C)[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
CHEMBL189525 67158 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor
ChEMBL 548 12 2 5 4.5 CC(C)[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)N[C@H]1CCN(Cc2ccc(OCCCN(C)C)cc2)C1 10.1016/j.bmcl.2005.04.074
44448733 94396 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 421 7 0 4 4.0 COc1cccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)c1 10.1016/j.bmcl.2008.03.078
CHEMBL253747 94396 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 421 7 0 4 4.0 COc1cccc(N(C)CC(=O)N2CCC[C@H](c3ccccc3)[C@@H]2CN2CCCC2)c1 10.1016/j.bmcl.2008.03.078
44448586 95087 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 378 4 0 4 3.4 O=C(Cc1csc2ccc(Cl)cc12)N1CCOCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257552 95087 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 378 4 0 4 3.4 O=C(Cc1csc2ccc(Cl)cc12)N1CCOCC1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44448289 154979 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccccc1Cl 10.1016/j.bmcl.2008.03.078
CHEMBL404244 154979 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 425 6 0 3 4.6 CN(CC(=O)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1)c1ccccc1Cl 10.1016/j.bmcl.2008.03.078
44580680 187409 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 2 4.7 c1ccc2c(c1)[nH]c1nccc(NCC3CCCCC3)c12 10.1016/j.bmcl.2008.08.054
CHEMBL497369 187409 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 279 3 2 2 4.7 c1ccc2c(c1)[nH]c1nccc(NCC3CCCCC3)c12 10.1016/j.bmcl.2008.08.054
44580630 192133 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 295 7 1 2 5.1 CCCCN(CCCC)c1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL522074 192133 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 295 7 1 2 5.1 CCCCN(CCCC)c1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44580474 192448 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.3 CCCC(C)Nc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
CHEMBL522381 192448 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 253 4 2 2 4.3 CCCC(C)Nc1nccc2[nH]c3ccccc3c12 10.1016/j.bmcl.2008.08.054
44448657 94574 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 5.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL254995 94574 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 390 4 0 3 5.0 O=C(Cc1csc2ccc(Cl)cc12)N1CCCCC1CN1CCCCC1 10.1016/j.bmcl.2008.03.078
44448396 95012 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 412 5 0 2 5.3 O=C(Cc1ccc2ccccc2c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
CHEMBL257187 95012 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]human urotensin 2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 412 5 0 2 5.3 O=C(Cc1ccc2ccccc2c1)N1CCC[C@H](c2ccccc2)[C@@H]1CN1CCCC1 10.1016/j.bmcl.2008.03.078
44449171 94950 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 503 9 0 4 5.3 COCCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
CHEMBL256937 94950 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cellsDisplacement of [125I]hU-2 from human recombinant Urotensin 2 receptor expressed in HEK293 cells
ChEMBL 503 9 0 4 5.3 COCCN(CC(=O)N1CCCC(c2ccccc2)C1CN1CCCC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2008.05.027
21023902 3466 25 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
2165 3466 25 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
CHEMBL522770 3466 25 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 10.1021/jm900683d
45487748 196063 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL571625 196063 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 560 12 1 9 4.2 CCN1CCN(c2cccc3c2CN([C@H](CCCNc2cncc(OC)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
155532198 171164 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
CHEMBL4467241 171164 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assayDisplacement of [125I]-URP or human [125I[-urotensin-2 from human urotensin 2 receptor expressed in HEK293 or CHOK1 cells after 2 hrs by gamma-counting assay
ChEMBL 1402 27 16 19 -1.1 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.8b01601
44596967 195084 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL565388 195084 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 664 12 2 8 5.5 COc1ccc([C@@H](CCCNC(=O)c2c(C)n[nH]c2C)N2C(=O)c3cccc(N4CCN([C@H](C)c5ccccc5)CC4)c3C2=O)cc1OC 10.1021/jm900683d
CHEMBL383996 210558 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cellsDisplacement of [125I]human urotensin-2 from human GPR14 transfected in CHO cells
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(C(C)(C)C)cc2)C(=O)N1)C(=O)O 10.1021/jm0602110
CHEMBL501794 212364 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL509009 213458 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H]2Cc3ccccc3CN2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
CHEMBL504723 212401 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [125I]urotensin-2 from human UT2 receptor expressed in CHO-K1 cells by liquid scintillation counting
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)O 10.1021/jm900148c
44597069 195798 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
CHEMBL569923 195798 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assayDisplacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay
ChEMBL 624 12 1 10 3.0 CCN1CCN(c2cccc3c2C(=O)N([C@H](CCCNS(=O)(=O)c2cn(C)c(C)n2)c2ccc(OC)c(OC)c2)C3=O)CC1 10.1021/jm900683d
44568309 190602 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 447 6 1 4 4.1 CN1CCC(Oc2ccc(CN3CCC(NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2)C1 10.1016/j.bmcl.2008.06.019
CHEMBL518949 190602 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cellsDisplacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells
ChEMBL 447 6 1 4 4.1 CN1CCC(Oc2ccc(CN3CCC(NC(=O)c4ccc(Cl)c(Cl)c4)C3)cc2)C1 10.1016/j.bmcl.2008.06.019
