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
155550061 173302 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 862 21 12 7 2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4539775 173302 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 862 21 12 7 2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2152055 207543 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
155547823 173005 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 795 19 11 7 1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4533110 173005 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 795 19 11 7 1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
155529648 170853 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 759 19 11 7 0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4462883 170853 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 759 19 11 7 0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2152060 207548 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
155545453 172815 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4528114 172815 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2152056 207544 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N(C)C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
71454755 80326 0 None 9 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1332 38 19 16 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=S)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151643 80326 0 None 9 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1332 38 19 16 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=S)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
1281 2148 27 None 1 4 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
1283 2148 27 None 1 4 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
25240297 2148 27 None 1 4 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
CHEMBL376756 2148 27 None 1 4 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
71461938 80329 0 None -2 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151646 80329 0 None -2 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL3085809 209239 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
155522287 170062 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 761 19 11 7 0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4451244 170062 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 761 19 11 7 0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2151642 207534 0 None -3 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
1281 2148 27 None 1 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2012.08.087
1283 2148 27 None 1 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2012.08.087
25240297 2148 27 None 1 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2012.08.087
CHEMBL376756 2148 27 None 1 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2012.08.087
CHEMBL2152058 207546 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CCNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
155551159 173369 0 None 17 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4541289 173369 0 None 17 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
90324535 118355 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1384 39 19 19 -3.3 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCc1cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1 10.1021/jm5019675
CHEMBL3422408 118355 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1384 39 19 19 -3.3 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCc1cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1 10.1021/jm5019675
CHEMBL3422407 209909 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm5019675
71461940 80337 0 None 1 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151654 80337 0 None 1 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
25084920 149334 0 None 16 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3949159 149334 0 None 16 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3422414 209912 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm5019675
1281 2148 27 None 1 4 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2018.12.016
1283 2148 27 None 1 4 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2018.12.016
25240297 2148 27 None 1 4 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2018.12.016
CHEMBL376756 2148 27 None 1 4 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2018.12.016
71460220 80336 0 None 1 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1328 36 19 16 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151653 80336 0 None 1 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1328 36 19 16 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71460219 80333 0 None 1 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1284 36 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151650 80333 0 None 1 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1284 36 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL3422413 209911 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm5019675
71451197 80335 0 None -3 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151652 80335 0 None -3 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
155536247 171567 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 785 19 11 8 1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccoc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4473151 171567 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 785 19 11 8 1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccoc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
155565826 175226 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 801 19 11 7 1.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)C1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4584512 175226 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 801 19 11 7 1.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)C1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
71460218 80332 0 None 1 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1244 36 19 16 -4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151649 80332 0 None 1 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1244 36 19 16 -4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
155527587 170643 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 1025 28 15 11 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4459547 170643 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 1025 28 15 11 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
155559289 174289 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 747 19 11 7 0.6 CCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4563528 174289 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 747 19 11 7 0.6 CCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2152061 207549 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CNC(=N)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
CHEMBL2152062 207550 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
155548337 173159 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4536531 173159 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
155514052 169228 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 986 28 14 11 -1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4439387 169228 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 986 28 14 11 -1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
155534639 171407 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 784 19 12 7 0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4470916 171407 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 784 19 12 7 0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
1281 2148 27 None 1 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL None None None None 10.1021/jm800930w
1283 2148 27 None 1 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL None None None None 10.1021/jm800930w
25240297 2148 27 None 1 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL None None None None 10.1021/jm800930w
CHEMBL376756 2148 27 None 1 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL None None None None 10.1021/jm800930w
71449398 80331 0 None 1 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1232 35 20 17 -6.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151648 80331 0 None 1 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1232 35 20 17 -6.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461939 80334 0 None 2 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151651 80334 0 None 2 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
155549139 173228 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 785 19 12 8 0.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4538305 173228 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 785 19 12 8 0.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
155533419 171243 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 809 20 11 7 1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4468499 171243 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 809 20 11 7 1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL3086284 209246 2 None -1 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2152052 207540 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
CHEMBL2152054 207542 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
25138123 178658 0 None 3388 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 781 21 9 6 2.9 CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL472833 178658 0 None 3388 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 781 21 9 6 2.9 CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
118707492 112614 0 None 3 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1241 32 18 13 -0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314223 112614 0 None 3 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1241 32 18 13 -0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707486 112608 0 None 7 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1254 32 18 13 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314217 112608 0 None 7 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1254 32 18 13 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL2152057 207545 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None C/N=C(/NC)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
155554573 174015 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 694 18 10 7 -0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4557192 174015 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 694 18 10 7 -0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
49787129 112615 3 None 3 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3314224 112615 3 None 3 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
49787129 112615 3 None 3 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314224 112615 3 None 3 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL2152064 207552 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN(C)C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
CHEMBL2152063 207551 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CNC(=N)NCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
25138131 173288 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL453956 173288 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL2152059 207547 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CCCNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
24996490 149342 0 None 16 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1258 35 19 15 -2.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3949224 149342 0 None 16 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1258 35 19 15 -2.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707495 112618 0 None 3 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1360 34 19 14 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314227 112618 0 None 3 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1360 34 19 14 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3315315 209623 0 None 2 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
16735569 141790 0 None 263 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL388586 141790 0 None 263 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
25075973 152676 0 None 42 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1259 34 19 15 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3977314 152676 0 None 42 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1259 34 19 15 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134132372 144554 0 None 19 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3911692 144554 0 None 19 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134150351 151174 0 None 14 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1271 30 17 14 -1.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3964403 151174 0 None 14 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1271 30 17 14 -1.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707489 112611 0 None 13 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1199 30 18 13 -0.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314220 112611 0 None 13 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1199 30 18 13 -0.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707484 112606 0 None 4 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314215 112606 0 None 4 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
25075960 145811 0 None 5 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1332 33 19 14 -0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3921327 145811 0 None 5 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1332 33 19 14 -0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
71449399 80338 0 None -1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151655 80338 0 None -1 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
118707481 112603 0 None 12 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1303 33 18 14 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314212 112603 0 None 12 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1303 33 18 14 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
155538456 171813 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 756 19 10 7 1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4476438 171813 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 756 19 10 7 1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
118735592 118356 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1384 39 19 19 -3.3 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)c1cn(CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1 10.1021/jm5019675
CHEMBL3422409 118356 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1384 39 19 19 -3.3 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)c1cn(CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1 10.1021/jm5019675
134157013 153565 0 None 7 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3985112 153565 0 None 7 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
71456524 80327 0 None 2 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1302 39 19 16 -3.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151644 80327 0 None 2 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1302 39 19 16 -3.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
155529496 170883 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 823 21 11 7 1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4463349 170883 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 823 21 11 7 1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
118707490 112612 0 None 20 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 30 18 13 0.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314221 112612 0 None 20 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 30 18 13 0.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707491 112613 0 None 4 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314222 112613 0 None 4 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
25075963 146697 0 None 2 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1F)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3928465 146697 0 None 2 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1F)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
