Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
155550061 180663 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 180663 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 216077 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 180366 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 180366 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 178208 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 178208 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 216082 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 180176 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 180176 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 216078 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 87528 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 87528 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 87531 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 87531 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 217774 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 177418 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 177418 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 216068 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 216080 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 180730 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 180730 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 125651 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 125651 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 218444 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 87539 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 87539 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 156657 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 156657 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 218447 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 87538 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 87538 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 87535 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 87535 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 218446 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 87537 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 87537 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 178922 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 178922 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 182588 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 182588 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 87534 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 87534 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 177998 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 177998 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 181650 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 181650 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 216083 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 216084 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 180520 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 180520 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 176585 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 176585 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 178762 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 178762 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 87533 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 87533 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 87536 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 87536 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 180589 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 180589 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 178598 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 178598 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 217781 4 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 216074 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 216076 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 186026 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 186026 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 119903 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 119903 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 119897 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 119897 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 216079 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 181376 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 181376 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 119904 6 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 119904 6 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 119904 6 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 119904 6 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 216086 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 216085 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 180649 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 180649 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 216081 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 156665 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 156665 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 119907 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 119907 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 218158 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 149112 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 149112 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 160001 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 160001 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 151877 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 151877 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 158497 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 158497 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 119900 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 119900 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 119895 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 119895 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 153134 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 153134 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 87540 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 87540 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 119892 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 119892 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 179168 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 179168 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 125652 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 125652 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 160890 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 160890 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 87529 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 87529 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 178238 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 178238 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 119901 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 119901 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 119902 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 119902 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 154020 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 154020 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 149112 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 149112 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 119898 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 119898 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 87532 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 87532 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 158893 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 158893 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 119908 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 119908 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 104001 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 104001 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 119905 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 119905 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 119906 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 119906 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 119887 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 119887 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 177100 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 177100 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 218445 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 119909 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 119909 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 87530 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 87530 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 92247 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 92247 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 175935 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 175935 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 148873 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 148873 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 119896 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 119896 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 155395 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 155395 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 119903 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 119903 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 91583 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 91583 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 92213 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 92213 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 152350 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 152350 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 159007 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 159007 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 119893 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 119893 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 156657 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 156657 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 149111 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 149111 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 119899 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 119899 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 119904 6 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 119904 6 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 119904 6 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 119904 6 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 218158 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 92592 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 92592 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 178889 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 178889 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 154244 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 154244 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 216070 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 216088 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 179792 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 179792 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 119891 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 119891 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 216071 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 92226 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 92226 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 157540 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 157540 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 119888 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 119888 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 125665 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 125665 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 92274 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 92274 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 104010 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 104010 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 104011 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 104011 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 119907 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 119907 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 159986 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 159986 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 119889 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 119889 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 154020 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 154020 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 157712 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 157712 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 158803 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 158803 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 216089 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 217781 4 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 216202 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 217316 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 218971 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 218985 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 219614 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 220125 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 218989 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 218976 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 8970 11 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 8970 11 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 8970 11 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 8970 11 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 219181 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 157799 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 157799 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 160908 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 160908 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 216203 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 220442 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 220600 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 158693 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 158693 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 119890 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 119890 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 159850 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 159850 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 119889 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 119889 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 125653 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 125653 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 119893 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 119893 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 119901 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 119901 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 218450 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 180484 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 180484 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 154444 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 154444 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 151040 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 151040 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 158803 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 158803 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 149820 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 149820 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 158555 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 158555 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 216201 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 152220 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 152220 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 125662 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 125662 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 92228 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 92228 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 159850 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 159850 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 150078 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 150078 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 181062 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 181062 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 216090 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 119897 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 119897 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 154444 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 154444 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 157487 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 157487 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 119895 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 119895 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 158555 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 158555 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 177085 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 177085 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 218443 21 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 217781 4 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 92594 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 92594 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 151040 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 151040 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 149820 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 149820 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 157799 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 157799 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 119894 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 119894 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 153134 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 153134 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 119902 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 119902 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 125663 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 125663 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 157562 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 157562 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 160001 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 160001 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 216207 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 216205 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 218975 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 125666 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 125666 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 160783 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 160783 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 119891 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 119891 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 216204 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 8970 11 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 8970 11 