11439 3231 0 None - 0 Human 9.0 pIC50 = 9 Binding
Determined in a hUT binding assayDetermined in a hUT binding assay
Guide to Pharmacology 603 8 0 8 1.0 O=C(N1CCN(C[C@@H]1CN1CCCC1)S(=O)(=O)CCN1CCOCC1)CN1C(=O)COc2c1cc(Cl)c(c2)Cl 32745605
155817517 3231 0 None - 0 Human 9.0 pIC50 = 9 Binding
Determined in a hUT binding assayDetermined in a hUT binding assay
Guide to Pharmacology 603 8 0 8 1.0 O=C(N1CCN(C[C@@H]1CN1CCCC1)S(=O)(=O)CCN1CCOCC1)CN1C(=O)COc2c1cc(Cl)c(c2)Cl 32745605
2161 115 0 None - 1 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12535707
11995575 3886 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
11995575 3886 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
2156 3886 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
2156 3886 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
CHEMBL437110 3886 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17628210
CHEMBL437110 3886 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18710417
2162 642 0 None - 1 Human 6.7 pKd None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12770925
2166 3771 0 None - 1 Human 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12535707
24893978 993 5 None 9 8 Human 8.4 pKi = 8.4 Binding
Ligand binding.Ligand binding.
Guide to Pharmacology 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 18573659
8872 993 5 None 9 8 Human 8.4 pKi = 8.4 Binding
Ligand binding.Ligand binding.
Guide to Pharmacology 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 18573659
CHEMBL495075 993 5 None 9 8 Human 8.4 pKi = 8.4 Binding
Ligand binding.Ligand binding.
Guide to Pharmacology 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 18573659
9439 892 0 None - 1 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17125276
2151 242 6 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 12408704
2151 242 6 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 15781415
9797568 242 6 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 12408704
9797568 242 6 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 15781415
CHEMBL192359 242 6 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 12408704
CHEMBL192359 242 6 None - 1 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 4 0 3 3.9 CN(CCC1(OC(=O)c2c(C1)cccc2)c1ccc(cc1)Cl)C 15781415
10278166 3459 32 None -2 2 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 16171813
3531 3459 32 None -2 2 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 16171813
CHEMBL1164033 3459 32 None -2 2 Human 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 490 7 1 4 5.4 CN(CCOc1cc(ccc1Cl)NS(=O)(=O)c1c(Cl)cc(cc1Cl)C(F)(F)F)C 16171813
2164 3457 13 None 1 3 Rat 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 15936190
9846574 3457 13 None 1 3 Rat 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 15936190
CHEMBL366221 3457 13 None 1 3 Rat 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 9 1 4 4.3 CN(CCCOc1ccc(cc1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl)C 15936190
134813899 2908 0 None - 1 Rat 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18082287
9438 2908 0 None - 1 Rat 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18082287
21023902 3466 25 None 2 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2165 3466 25 None 2 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
CHEMBL522770 3466 25 None 2 3 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2167 3873 0 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14645137
25126427 2101 6 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 19731961
9437 2101 6 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 19731961
CHEMBL567713 2101 6 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 598 12 1 8 4.4 CCN1CCN(CC1)c1cccc2c1CN(C2=O)[C@@H](c1ccc(c(c1)OC)OC)CCCNS(=O)(=O)c1cccs1 19731961
2153 3884 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10499587
2153 3884 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10548501
2153 3884 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10559967
2153 3884 0 None -1 3 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10581185
10213684 3860 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
2152 3860 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
CHEMBL414256 3860 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
2160 2981 0 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12238917
21023902 3466 25 None -2 3 Mouse 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
21023902 3466 25 None -2 3 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2165 3466 25 None -2 3 Mouse 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2165 3466 25 None -2 3 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
CHEMBL522770 3466 25 None -2 3 Mouse 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
CHEMBL522770 3466 25 None -2 3 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 7 1 6 4.4 COc1cc(c(cc1OC)Br)S(=O)(=O)Nc1ccc(c(c1)O[C@@H]1CCN(C1)C)C(F)(F)F 15852036
2154 3885 0 None -1 3 Mouse 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2154 3885 0 None -1 3 Mouse 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 3883 0 None -1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2154 3885 0 None -1 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2153 3884 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2153 3884 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 3883 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11976263
2155 3883 0 None -1 3 Mouse 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2153 3884 0 None 1 3 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2155 3883 0 None 1 3 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2154 3885 0 None 1 3 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15852036
2159 748 0 None - 1 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12495432