16735569 141790 0 None 263 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL388586 141790 0 None 263 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
118707487 112609 0 None 13 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314218 112609 0 None 13 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
71456525 80330 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1218 35 20 17 -6.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151647 80330 0 None -1 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1218 35 20 17 -6.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
57653049 151570 0 None 11 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1243 30 18 15 -3.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3967782 151570 0 None 11 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1243 30 18 15 -3.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707496 112619 0 None 5 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314228 112619 0 None 5 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
16735730 96764 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 781 21 10 8 0.5 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL268579 96764 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 781 21 10 8 0.5 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
118707493 112616 0 None 4 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1326 35 19 14 -0.2 CCCC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)O 10.1021/jm5005489
CHEMBL3314225 112616 0 None 4 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1326 35 19 14 -0.2 CCCC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)O 10.1021/jm5005489
118707494 112617 0 None 5 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314226 112617 0 None 5 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707476 112598 0 None 6 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314207 112598 0 None 6 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
155518633 169742 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 781 20 11 7 1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4446920 169742 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 781 20 11 7 1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL3422412 209910 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm5019675
118707497 112620 0 None 4 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL3314229 112620 0 None 4 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
71461937 80328 0 None 4 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1316 38 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(=O)N[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151645 80328 0 None 4 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL 1316 38 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(=O)N[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
1281 2148 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
1283 2148 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
25240297 2148 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
CHEMBL376756 2148 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
1281 2148 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
1283 2148 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
25240297 2148 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
CHEMBL376756 2148 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
16737378 85033 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 780 21 10 7 1.1 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL226757 85033 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 780 21 10 7 1.1 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
16735542 168579 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 851 23 11 8 0.8 CC(=O)NCc1ccc(C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1 10.1021/jm070064l
CHEMBL440431 168579 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 851 23 11 8 0.8 CC(=O)NCc1ccc(C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1 10.1021/jm070064l
16735568 141551 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 825 22 10 9 1.0 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL388146 141551 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 825 22 10 9 1.0 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
118707485 112607 0 None 4 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1256 32 19 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314216 112607 0 None 4 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1256 32 19 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
24996809 148072 0 None 6 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1187 31 18 14 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3939287 148072 0 None 6 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1187 31 18 14 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707492 112614 0 None -3 2 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1241 32 18 13 -0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314223 112614 0 None -3 2 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1241 32 18 13 -0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
16736193 84370 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 810 22 10 8 1.1 COc1ccc(C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1 10.1021/jm070064l
CHEMBL223390 84370 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 810 22 10 8 1.1 COc1ccc(C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1 10.1021/jm070064l
16735543 84999 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 796 21 11 8 0.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccc(O)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL226566 84999 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 796 21 11 8 0.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccc(O)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
24995518 145027 0 None 5 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3915251 145027 0 None 5 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24992020 151684 0 None 5 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1215 31 18 14 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3968824 151684 0 None 5 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1215 31 18 14 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707482 112604 0 None 10 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1214 30 16 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314213 112604 0 None 10 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1214 30 16 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
25084920 149334 0 None -16 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3949159 149334 0 None -16 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
16735779 141789 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 814 21 10 7 1.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL388585 141789 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 814 21 10 7 1.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
118707488 112610 0 None 24 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1191 31 18 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314219 112610 0 None 24 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1191 31 18 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
49787129 112615 3 None -3 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3314224 112615 3 None -3 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
49787129 112615 3 None -3 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314224 112615 3 None -3 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3315315 209623 0 None -2 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
10328205 85376 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 851 23 13 8 0.1 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CNC(=N)N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL229621 85376 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 851 23 13 8 0.1 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CNC(=N)N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
155535993 171534 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 750 22 10 7 1.3 CCCCCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4472672 171534 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 750 22 10 7 1.3 CCCCCC(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
25075965 146921 0 None 3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3930297 146921 0 None 3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL2152048 207536 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
CHEMBL2152066 207554 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
155541282 172434 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 987 28 14 12 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)CCc1ccncc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4518378 172434 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 987 28 14 12 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)CCc1ccncc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
118707480 112602 0 None 14 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 31 17 14 -0.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314211 112602 0 None 14 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 31 17 14 -0.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL2152049 207537 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
16735508 85012 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 795 21 11 8 0.7 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL226633 85012 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 795 21 11 8 0.7 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
24996486 150216 0 None 4 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3956437 150216 0 None 4 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707477 112599 0 None 3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1218 32 18 15 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314208 112599 0 None 3 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1218 32 18 15 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118735685 118369 0 None 141 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1765 61 21 21 3.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCc1cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1)C(=O)O 10.1021/jm5019675
CHEMBL3422516 118369 0 None 141 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1765 61 21 21 3.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCc1cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1)C(=O)O 10.1021/jm5019675
16736170 85060 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 837 22 13 8 0.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL227165 85060 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 837 22 13 8 0.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
16735729 96773 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 781 21 10 8 0.5 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccncc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL268659 96773 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 781 21 10 8 0.5 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccncc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
16738337 96774 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 770 21 11 8 -0.2 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL268660 96774 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 770 21 11 8 -0.2 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
118707495 112618 0 None -3 2 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1360 34 19 14 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314227 112618 0 None -3 2 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1360 34 19 14 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
24994272 152661 0 None 3 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3977235 152661 0 None 3 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707478 112600 0 None 6 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1216 32 17 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314209 112600 0 None 6 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1216 32 17 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
25075963 146697 0 None -2 2 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1F)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3928465 146697 0 None -2 2 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1F)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134154824 150388 0 None 2 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3957784 150388 0 None 2 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24993970 151480 0 None 8 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3967058 151480 0 None 8 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL2152067 207555 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CNC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
CHEMBL3086284 209246 2 None 1 2 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL221141 207668 0 None - 1 Human 5.0 pEC50 = 5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/jm0609824
CHEMBL262316 208782 0 None - 1 Human 5.0 pEC50 = 5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL373854 210435 0 None - 1 Human 5.0 pEC50 = 5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374748 210449 0 None - 1 Human 5.0 pEC50 = 5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(N)=O 10.1021/jm0609824
CHEMBL410741 211078 0 None - 1 Human 5.0 pEC50 = 5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL426552 211588 0 None - 1 Human 5.0 pEC50 = 5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/jm0609824
CHEMBL375006 210453 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374260 210440 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cccnc1)C(N)=O 10.1021/jm0609824
101134421 2149 10 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
1284 2149 10 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2149 10 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2149 10 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL386958 210645 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
25084922 150476 0 None -3 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3958495 150476 0 None -3 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24993005 153583 0 None -3 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 32 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CCNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3985323 153583 0 None -3 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 32 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CCNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL221602 207669 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL435315 211905 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cccnc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL439094 212063 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
134150893 151370 0 None -19 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3966187 151370 0 None -19 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707479 112601 0 None -25 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1250 32 17 14 -0.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314210 112601 0 None -25 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1250 32 17 14 -0.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
134151953 152525 0 None -6 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1225 33 18 14 -1.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3976038 152525 0 None -6 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1225 33 18 14 -1.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707478 112600 0 None -6 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1216 32 17 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314209 112600 0 None -6 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1216 32 17 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
90324512 118357 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1408 39 18 21 -2.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)c1cn(Cc2cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)nn2)nn1 10.1021/jm5019675