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 8970 11 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 8970 11 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 157487 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 157487 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 125664 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 125664 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 220434 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 216200 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 219014 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 219013 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 218972 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 220682 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 148837 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 148837 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 149818 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 149818 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 168653 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 168653 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 92227 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 92227 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 143735 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 143735 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 92593 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 92593 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 148808 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 148808 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 160908 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 160908 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 152220 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 152220 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 119905 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 119905 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 216087 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 119909 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 119909 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 219001 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 119899 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 119899 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 8970 11 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 8970 11 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 8970 11 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 8970 11 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 217321 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 218970 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 10512 9 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 10512 9 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 10512 9 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 10512 9 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 216206 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 218969 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 219886 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 119896 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 119896 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 119908 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 119908 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 119906 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 119906 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 195412 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 195412 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 156504 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 156504 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 119890 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 119890 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 148841 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 148841 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 157712 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 157712 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 154244 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 154244 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 160890 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 160890 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 157562 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 157562 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 160783 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 160783 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 156504 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 156504 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 160620 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 160620 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 150013 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 150013 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 219886 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 155331 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 155331 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 104012 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 104012 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 10512 9 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 10512 9 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 10512 9 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 10512 9 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 150013 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 150013 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 155331 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 155331 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 195129 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 195129 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 160620 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 160620 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 119888 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 119888 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 158693 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 158693 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 216072 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 152350 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 152350 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 119887 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 119887 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 157540 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 157540 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 119900 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 119900 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 218978 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 218999 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 158497 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 158497 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 159007 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 159007 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 156665 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 156665 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 216073 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 218451 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 159986 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 159986 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 155395 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 155395 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 119892 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 119892 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 178724 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 178724 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 220432 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 216075 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 219937 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 181625 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 181625 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 158893 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 158893 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 220453 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 219121 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 151877 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 151877 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 119898 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 119898 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 218998 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 119894 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 119894 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 17241 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 17241 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 17246 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 17246 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 17224 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 17224 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 17260 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 17260 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 17266 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 17266 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 17253 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 17253 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 17217 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 17217 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 17214 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 17214 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 17248 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 17248 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 17218 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 17218 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 17210 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 17210 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 217781 4 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 10.6019/CHEMBL5209897
136016389 17216 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 17216 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 17767 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 17767 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 10512 9 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 10512 9 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 10512 9 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 10512 9 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 8973 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
155817402 8973 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
4014 6905 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18302161
4015 8302 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19934405


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
CHEMBL3086284 217781 4 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 180730 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 180730 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 216068 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 132169 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 132169 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 186026 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 186026 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 186026 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 186026 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 87538 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 87538 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 87531 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 87531 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 87531 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 87531 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 87535 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 87535 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 87539 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 87539 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 87538 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 87538 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 87539 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 87539 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 132174 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 132174 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 87535 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 87535 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 180649 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 180649 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 216068 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 87540 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 87540 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 87537 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 87537 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 87540 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 87540 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 87537 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 87537 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 87534 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 87534 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 87532 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 87532 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 87534 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 87534 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 87532 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 87532 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 87530 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 87530 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 87529 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 87529 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 87536 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 87536 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 132168 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 132168 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 149112 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 149112 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 149112 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 149112 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 87533 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 87533 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 87533 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 87533 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 87536 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 87536 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 132170 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 132170 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 177085 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 177085 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 87529 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 87529 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 17357 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 17357 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 17430 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 17430 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 17456 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 17456 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 17489 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 17489 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 17701 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 17701 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 17260 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 17260 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 17581 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 17581 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 17216 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 17216 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 17207 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 17207 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 17221 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 17221 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 17211 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 17211 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 17581 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 17581 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 17520 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 17520 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 17254 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 17254 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 17521 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 17521 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 17697 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 17697 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 17767 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 17767 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 17209 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 17209 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 17226 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 17226 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 17455 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 17455 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 17509 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 17509 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 215610 5 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 17485 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 17485 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 17484 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 17484 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 17508 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 17508 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 17750 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 17750 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 87537 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 87537 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 17351 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 17351 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 17218 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 17218 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 87528 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 87528 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 87530 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 87530 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 17758 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 17758 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 21122 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 21122 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 21122 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 17356 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 17356 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 17241 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 17241 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 17236 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 17236 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 17566 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 17566 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 195696 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 195696 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 21152 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 21152 