CHEMBL3422410 118357 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1408 39 18 21 -2.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)c1cn(Cc2cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)nn2)nn1 10.1021/jm5019675
118707482 112604 0 None -10 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1214 30 16 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314213 112604 0 None -10 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1214 30 16 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707490 112612 0 None -20 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 30 18 13 0.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314221 112612 0 None -20 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 30 18 13 0.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3422510 209915 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm5019675
155547611 173123 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 652 17 10 7 -0.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4535825 173123 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 652 17 10 7 -0.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
24996155 147121 0 None -6 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C1CN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3931718 147121 0 None -6 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C1CN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134135834 143718 0 None -5 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3904889 143718 0 None -5 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24993970 151480 0 None -8 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3967058 151480 0 None -8 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24995205 142498 0 None -6 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3894943 142498 0 None -6 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24996810 151232 0 None -7 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 18 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3964945 151232 0 None -7 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 18 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
1281 2148 27 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
1283 2148 27 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
25240297 2148 27 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL376756 2148 27 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220855 207667 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1CCCCC1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
134143614 144897 0 None -4 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3914238 144897 0 None -4 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118735681 118366 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1612 56 20 17 2.8 CCCCCCCCCCCCCCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm5019675
CHEMBL3422512 118366 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1612 56 20 17 2.8 CCCCCCCCCCCCCCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm5019675
16735731 85014 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 769 21 11 7 0.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL226635 85014 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 769 21 11 7 0.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
134151953 152525 0 None 6 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1225 33 18 14 -1.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3976038 152525 0 None 6 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1225 33 18 14 -1.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
16736192 142756 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 796 21 11 8 0.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL389708 142756 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 796 21 11 8 0.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
155550676 173701 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 1082 29 16 12 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4549804 173701 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 1082 29 16 12 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2152151 207556 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CNC(=O)CNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
118707486 112608 0 None -7 2 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1254 32 18 13 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314217 112608 0 None -7 2 Rat 8.7 pEC50 = 8.7 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1254 32 18 13 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
24996155 147121 0 None 6 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C1CN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3931718 147121 0 None 6 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1195 30 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C1CN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
57653056 150163 0 None 10 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1227 30 17 15 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CSCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3956072 150163 0 None 10 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1227 30 17 15 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CSCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707484 112606 0 None -4 2 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314215 112606 0 None -4 2 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
24996810 151232 0 None 7 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 18 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3964945 151232 0 None 7 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 18 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
25138124 169727 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 783 22 9 6 3.2 CC(C)C[C@H](CCCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL444664 169727 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 783 22 9 6 3.2 CC(C)C[C@H](CCCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL3422406 209908 16 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm5019675
CHEMBL3086284 209246 2 None -1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
16735781 85378 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 900 25 11 9 1.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CNCc2ccccn2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL229656 85378 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 900 25 11 9 1.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CNCc2ccccn2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
134135834 143718 0 None 5 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3904889 143718 0 None 5 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24995205 142498 0 None 6 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3894943 142498 0 None 6 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
25084922 150476 0 None 3 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3958495 150476 0 None 3 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707483 112605 0 None 33 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 30 17 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(O)CN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314214 112605 0 None 33 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 30 17 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(O)CN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
25075960 145811 0 None -5 2 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1332 33 19 14 -0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3921327 145811 0 None -5 2 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1332 33 19 14 -0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707491 112613 0 None -4 2 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314222 112613 0 None -4 2 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118735683 118367 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1741 61 22 19 2.1 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)O 10.1021/jm5019675
CHEMBL3422514 118367 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1741 61 22 19 2.1 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)O 10.1021/jm5019675
24996487 150238 0 None -4 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CN(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3956626 150238 0 None -4 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CN(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
25075973 152676 0 None -42 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1259 34 19 15 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3977314 152676 0 None -42 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1259 34 19 15 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL221817 207673 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0609824
CHEMBL221764 207671 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374246 210439 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
118735686 118370 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1693 61 21 22 0.1 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCc1cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1)C(=O)O 10.1021/jm5019675
CHEMBL3422517 118370 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1693 61 21 22 0.1 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCc1cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1)C(=O)O 10.1021/jm5019675
134157281 153458 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3984058 153458 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707480 112602 0 None -14 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 31 17 14 -0.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314211 112602 0 None -14 2 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 31 17 14 -0.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL221761 207670 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
101134421 2149 10 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
1284 2149 10 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2149 10 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2149 10 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
57653056 150163 0 None -10 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1227 30 17 15 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CSCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3956072 150163 0 None -10 2 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1227 30 17 15 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CSCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118735684 118368 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1669 61 22 20 -0.7 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)O 10.1021/jm5019675
CHEMBL3422515 118368 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL 1669 61 22 20 -0.7 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)O 10.1021/jm5019675
CHEMBL434382 211897 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL220759 207666 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CCCC[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL375983 210478 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL375982 210477 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374077 210436 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL441935 212145 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
16735544 141515 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 916 23 11 10 2.0 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1OC(=O)c1ccccc1O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL387875 141515 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 916 23 11 10 2.0 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1OC(=O)c1ccccc1O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
16735511 142496 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 781 21 10 8 0.5 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccnc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL389493 142496 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 781 21 10 8 0.5 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccnc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
16736191 161314 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 810 22 11 8 0.6 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CO)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL415004 161314 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 810 22 11 8 0.6 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CO)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
16735509 85013 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 795 21 11 8 0.7 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL226634 85013 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 795 21 11 8 0.7 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
44425065 136421 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 809 22 11 8 0.6 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CN)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL374398 136421 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 809 22 11 8 0.6 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CN)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
9919540 85377 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 992 27 10 10 3.1 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CN(Cc2ccccn2)Cc2ccccn2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL229655 85377 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 992 27 10 10 3.1 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CN(Cc2ccccn2)Cc2ccccn2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
16736169 141486 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 899 25 11 8 2.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CNCc2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL387648 141486 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 899 25 11 8 2.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(CNCc2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
24993005 153583 0 None 3 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 32 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CCNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3985323 153583 0 None 3 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 32 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CCNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134143614 144897 0 None 4 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3914238 144897 0 None 4 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707493 112616 0 None -4 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1326 35 19 14 -0.2 CCCC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)O 10.1021/jm5005489
CHEMBL3314225 112616 0 None -4 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1326 35 19 14 -0.2 CCCC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)O 10.1021/jm5005489
CHEMBL2152065 207553 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
118707497 112620 0 None -4 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL3314229 112620 0 None -4 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL375450 210465 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
118707488 112610 0 None -24 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1191 31 18 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314219 112610 0 None -24 2 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1191 31 18 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
101134421 2149 10 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
1284 2149 10 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2149 10 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2149 10 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL262577 208787 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0609824
CHEMBL373714 210434 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(N)=O 10.1021/jm0609824
10222 3671 6 None -6 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
46700761 3671 6 None -6 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
CHEMBL3924151 3671 6 None -6 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
DB11975 3671 6 None -6 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
CHEMBL221816 207672 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(N)=O 10.1021/jm0609824
CHEMBL373676 210433 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL414073 211349 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm0609824
118707485 112607 0 None -4 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1256 32 19 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314216 112607 0 None -4 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1256 32 19 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707496 112619 0 None -5 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314228 112619 0 None -5 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
1281 2148 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
1283 2148 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
25240297 2148 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
CHEMBL376756 2148 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
1281 2148 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
1283 2148 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
25240297 2148 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
CHEMBL376756 2148 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
118707494 112617 0 None -5 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314226 112617 0 None -5 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
25138129 188038 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL503052 188038 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
24994895 149181 0 None 9 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3947975 149181 0 None 9 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707479 112601 0 None 25 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1250 32 17 14 -0.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314210 112601 0 None 25 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1250 32 17 14 -0.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
16736392 141519 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 795 21 11 8 0.7 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccc(N)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL387923 141519 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 795 21 11 8 0.7 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1cccc(N)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
134154824 150388 0 None -2 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3957784 150388 0 None -2 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
25075965 146921 0 None -3 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3930297 146921 0 None -3 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1316 33 19 14 -0.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134157013 153565 0 None -7 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3985112 153565 0 None -7 2 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24996487 150238 0 None 4 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CN(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3956626 150238 0 None 4 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 17 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CN(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134157281 153458 0 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3984058 153458 0 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1241 34 19 15 -2.8 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24994895 149181 0 None -9 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3947975 149181 0 None -9 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
134157735 153295 0 None -8 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3982675 153295 0 None -8 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24995519 142691 0 None -8 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1169 31 18 14 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3896533 142691 0 None -8 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1169 31 18 14 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL414073 211349 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm0609824
25075978 148008 0 None -8 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1231 31 18 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)c1ccccc1NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3938759 148008 0 None -8 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1231 31 18 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)c1ccccc1NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
16737730 96775 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 796 21 11 8 0.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
CHEMBL268661 96775 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 796 21 11 8 0.8 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccccc1O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm070064l
10222 3671 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
46700761 3671 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
CHEMBL3924151 3671 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
DB11975 3671 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
24995519 142691 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1169 31 18 14 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3896533 142691 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1169 31 18 14 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
25075978 148008 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1231 31 18 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)c1ccccc1NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3938759 148008 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1231 31 18 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)c1ccccc1NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
25138125 187756 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 781 21 9 6 3.1 CC(C)C/C(=C\CCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL501043 187756 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL 781 21 9 6 3.1 CC(C)C/C(=C\CCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
134157735 153295 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3982675 153295 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1223 30 17 14 -1.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN(C(=O)[C@@H](Cc2ccc(O)cc2)NC(C)=O)C1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707477 112599 0 None -3 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1218 32 18 15 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314208 112599 0 None -3 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1218 32 18 15 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
134150893 151370 0 None 19 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3966187 151370 0 None 19 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL2152050 207538 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
24995518 145027 0 None -5 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3915251 145027 0 None -5 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1183 31 18 14 -2.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707476 112598 0 None -6 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314207 112598 0 None -6 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
24996486 150216 0 None -4 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3956437 150216 0 None -4 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1240 35 19 15 -2.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707489 112611 0 None -13 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1199 30 18 13 -0.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314220 112611 0 None -13 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1199 30 18 13 -0.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL374295 210442 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL375432 210463 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
134150351 151174 0 None -14 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1271 30 17 14 -1.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3964403 151174 0 None -14 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1271 30 17 14 -1.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24992020 151684 0 None -5 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1215 31 18 14 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3968824 151684 0 None -5 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1215 31 18 14 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24996490 149342 0 None -16 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1258 35 19 15 -2.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3949224 149342 0 None -16 2 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1258 35 19 15 -2.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL2152051 207539 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
CHEMBL3422511 209916 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm5019675
24994272 152661 0 None -3 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3977235 152661 0 None -3 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1197 31 17 14 -2.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)N(C)C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
24996809 148072 0 None -6 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1187 31 18 14 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3939287 148072 0 None -6 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1187 31 18 14 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707481 112603 0 None -12 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1303 33 18 14 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314212 112603 0 None -12 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1303 33 18 14 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
155534572 171369 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 1040 28 16 12 -2.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4470482 171369 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 1040 28 16 12 -2.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL434379 211895 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL2152053 207541 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
CHEMBL414811 211400 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
155559308 174264 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 910 24 13 9 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4562955 174264 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL 910 24 13 9 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
57653049 151570 0 None -11 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1243 30 18 15 -3.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3967782 151570 0 None -11 2 Rat 8.1 pEC50 = 8.1 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1243 30 18 15 -3.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1cccc(F)c1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL435922 211916 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL385105 210585 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
134132372 144554 0 None -19 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3911692 144554 0 None -19 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1209 30 17 14 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
118707487 112609 0 None -13 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314218 112609 0 None -13 2 Rat 8.0 pEC50 = 8.0 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL375395 210462 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/jm0609824
118707483 112605 0 None -33 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 30 17 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(O)CN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314214 112605 0 None -33 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1230 30 17 15 -2.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(O)CN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
135936864 10355 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 483 7 4 7 4.6 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164674 10355 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 483 7 4 7 4.6 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016360 10359 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 497 8 4 7 5.0 N#Cc1c(-c2cccc(NC(=O)CCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164939 10359 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 497 8 4 7 5.0 N#Cc1c(-c2cccc(NC(=O)CCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016359 10338 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 477 7 4 6 4.5 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1ccccc1 10.1016/j.bmc.2010.04.036
CHEMBL1164153 10338 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 477 7 4 6 4.5 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1ccccc1 10.1016/j.bmc.2010.04.036
136016412 10373 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 527 8 4 7 4.7 CC(C)(CN)CNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.04.036
CHEMBL1165432 10373 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 527 8 4 7 4.7 CC(C)(CN)CNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.04.036
136016444 10379 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 469 6 4 7 4.2 N#Cc1c(-c2cccc(NC(=O)CN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1165783 10379 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 469 6 4 7 4.2 N#Cc1c(-c2cccc(NC(=O)CN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016380 10366 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 501 7 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1165222 10366 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 501 7 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016381 10331 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 517 7 4 7 5.2 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Cl)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1163896 10331 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 517 7 4 7 5.2 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Cl)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
135936875 10328 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 485 7 4 7 4.3 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
CHEMBL1163809 10328 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 485 7 4 7 4.3 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
136016362 10361 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1165100 10361 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016382 10332 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 561 7 4 7 5.4 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Br)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1163897 10332 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 561 7 4 7 5.4 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Br)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016407 10324 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 485 7 4 7 3.7 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
CHEMBL1163736 10324 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 485 7 4 7 3.7 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
CHEMBL3086284 209246 2 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Affinity Phenotypic Cellular interaction (Cell proliferation assay (cell growth inhibition in CHO/h175 cells)) EUB0000349a KISS1RAffinity Phenotypic Cellular interaction (Cell proliferation assay (cell growth inhibition in CHO/h175 cells)) EUB0000349a KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O nan
136016389 10330 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 497 7 4 7 4.9 Cc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3cccs3)n2)c(O)c1 10.1016/j.bmc.2010.04.036
CHEMBL1163888 10330 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assayAntagonist activity at human GPR54 receptor expressed in CHO cells assessed as inhibition of metastin(40-54)-induced intracellular calcium mobilization by FLIPR assay
ChEMBL 497 7 4 7 4.9 Cc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3cccs3)n2)c(O)c1 10.1016/j.bmc.2010.04.036
135401501 10878 2 None -3 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GPR54 receptor assessed as inhibition of metastin-induced calcium mobilizationAntagonist activity at human GPR54 receptor assessed as inhibition of metastin-induced calcium mobilization