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 21152 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 17488 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 17488 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 17490 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 17490 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 87528 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 87528 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 17767 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 17767 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 17214 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 17214 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 17214 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 17214 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 17510 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 17510 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 17552 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 17552 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 17248 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 17248 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 17208 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 17208 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 132172 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 132172 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 132174 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 132174 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 179249 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 179249 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 179531 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 179531 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 17213 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 17213 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 17261 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 17261 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 17225 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 17225 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 17246 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 17246 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 132175 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 132175 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 17489 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 17489 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 132173 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 132173 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 188779 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 188779 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 17533 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 17533 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 132171 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 132171 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 195129 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 195129 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 17356 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 17356 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 217793 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 17255 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 17255 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 132176 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 132176 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 176984 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 176984 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 17357 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 17357 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 17701 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 17701 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 17249 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 17249 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 17247 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 17247 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 132173 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 132173 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 195412 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 195412 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 17224 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 17224 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 17266 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 17266 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 17240 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 17240 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 17768 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 17768 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 17253 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 17253 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 17253 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 17253 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 17488 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 17488 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 17486 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 17486 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 17210 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 17210 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 17490 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 17490 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 217781 4 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 10096 28 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 10096 28 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 10096 28 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 216068 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 17259 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 17259 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 87531 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 87531 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 17462 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 17462 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 21098 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 21098 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 21098 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 17217 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 17217 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 17227 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 17227 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 218158 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 119907 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 119907 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 119897 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 119897 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 217779 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 217789 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 119906 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 119906 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 119896 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 119896 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 119904 6 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 119904 6 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 119895 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 119895 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 119909 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 119909 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 119903 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 119903 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 217786 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 217787 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 217789 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 217774 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 217786 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 216068 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 87531 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 87531 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 217779 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 217769 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 119889 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 119889 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 217791 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 217774 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 217787 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 217780 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 87531 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 87531 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 119904 6 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 119904 6 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 217769 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 119887 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 119887 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 217791 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 119895 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 119895 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 87539 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 87539 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 217778 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 217788 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 119888 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 119888 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 119906 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 119906 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 119909 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 119909 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 217781 4 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 10.6019/CHEMBL5210307
CHEMBL3086284 217781 4 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 119908 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 119908 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 87539 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 87539 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 217788 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 217793 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 119893 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 119893 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 217781 4 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 217783 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 217793 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 216068 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 217780 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 217781 4 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 119905 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 119905 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 87537 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 87537 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 87540 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 87540 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 217771 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 217777 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 217790 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 87537 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 87537 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 87540 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 87540 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 217790 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 119902 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 119902 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 217777 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 217783 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 119887 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 119887 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 217771 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 217781 4 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 217778 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 217773 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 119908 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 119908 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 217772 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 217772 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 217776 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 217782 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 119898 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 119898 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 217773 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 217775 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 217776 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 217792 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 217782 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 217792 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 217775 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 217770 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 217770 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 219013 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 119902 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 119902 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 8970 11 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 8970 11 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 8970 11 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 8970 11 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 8968 36 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 8968 36 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 8968 36 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 8968 36 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 217321 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 216203 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 8970 11 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 8970 11 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 8970 11 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 8970 11 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 216202 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 217316 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 218971 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 218978 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 218985 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 219614 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 220125 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 218989 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 218998 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 220682 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 216200 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 220432 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 216206 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 220453 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 219014 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 216201 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 219886 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 219001 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 218970 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 219181 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 218975 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 119898 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 119898 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 218969 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 18620 22 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 18620 22 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 18620 22 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 18620 22 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 220442 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 216207 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 216204 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 220600 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 8970 11 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 8970 11 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 8970 11 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 8970 11 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 220434 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 90014 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 90014 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 219937 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 219886 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 219121 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 216205 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 218976 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 218999 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 218972 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 8968 36 None 1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1283 8968 36 None 1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
25240297 8968 36 None 1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL376756 8968 36 None 1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
2335 18620 22 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 18620 22 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 18620 22 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 18620 22 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 8972 0 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
155817401 8972 0 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1289 8977 0 None - 1 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
155817403 8977 0 None - 1 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
101134421 8970 11 None -6 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1284 8970 11 None -6 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL220853 8970 11 None -6 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL373467 8970 11 None -6 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
101134421 8970 11 None 6 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1284 8970 11 None 6 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL220853 8970 11 None 6 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL373467 8970 11 None 6 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1285 8971 0 None -1 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1288 8976 0 None -2 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1281 8968 36 None -1 2 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1283 8968 36 None -1 2 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
25240297 8968 36 None -1 2 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL376756 8968 36 None -1 2 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1285 8971 0 None 1 2 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1288 8976 0 None 2 2 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1288 8976 0 None 2 2 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1281 8968 36 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1281 8968 36 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1283 8968 36 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1283 8968 36 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
25240297 8968 36 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
25240297 8968 36 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL376756 8968 36 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
CHEMBL376756 8968 36 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843