ChEMBL 483 5 3 7 4.4 N#Cc1c(-c2cccc(N3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1173643 10878 2 None -3 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GPR54 receptor assessed as inhibition of metastin-induced calcium mobilizationAntagonist activity at human GPR54 receptor assessed as inhibition of metastin-induced calcium mobilization
ChEMBL 483 5 3 7 4.4 N#Cc1c(-c2cccc(N3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
10222 3671 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 27589480
46700761 3671 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 27589480
CHEMBL3924151 3671 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 27589480
DB11975 3671 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 27589480
1287 2152 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
155817402 2152 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
4014 117 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18302161
4015 1487 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19934405


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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
CHEMBL3086284 209246 2 None -1 3 Rat 9.8 pEC50 = 9.8 Binding
Agonist activity at rat KISS1RAgonist activity at rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
155551159 173369 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at rat KISS1RAgonist activity at rat KISS1R
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL4541289 173369 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at rat KISS1RAgonist activity at rat KISS1R
ChEMBL 796 19 11 8 0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2018.12.016
1281 2148 27 None 1 2 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL None None None None 10.1021/jm800930w
1283 2148 27 None 1 2 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL None None None None 10.1021/jm800930w
25240297 2148 27 None 1 2 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL None None None None 10.1021/jm800930w
CHEMBL376756 2148 27 None 1 2 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL None None None None 10.1021/jm800930w
1281 2148 27 None 1 2 Human 10.1 pIC50 = 10.1 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
1283 2148 27 None 1 2 Human 10.1 pIC50 = 10.1 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
25240297 2148 27 None 1 2 Human 10.1 pIC50 = 10.1 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
CHEMBL376756 2148 27 None 1 2 Human 10.1 pIC50 = 10.1 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
CHEMBL2151642 207534 0 None 2 2 Human 10.0 pIC50 = 10.0 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
1281 2148 27 None -1 2 Rat 10.0 pIC50 = 10.0 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
1283 2148 27 None -1 2 Rat 10.0 pIC50 = 10.0 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
25240297 2148 27 None -1 2 Rat 10.0 pIC50 = 10.0 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
CHEMBL376756 2148 27 None -1 2 Rat 10.0 pIC50 = 10.0 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
58143625 124858 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 183 6 1 2 2.0 CNC/C=C/[C@@H](CC(C)C)C(C)=O nan
CHEMBL3645499 124858 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 183 6 1 2 2.0 CNC/C=C/[C@@H](CC(C)C)C(C)=O nan
1281 2148 27 None 1 2 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None None 10.1021/ml1002053
1283 2148 27 None 1 2 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None None 10.1021/ml1002053
25240297 2148 27 None 1 2 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None None 10.1021/ml1002053
CHEMBL376756 2148 27 None 1 2 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None None 10.1021/ml1002053
25138123 178658 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL 781 21 9 6 2.9 CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml1002053
CHEMBL472833 178658 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL 781 21 9 6 2.9 CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml1002053
25138123 178658 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 781 21 9 6 2.9 CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL472833 178658 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 781 21 9 6 2.9 CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
71460220 80336 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1328 36 19 16 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151653 80336 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1328 36 19 16 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461938 80329 0 None 1 2 Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151646 80329 0 None 1 2 Human 9.8 pIC50 = 9.8 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461938 80329 0 None -1 2 Rat 9.8 pIC50 = 9.8 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151646 80329 0 None -1 2 Rat 9.8 pIC50 = 9.8 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71460219 80333 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1284 36 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151650 80333 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1284 36 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461940 80337 0 None 1 2 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151654 80337 0 None 1 2 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71460220 80336 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1328 36 19 16 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151653 80336 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1328 36 19 16 -3.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461940 80337 0 None -1 2 Rat 9.7 pIC50 = 9.7 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151654 80337 0 None -1 2 Rat 9.7 pIC50 = 9.7 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
58143618 124863 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@@H](O)CC(CC(C)C)C(C)=O nan
CHEMBL3645504 124863 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@@H](O)CC(CC(C)C)C(C)=O nan
71460219 80333 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1284 36 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151650 80333 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1284 36 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
25138131 173288 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL453956 173288 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL2151642 207534 0 None -2 2 Rat 9.6 pIC50 = 9.6 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71449399 80338 0 None 1 2 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151655 80338 0 None 1 2 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71451197 80335 0 None -1 2 Rat 9.6 pIC50 = 9.6 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151652 80335 0 None -1 2 Rat 9.6 pIC50 = 9.6 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71449399 80338 0 None -1 2 Rat 9.6 pIC50 = 9.6 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151655 80338 0 None -1 2 Rat 9.6 pIC50 = 9.6 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71451197 80335 0 None 1 2 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151652 80335 0 None 1 2 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71460218 80332 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1244 36 19 16 -4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151649 80332 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1244 36 19 16 -4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71456525 80330 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1218 35 20 17 -6.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151647 80330 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1218 35 20 17 -6.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71460218 80332 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1244 36 19 16 -4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151649 80332 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1244 36 19 16 -4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71456525 80330 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1218 35 20 17 -6.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151647 80330 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1218 35 20 17 -6.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461937 80328 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1316 38 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(=O)N[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151645 80328 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1316 38 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(=O)N[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71456524 80327 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1302 39 19 16 -3.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151644 80327 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1302 39 19 16 -3.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461939 80334 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151651 80334 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
59002736 124857 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 200 6 2 3 0.3 CNCC(=O)N[C@@H](CC(C)C)C(C)=O nan
CHEMBL3645498 124857 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 200 6 2 3 0.3 CNCC(=O)N[C@@H](CC(C)C)C(C)=O nan
16735569 141790 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml1002053
CHEMBL388586 141790 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml1002053
16735569 141790 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL388586 141790 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
71449398 80331 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1232 35 20 17 -6.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151648 80331 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1232 35 20 17 -6.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71449398 80331 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1232 35 20 17 -6.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151648 80331 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1232 35 20 17 -6.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461939 80334 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151651 80334 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
58143621 124859 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 185 7 1 2 2.2 CNCCC[C@@H](CC(C)C)C(C)=O nan
CHEMBL3645500 124859 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 185 7 1 2 2.2 CNCCC[C@@H](CC(C)C)C(C)=O nan
25138124 169727 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 783 22 9 6 3.2 CC(C)C[C@H](CCCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL444664 169727 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 783 22 9 6 3.2 CC(C)C[C@H](CCCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
71456524 80327 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1302 39 19 16 -3.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151644 80327 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1302 39 19 16 -3.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
136016473 10470 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 513 8 3 7 4.9 CN(C)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1169902 10470 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 513 8 3 7 4.9 CN(C)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016474 10543 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 9 3 7 5.3 CCN(C)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170468 10543 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 9 3 7 5.3 CCN(C)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016476 10569 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 9 4 7 5.3 CCNC(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170685 10569 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 9 4 7 5.3 CCNC(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
135410889 10602 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1170904 10602 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016519 10813 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 2 7 5.1 CCN1CCN(c2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
CHEMBL1173008 10813 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 2 7 5.1 CCN1CCN(c2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
136016412 10373 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 527 8 4 7 4.7 CC(C)(CN)CNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.04.036
CHEMBL1165432 10373 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 527 8 4 7 4.7 CC(C)(CN)CNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.04.036
136016490 10693 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 499 7 3 7 4.5 CN(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1171977 10693 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 499 7 3 7 4.5 CN(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016389 10330 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 7 4 7 4.9 Cc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3cccs3)n2)c(O)c1 10.1016/j.bmc.2010.04.036
CHEMBL1163888 10330 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 7 4 7 4.9 Cc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3cccs3)n2)c(O)c1 10.1016/j.bmc.2010.04.036
136016372 10321 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2ccc(C(=O)NCCN)cc2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1163732 10321 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2ccc(C(=O)NCCN)cc2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016390 10335 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 8 4 7 4.5 COc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3ccccc3)n2)c(O)c1 10.1016/j.bmc.2010.04.036
CHEMBL1163972 10335 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 8 4 7 4.5 COc1ccc(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3ccccc3)n2)c(O)c1 10.1016/j.bmc.2010.04.036
136016413 10325 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 481 7 4 7 4.4 Cc1c(-c2ccccc2O)nc(NC(=O)c2ccco2)c(C#N)c1-c1cccc(NC(=O)CCN)c1 10.1016/j.bmc.2010.04.036
CHEMBL1163739 10325 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 481 7 4 7 4.4 Cc1c(-c2ccccc2O)nc(NC(=O)c2ccco2)c(C#N)c1-c1cccc(NC(=O)CCN)c1 10.1016/j.bmc.2010.04.036
136016490 10693 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 499 7 3 7 4.5 CN(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1171977 10693 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 499 7 3 7 4.5 CN(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016484 10633 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 539 7 4 7 5.4 N#Cc1c(-c2cccc(NC(=O)CC3CCCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1171294 10633 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 539 7 4 7 5.4 N#Cc1c(-c2cccc(NC(=O)CC3CCCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016391 10367 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 467 7 4 7 3.5 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
CHEMBL1165223 10367 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 467 7 4 7 3.5 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
136016492 10634 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 539 7 3 7 5.4 N#Cc1c(-c2cccc(NC(=O)CN3CCCCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1171296 10634 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 539 7 3 7 5.4 N#Cc1c(-c2cccc(NC(=O)CN3CCCCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016518 10809 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 5 2 7 4.7 CN1CCN(c2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
CHEMBL1172940 10809 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 5 2 7 4.7 CN1CCN(c2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
135401501 10878 2 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 483 5 3 7 4.4 N#Cc1c(-c2cccc(N3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1173643 10878 2 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 483 5 3 7 4.4 N#Cc1c(-c2cccc(N3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016398 10323 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 495 7 4 7 4.3 CC(C)(CN)NC(=O)c1cccc(-c2cc(-c3ccccc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.04.036
CHEMBL1163735 10323 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 495 7 4 7 4.3 CC(C)(CN)NC(=O)c1cccc(-c2cc(-c3ccccc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.04.036
136016436 10340 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 427 5 3 6 4.8 N#Cc1c(-c2cccc(CO)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164235 10340 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 427 5 3 6 4.8 N#Cc1c(-c2cccc(CO)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016475 10568 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 541 10 3 7 5.6 CCN(CC)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170684 10568 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 541 10 3 7 5.6 CCN(CC)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016489 10622 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)[C@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1171102 10622 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)[C@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1672381 207078 4 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None CN(C)c1cccc2c(S(=O)(=O)N3CCC[C@H]3C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)cccc12 10.1021/ml1002053
136016478 10598 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 555 10 3 7 6.0 CCN(CC)C(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170895 10598 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 555 10 3 7 6.0 CCN(CC)C(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016477 10597 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 8 3 7 5.3 CC(CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1)N(C)C 10.1016/j.bmc.2010.05.061
CHEMBL1170894 10597 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 8 3 7 5.3 CC(CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1)N(C)C 10.1016/j.bmc.2010.05.061
136016483 10621 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 539 7 3 7 5.4 CN1CCC[C@H]1CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1171097 10621 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 539 7 3 7 5.4 CN1CCC[C@H]1CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016522 10861 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 2 7 4.7 CN1CCN(Cc2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
CHEMBL1173438 10861 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 2 7 4.7 CN1CCN(Cc2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
71451197 80335 0 None 1 2 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151652 80335 0 None 1 2 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
136016471 10464 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 7 3 7 4.8 CN(C)CC(=O)Nc1cccc(-c2cc(-c3ccccc3O)nc(NC(=O)c3cccs3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1169893 10464 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 7 3 7 4.8 CN(C)CC(=O)Nc1cccc(-c2cc(-c3ccccc3O)nc(NC(=O)c3cccs3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016382 10332 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 561 7 4 7 5.4 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Br)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1163897 10332 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 561 7 4 7 5.4 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Br)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
71454755 80326 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1332 38 19 16 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=S)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151643 80326 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL 1332 38 19 16 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=S)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
71461937 80328 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1316 38 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(=O)N[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151645 80328 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1316 38 19 16 -3.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(=O)N[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
136016523 10869 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 525 7 2 7 5.1 CCN1CCN(Cc2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
CHEMBL1173512 10869 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 525 7 2 7 5.1 CCN1CCN(Cc2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
136016486 14220 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 513 8 3 7 4.3 CN(C)CCNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1171483 14220 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 513 8 3 7 4.3 CN(C)CCNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1200097 14220 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 513 8 3 7 4.3 CN(C)CCNC(=O)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016472 10469 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 499 8 4 7 4.5 CNCCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1169901 10469 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 499 8 4 7 4.5 CNCCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
135936864 10355 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.6 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164674 10355 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.6 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
135528869 10350 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 4 3 6 4.9 N#Cc1c(-c2cccc(N)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164603 10350 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 412 4 3 6 4.9 N#Cc1c(-c2cccc(N)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016480 10679 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 569 11 3 7 6.4 CCC(CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1)N(CC)CC 10.1016/j.bmc.2010.05.061
CHEMBL1171797 10679 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 569 11 3 7 6.4 CCC(CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1)N(CC)CC 10.1016/j.bmc.2010.05.061
25138132 188320 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 798 21 10 7 1.3 CC(C)C[C@@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL507796 188320 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 798 21 10 7 1.3 CC(C)C[C@@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
135410892 14250 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 3 7 4.8 N#Cc1c(-c2cccc(CN3CCCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1200240 14250 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 3 7 4.8 N#Cc1c(-c2cccc(CN3CCCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL3216935 14250 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 511 6 3 7 4.8 N#Cc1c(-c2cccc(CN3CCCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016482 10601 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1170903 10601 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016488 10603 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 485 7 4 7 4.1 CNCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170911 10603 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 485 7 4 7 4.1 CNCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
71454755 80326 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1332 38 19 16 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=S)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
CHEMBL2151643 80326 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1332 38 19 16 -2.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=S)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.069
135401501 10878 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 483 5 3 7 4.4 N#Cc1c(-c2cccc(N3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1173643 10878 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 483 5 3 7 4.4 N#Cc1c(-c2cccc(N3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
135936875 10328 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 485 7 4 7 4.3 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1163809 10328 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 485 7 4 7 4.3 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
135936875 10328 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 485 7 4 7 4.3 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
CHEMBL1163809 10328 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 485 7 4 7 4.3 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
136016491 10623 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 9 4 7 5.3 CCNC(CC)C(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1171104 10623 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 527 9 4 7 5.3 CCNC(CC)C(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016493 10665 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 499 8 2 7 5.0 CN(C)CCN(C)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1171663 10665 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 499 8 2 7 5.0 CN(C)CCN(C)c1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016362 10361 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1165100 10361 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016397 10322 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 8 4 7 3.9 COc1ccc(C(=O)Nc2nc(-c3ccccc3O)cc(-c3cccc(C(=O)NCCN)c3)c2C#N)cc1 10.1016/j.bmc.2010.04.036
CHEMBL1163734 10322 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 8 4 7 3.9 COc1ccc(C(=O)Nc2nc(-c3ccccc3O)cc(-c3cccc(C(=O)NCCN)c3)c2C#N)cc1 10.1016/j.bmc.2010.04.036
58143614 124861 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 199 6 2 3 1.1 CNC[C@H](O)/C=C(\CC(C)C)C(C)=O nan
CHEMBL3645502 124861 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 199 6 2 3 1.1 CNC[C@H](O)/C=C(\CC(C)C)C(C)=O nan
58143618 124863 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@@H](O)CC(CC(C)C)C(C)=O nan
CHEMBL3645504 124863 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@@H](O)CC(CC(C)C)C(C)=O nan
25138126 171893 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 797 21 10 7 2.1 CC(C)C/C(=C\[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL448207 171893 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 797 21 10 7 2.1 CC(C)C/C(=C\[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
25138130 172173 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@@H](C[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL450923 172173 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@@H](C[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
136016399 10327 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 535 8 4 7 4.7 COc1ccccc1C(=O)Nc1nc(-c2ccccc2O)cc(-c2cccc(C(=O)NC(C)(C)CN)c2)c1C#N 10.1016/j.bmc.2010.04.036
CHEMBL1163808 10327 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 535 8 4 7 4.7 COc1ccccc1C(=O)Nc1nc(-c2ccccc2O)cc(-c2cccc(C(=O)NC(C)(C)CN)c2)c1C#N 10.1016/j.bmc.2010.04.036
136016406 10374 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 535 8 4 7 4.7 COc1ccc(C(=O)Nc2nc(-c3ccccc3O)cc(-c3cccc(C(=O)NC(C)(C)CN)c3)c2C#N)cc1 10.1016/j.bmc.2010.04.036
CHEMBL1165467 10374 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 535 8 4 7 4.7 COc1ccc(C(=O)Nc2nc(-c3ccccc3O)cc(-c3cccc(C(=O)NC(C)(C)CN)c3)c2C#N)cc1 10.1016/j.bmc.2010.04.036
136016361 10339 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2ccccc2C(=O)NCCN)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164154 10339 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 483 7 4 7 4.0 N#Cc1c(-c2ccccc2C(=O)NCCN)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016360 10359 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 8 4 7 5.0 N#Cc1c(-c2cccc(NC(=O)CCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164939 10359 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 8 4 7 5.0 N#Cc1c(-c2cccc(NC(=O)CCCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
88978455 124864 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 200 6 2 3 0.3 CNCC(=O)N[C@H](CC(C)C)C(C)=O nan
CHEMBL3645505 124864 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 200 6 2 3 0.3 CNCC(=O)N[C@H](CC(C)C)C(C)=O nan
135410889 10602 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1170904 10602 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
58143615 124862 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@H](O)CC(CC(C)C)C(C)=O nan
CHEMBL3645503 124862 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@H](O)CC(CC(C)C)C(C)=O nan
25138128 181408 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@@H](C[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL478053 181408 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@@H](C[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
136016487 10646 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 471 6 4 7 3.9 N#Cc1c(-c2cccc(NC(=O)CN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1171484 10646 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 471 6 4 7 3.9 N#Cc1c(-c2cccc(NC(=O)CN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
122196636 124860 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 183 6 1 2 2.2 CNCC/C=C(/CC(C)C)C(C)=O nan
CHEMBL3645501 124860 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 183 6 1 2 2.2 CNCC/C=C(/CC(C)C)C(C)=O nan
25138125 187756 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 781 21 9 6 3.1 CC(C)C/C(=C\CCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL501043 187756 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 781 21 9 6 3.1 CC(C)C/C(=C\CCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
136016472 10469 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 499 8 4 7 4.5 CNCCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1169901 10469 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 499 8 4 7 4.5 CNCCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL3087931 209258 0 None -1 2 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
136016392 10368 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 8 4 7 3.9 COc1ccccc1C(=O)Nc1nc(-c2ccccc2O)cc(-c2cccc(C(=O)NCCN)c2)c1C#N 10.1016/j.bmc.2010.04.036
CHEMBL1165224 10368 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 8 4 7 3.9 COc1ccccc1C(=O)Nc1nc(-c2ccccc2O)cc(-c2cccc(C(=O)NCCN)c2)c1C#N 10.1016/j.bmc.2010.04.036
58143616 124865 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 199 6 2 3 1.1 CNC[C@@H](O)/C=C(\CC(C)C)C(C)=O nan
CHEMBL3645506 124865 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 199 6 2 3 1.1 CNC[C@@H](O)/C=C(\CC(C)C)C(C)=O nan
25138127 169627 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 797 21 10 7 2.1 CC(C)C/C(=C\[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL444522 169627 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 797 21 10 7 2.1 CC(C)C/C(=C\[C@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
136016473 10470 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 513 8 3 7 4.9 CN(C)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1169902 10470 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 513 8 3 7 4.9 CN(C)CCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016519 10813 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 511 6 2 7 5.1 CCN1CCN(c2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
CHEMBL1173008 10813 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]metastin from rat GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from rat GPR54 receptor expressed in CHO cells
ChEMBL 511 6 2 7 5.1 CCN1CCN(c2cccc(-c3cc(-c4ccc(F)cc4O)nc(NC(=O)c4ccco4)c3C#N)c2)CC1 10.1016/j.bmc.2010.05.061
136016379 10362 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 513 8 4 8 4.6 COc1ccc(O)c(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3cccs3)n2)c1 10.1016/j.bmc.2010.04.036
CHEMBL1165103 10362 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 513 8 4 8 4.6 COc1ccc(O)c(-c2cc(-c3cccc(NC(=O)CCN)c3)c(C#N)c(NC(=O)c3cccs3)n2)c1 10.1016/j.bmc.2010.04.036
136016373 10360 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 517 7 4 7 5.2 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2cc(Cl)ccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164988 10360 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 517 7 4 7 5.2 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2cc(Cl)ccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
58143615 124862 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@H](O)CC(CC(C)C)C(C)=O nan
CHEMBL3645503 124862 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: Binding inhibition assay using human GPR54.Binding Assay: Binding inhibition assay using human GPR54.
ChEMBL 201 7 2 3 1.2 CNC[C@H](O)CC(CC(C)C)C(C)=O nan
25138129 188038 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
CHEMBL503052 188038 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL 799 22 10 7 2.1 CC(C)C[C@H](C[C@@H](O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800930w
136016359 10338 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 477 7 4 6 4.5 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1ccccc1 10.1016/j.bmc.2010.04.036
CHEMBL1164153 10338 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 477 7 4 6 4.5 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2O)nc1NC(=O)c1ccccc1 10.1016/j.bmc.2010.04.036
136016444 10379 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 469 6 4 7 4.2 N#Cc1c(-c2cccc(NC(=O)CN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1165783 10379 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 469 6 4 7 4.2 N#Cc1c(-c2cccc(NC(=O)CN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016443 10354 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 3 6 4.8 N#Cc1c(-c2cccc(CN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164673 10354 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 426 5 3 6 4.8 N#Cc1c(-c2cccc(CN)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016517 10879 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 5 3 7 4.8 N#Cc1c(-c2cccc(N3CCCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1173644 10879 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 5 3 7 4.8 N#Cc1c(-c2cccc(N3CCCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016380 10366 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 501 7 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.05.061
CHEMBL1165222 10366 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 501 7 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.05.061
136016380 10366 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 501 7 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1165222 10366 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 501 7 4 7 4.7 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016482 10601 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1170903 10601 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 525 7 4 7 5.1 N#Cc1c(-c2cccc(NC(=O)C[C@@H]3CCCN3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016479 10599 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 541 10 4 7 5.7 CCNC(CC)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170896 10599 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 541 10 4 7 5.7 CCNC(CC)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016407 10324 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 485 7 4 7 3.7 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
CHEMBL1163736 10324 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 485 7 4 7 3.7 N#Cc1c(-c2cccc(C(=O)NCCN)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.04.036
136016488 10603 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 485 7 4 7 4.1 CNCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170911 10603 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 485 7 4 7 4.1 CNCC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL3086284 209246 2 None 1 3 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
1486 3259 23 None - 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/ml1002053
53320361 3259 23 None - 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/ml1002053
CHEMBL1672380 3259 23 None - 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/ml1002053
1281 2148 27 None 1 2 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None None 10.1021/jm401056w
1283 2148 27 None 1 2 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None None 10.1021/jm401056w
25240297 2148 27 None 1 2 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None None 10.1021/jm401056w
CHEMBL376756 2148 27 None 1 2 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None None 10.1021/jm401056w
CHEMBL2151642 207534 0 None 2 2 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
46906647 10372 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 476 7 4 6 4.4 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2N)nc1NC(=O)c1ccccc1 10.1016/j.bmc.2010.04.036
CHEMBL1165431 10372 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 476 7 4 6 4.4 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccccc2N)nc1NC(=O)c1ccccc1 10.1016/j.bmc.2010.04.036
71461938 80329 0 None 1 2 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151646 80329 0 None 1 2 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
136016481 10575 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 541 9 4 7 5.7 CC(C)NC(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
CHEMBL1170692 10575 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 541 9 4 7 5.7 CC(C)NC(C)CC(=O)Nc1cccc(-c2cc(-c3ccc(F)cc3O)nc(NC(=O)c3ccco3)c2C#N)c1 10.1016/j.bmc.2010.05.061
136016521 14196 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 6 3 7 4.4 N#Cc1c(-c2cccc(CN3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1170870 14196 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 6 3 7 4.4 N#Cc1c(-c2cccc(CN3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
CHEMBL1200013 14196 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]metastin from human GPR54 receptor expressed in CHO cellsDisplacement of [125I]metastin from human GPR54 receptor expressed in CHO cells
ChEMBL 497 6 3 7 4.4 N#Cc1c(-c2cccc(CN3CCNCC3)c2)cc(-c2ccc(F)cc2O)nc1NC(=O)c1ccco1 10.1016/j.bmc.2010.05.061
136016381 10331 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 517 7 4 7 5.2 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Cl)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1163896 10331 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 517 7 4 7 5.2 N#Cc1c(-c2cccc(NC(=O)CCN)c2)cc(-c2ccc(Cl)cc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
136016437 10341 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 441 5 3 6 5.0 N#Cc1c(-c2cccc(C(=O)O)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL1164236 10341 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 441 5 3 6 5.0 N#Cc1c(-c2cccc(C(=O)O)c2)cc(-c2ccccc2O)nc1NC(=O)c1cccs1 10.1016/j.bmc.2010.04.036
CHEMBL3315315 209623 0 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707495 112618 0 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1360 34 19 14 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314227 112618 0 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1360 34 19 14 0.3 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707486 112608 0 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1254 32 18 13 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314217 112608 0 None - 1 Human 10.6 pKi = 10.6 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1254 32 18 13 0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3086282 209244 0 None 1 2 Human 10.5 pKi = 10.5 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087927 209254 0 None 1 2 Human 10.5 pKi = 10.5 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1cnc[nH]1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707494 112617 0 None 2 2 Human 10.5 pKi = 10.5 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314226 112617 0 None 2 2 Human 10.5 pKi = 10.5 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
1281 2148 27 None 1 2 Human 10.5 pKi = 10.5 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
1283 2148 27 None 1 2 Human 10.5 pKi = 10.5 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
25240297 2148 27 None 1 2 Human 10.5 pKi = 10.5 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
CHEMBL376756 2148 27 None 1 2 Human 10.5 pKi = 10.5 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
118707485 112607 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1256 32 19 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314216 112607 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1256 32 19 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
49787129 112615 3 None 1 2 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314224 112615 3 None 1 2 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707484 112606 0 None 2 2 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314215 112606 0 None 2 2 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707497 112620 0 None 2 2 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL3314229 112620 0 None 2 2 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
1281 2148 27 None 1 2 Human 10.4 pKi = 10.4 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None None 10.1021/jm401056w
1283 2148 27 None 1 2 Human 10.4 pKi = 10.4 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None None 10.1021/jm401056w
25240297 2148 27 None 1 2 Human 10.4 pKi = 10.4 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None None 10.1021/jm401056w
CHEMBL376756 2148 27 None 1 2 Human 10.4 pKi = 10.4 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None None 10.1021/jm401056w
118707492 112614 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1241 32 18 13 -0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314223 112614 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1241 32 18 13 -0.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CCc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3087793 209251 0 None 1 2 Rat 10.4 pKi = 10.4 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CC(C)C[C@H](NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087925 209252 0 None 1 2 Rat 10.4 pKi = 10.4 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087927 209254 0 None -1 2 Rat 10.4 pKi = 10.4 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1cnc[nH]1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085809 209239 0 None 1 2 Human 10.4 pKi = 10.4 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087793 209251 0 None -1 2 Human 10.4 pKi = 10.4 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151642 207534 0 None 2 2 Human 10.3 pKi = 10.3 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
71461938 80329 0 None 1 2 Human 10.3 pKi = 10.3 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151646 80329 0 None 1 2 Human 10.3 pKi = 10.3 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086282 209244 0 None -1 2 Rat 10.3 pKi = 10.3 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085804 209234 0 None 1 2 Human 10.3 pKi = 10.3 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707478 112600 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1216 32 17 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314209 112600 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1216 32 17 14 -0.9 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3087929 209256 0 None 1 2 Human 10.3 pKi = 10.3 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
1281 2148 27 None -1 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1021/jm401056w
1283 2148 27 None -1 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1021/jm401056w
25240297 2148 27 None -1 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1021/jm401056w
CHEMBL376756 2148 27 None -1 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1021/jm401056w
CHEMBL3085809 209239 0 None -1 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087925 209252 0 None -1 2 Human 10.2 pKi = 10.2 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
1281 2148 27 None 1 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting methodDisplacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
1283 2148 27 None 1 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting methodDisplacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
25240297 2148 27 None 1 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting methodDisplacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
CHEMBL376756 2148 27 None 1 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting methodDisplacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
CHEMBL3086283 209245 0 None 1 2 Human 10.2 pKi = 10.2 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
71461938 80329 0 None -1 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151646 80329 0 None -1 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
49787129 112615 3 None -1 2 Rat 10.2 pKi = 10.2 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314224 112615 3 None -1 2 Rat 10.2 pKi = 10.2 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3085804 209234 0 None -1 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707476 112598 0 None 1 2 Human 10.1 pKi = 10.1 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314207 112598 0 None 1 2 Human 10.1 pKi = 10.1 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3087929 209256 0 None -1 2 Rat 10.1 pKi = 10.1 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707484 112606 0 None -2 2 Rat 10.1 pKi = 10.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314215 112606 0 None -2 2 Rat 10.1 pKi = 10.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1242 32 19 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
71461940 80337 0 None 1 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151654 80337 0 None 1 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086281 209243 0 None 1 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087926 209253 0 None 1 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CO)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707477 112599 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1218 32 18 15 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314208 112599 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1218 32 18 15 -2.2 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707494 112617 0 None -2 2 Rat 10.1 pKi = 10.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314226 112617 0 None -2 2 Rat 10.1 pKi = 10.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1324 34 19 14 -0.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)C1CC1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707497 112620 0 None -2 2 Rat 10.1 pKi = 10.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL3314229 112620 0 None -2 2 Rat 10.1 pKi = 10.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1259 33 18 14 -1.4 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
1281 2148 27 None -1 2 Rat 10.1 pKi = 10.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
1283 2148 27 None -1 2 Rat 10.1 pKi = 10.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
25240297 2148 27 None -1 2 Rat 10.1 pKi = 10.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
CHEMBL376756 2148 27 None -1 2 Rat 10.1 pKi = 10.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
CHEMBL3086284 209246 2 None 1 3 Human 10.1 pKi = 10.1 Binding
Affinity Biochemical interaction (Binding assay (used membrane fraction of human KISS1R-expressing cells)) EUB0000349a KISS1RAffinity Biochemical interaction (Binding assay (used membrane fraction of human KISS1R-expressing cells)) EUB0000349a KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O nan
CHEMBL3086284 209246 2 None 1 3 Human 10.1 pKi = 10.1 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707496 112619 0 None 1 2 Human 10.1 pKi = 10.1 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314228 112619 0 None 1 2 Human 10.1 pKi = 10.1 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
71461940 80337 0 None -1 2 Rat 10.0 pKi = 10.0 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151654 80337 0 None -1 2 Rat 10.0 pKi = 10.0 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1317 36 20 16 -3.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087926 209253 0 None -1 2 Rat 10.0 pKi = 10.0 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CO)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087931 209258 0 None 1 2 Rat 10.0 pKi = 10.0 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707482 112604 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1214 30 16 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314213 112604 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1214 30 16 14 -1.1 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3086284 209246 2 None -1 3 Rat 10.0 pKi = 10 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086286 209248 0 None 1 2 Human 10.0 pKi = 10.0 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087931 209258 0 None -1 2 Human 10.0 pKi = 10.0 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151642 207534 0 None -2 2 Rat 10.0 pKi = 10.0 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086283 209245 0 None -1 2 Rat 10.0 pKi = 10.0 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086284 209246 2 None 1 3 Human 10.0 pKi = 10.0 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
118707493 112616 0 None - 1 Rat 10.0 pKi = 10.0 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1326 35 19 14 -0.2 CCCC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)O 10.1021/jm5005489
CHEMBL3314225 112616 0 None - 1 Rat 10.0 pKi = 10.0 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1326 35 19 14 -0.2 CCCC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)O 10.1021/jm5005489
71451197 80335 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151652 80335 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
71449399 80338 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151655 80338 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085806 209236 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086280 209242 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087928 209255 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
71451197 80335 0 None -1 2 Rat 9.9 pKi = 9.9 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151652 80335 0 None -1 2 Rat 9.9 pKi = 9.9 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
71449399 80338 0 None -1 2 Rat 9.9 pKi = 9.9 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL2151655 80338 0 None -1 2 Rat 9.9 pKi = 9.9 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL 1279 36 19 17 -4.7 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087928 209255 0 None -1 2 Rat 9.9 pKi = 9.9 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707491 112613 0 None 6 2 Human 9.9 pKi = 9.9 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314222 112613 0 None 6 2 Human 9.9 pKi = 9.9 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3086280 209242 0 None -1 2 Rat 9.9 pKi = 9.9 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086286 209248 0 None -1 2 Rat 9.9 pKi = 9.9 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707476 112598 0 None -1 2 Rat 9.9 pKi = 9.9 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314207 112598 0 None -1 2 Rat 9.9 pKi = 9.9 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1204 32 18 15 -2.6 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3085806 209236 0 None -1 2 Rat 9.9 pKi = 9.9 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086284 209246 2 None -1 3 Rat 9.9 pKi = 9.9 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL3086281 209243 0 None -1 2 Rat 9.8 pKi = 9.8 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085808 209238 0 None 1 2 Rat 9.8 pKi = 9.8 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707496 112619 0 None -1 2 Rat 9.8 pKi = 9.8 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314228 112619 0 None -1 2 Rat 9.8 pKi = 9.8 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1260 33 18 15 -2.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3085807 209237 0 None 1 2 Rat 9.7 pKi = 9.7 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085807 209237 0 None -1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085811 209241 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086285 209247 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707487 112609 0 None 18 2 Human 9.7 pKi = 9.7 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314218 112609 0 None 18 2 Human 9.7 pKi = 9.7 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3085808 209238 0 None -1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085810 209240 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085811 209241 0 None -1 2 Rat 9.6 pKi = 9.6 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087930 209257 0 None 1 2 Rat 9.6 pKi = 9.6 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086285 209247 0 None -1 2 Rat 9.6 pKi = 9.6 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087930 209257 0 None -1 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085810 209240 0 None -1 2 Rat 9.5 pKi = 9.5 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085805 209235 0 None 1 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085805 209235 0 None -1 2 Rat 9.3 pKi = 9.3 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL375982 210477 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
118707491 112613 0 None -6 2 Rat 9.1 pKi = 9.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314222 112613 0 None -6 2 Rat 9.1 pKi = 9.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1213 31 18 13 0.0 CC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)NC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
101134421 2149 10 None -6 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1284 2149 10 None -6 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2149 10 None -6 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2149 10 None -6 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1281 2148 27 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1283 2148 27 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
25240297 2148 27 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL376756 2148 27 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL262577 208787 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0609824
CHEMBL221602 207669 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
101134421 2149 10 None -6 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1284 2149 10 None -6 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2149 10 None -6 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2149 10 None -6 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL221141 207668 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/jm0609824
CHEMBL262316 208782 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL373854 210435 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374295 210442 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374748 210449 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(N)=O 10.1021/jm0609824
CHEMBL410741 211078 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL426552 211588 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/jm0609824
CHEMBL375006 210453 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL375395 210462 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/jm0609824
CHEMBL441935 212145 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL220759 207666 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CCCC[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL434379 211895 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL221816 207672 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(N)=O 10.1021/jm0609824
CHEMBL435922 211916 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL375983 210478 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL220855 207667 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1CCCCC1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL414073 211349 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm0609824
CHEMBL375450 210465 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL373714 210434 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(N)=O 10.1021/jm0609824
CHEMBL386958 210645 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374246 210439 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
118707487 112609 0 None -18 2 Rat 8.4 pKi = 8.4 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314218 112609 0 None -18 2 Rat 8.4 pKi = 8.4 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1161 30 17 14 -1.5 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL373676 210433 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
2335 11728 21 None -8 12 Human 5.4 pKi = 5.4 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1021/jm0609824
8478 11728 21 None -8 12 Human 5.4 pKi = 5.4 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1021/jm0609824
CHEMBL1182210 11728 21 None -8 12 Human 5.4 pKi = 5.4 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1021/jm0609824
CHEMBL221753 11728 21 None -8 12 Human 5.4 pKi = 5.4 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1021/jm0609824
CHEMBL435315 211905 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cccnc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL221817 207673 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0609824
CHEMBL221761 207670 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL439094 212063 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
101134421 2149 10 None -6 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1284 2149 10 None -6 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2149 10 None -6 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2149 10 None -6 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL434382 211897 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
10301495 82812 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 517 6 2 7 5.1 NCCCn1nc(C2=C(c3cn(-c4csc5ccccc45)c4ccccc34)C(=O)NC2=O)c2ccccc21 10.1021/jm0609824
CHEMBL218690 82812 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 517 6 2 7 5.1 NCCCn1nc(C2=C(c3cn(-c4csc5ccccc45)c4ccccc34)C(=O)NC2=O)c2ccccc21 10.1021/jm0609824
CHEMBL414811 211400 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL414073 211349 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm0609824
CHEMBL385105 210585 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL221764 207671 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374260 210440 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cccnc1)C(N)=O 10.1021/jm0609824
CHEMBL375432 210463 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
CHEMBL374077 210436 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None CC(C)C[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0609824
1281 2148 27 None 1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1283 2148 27 None 1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
25240297 2148 27 None 1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL376756 2148 27 None 1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
2335 11728 21 None -8 12 Human 8.3 pKi = 8.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
8478 11728 21 None -8 12 Human 8.3 pKi = 8.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
CHEMBL1182210 11728 21 None -8 12 Human 8.3 pKi = 8.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
CHEMBL221753 11728 21 None -8 12 Human 8.3 pKi = 8.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
1286 2151 0 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
155817401 2151 0 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1289 2156 0 None - 1 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
155817403 2156 0 None - 1 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
101134421 2149 10 None -6 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1284 2149 10 None -6 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL220853 2149 10 None -6 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL373467 2149 10 None -6 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
101134421 2149 10 None 6 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1284 2149 10 None 6 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL220853 2149 10 None 6 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL373467 2149 10 None 6 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1285 2150 0 None -1 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1288 2155 0 None -2 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1281 2148 27 None -1 2 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1283 2148 27 None -1 2 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
25240297 2148 27 None -1 2 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL376756 2148 27 None -1 2 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1285 2150 0 None 1 2 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1288 2155 0 None 2 2 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1288 2155 0 None 2 2 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1281 2148 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1281 2148 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1283 2148 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1283 2148 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
25240297 2148 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
25240297 2148 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL376756 2148 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
CHEMBL376756 2148 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843