Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
155550061 173312 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 173312 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 207553 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 173015 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 173015 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 170863 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 170863 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 207558 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 172825 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 172825 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 207554 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 80341 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 80341 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 2157 27 None 1 4 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
1283 2157 27 None 1 4 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
25240297 2157 27 None 1 4 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
CHEMBL376756 2157 27 None 1 4 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysisAgonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
71461938 80344 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 80344 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 209249 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 170072 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 170072 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 207544 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 2157 27 None 1 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2012.08.087
1283 2157 27 None 1 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2012.08.087
25240297 2157 27 None 1 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2012.08.087
CHEMBL376756 2157 27 None 1 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2012.08.087
CHEMBL2152058 207556 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 173379 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 173379 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 118368 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 118368 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 209919 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 80352 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 80352 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 149346 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 149346 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 209922 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 2157 27 None 1 4 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2018.12.016
1283 2157 27 None 1 4 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2018.12.016
25240297 2157 27 None 1 4 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2018.12.016
CHEMBL376756 2157 27 None 1 4 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None None 10.1016/j.bmcl.2018.12.016
71460220 80351 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 80351 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 80348 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 80348 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 209921 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 80350 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 80350 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 171577 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 171577 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 175236 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 175236 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 80347 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 80347 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 170653 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 170653 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 174299 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 174299 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 207559 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 207560 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 173169 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 173169 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 169239 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 169239 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 171417 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 171417 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 2157 27 None 1 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL None None None None 10.1021/jm800930w
1283 2157 27 None 1 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL None None None None 10.1021/jm800930w
25240297 2157 27 None 1 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL None None None None 10.1021/jm800930w
CHEMBL376756 2157 27 None 1 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assayAgonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay
ChEMBL None None None None 10.1021/jm800930w
71449398 80346 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 80346 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 80349 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 80349 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 173238 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 173238 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 171253 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 171253 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 209256 2 None -1 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
CHEMBL2152052 207550 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 207552 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.08.087
25138123 178668 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 178668 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 112627 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 112627 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 112621 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 112621 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 207555 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 174025 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 174025 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 112628 3 None 3 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3314224 112628 3 None 3 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
49787129 112628 3 None 3 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314224 112628 3 None 3 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL2152064 207562 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 207561 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 173298 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 173298 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 207557 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 149354 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 149354 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 112631 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 112631 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 209633 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 141802 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 141802 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 152688 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 152688 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 144566 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 144566 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 151186 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 151186 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 112624 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 112624 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 112619 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 112619 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 145823 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 145823 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 80353 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 80353 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 112616 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 112616 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 171823 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 171823 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 118369 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 118369 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 153577 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 153577 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 80342 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 80342 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 170893 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 170893 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 112625 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 112625 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 112626 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 112626 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 146709 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 146709 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 141802 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 141802 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 112622 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 112622 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 80345 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 80345 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 151582 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 151582 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 112632 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 112632 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 96777 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 96777 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 112629 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 112629 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 112630 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 112630 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 112611 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 112611 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 169753 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 169753 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 209920 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 112633 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 112633 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 80343 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 80343 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 2157 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
1283 2157 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
25240297 2157 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
CHEMBL376756 2157 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
1281 2157 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
1283 2157 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
25240297 2157 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
CHEMBL376756 2157 27 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
16737378 85047 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 85047 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 168590 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 168590 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 141563 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 141563 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 112620 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 112620 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 148084 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 148084 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 112627 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 112627 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 84384 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 84384 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 85013 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 85013 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 145039 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 145039 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 151696 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 151696 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 112617 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 112617 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 149346 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 149346 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 141801 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 141801 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 112623 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 112623 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 112628 3 None -3 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
CHEMBL3314224 112628 3 None -3 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.6b00379
49787129 112628 3 None -3 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314224 112628 3 None -3 2 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3315315 209633 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 85390 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 85390 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 171544 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 171544 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 146933 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 146933 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 207546 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 207564 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 172444 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 172444 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 112615 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 112615 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 207547 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 85026 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 85026 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 150228 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 150228 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 112612 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 112612 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 118382 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 118382 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 85074 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 85074 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 96786 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 96786 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 96787 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 96787 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 112631 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 112631 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 152673 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 152673 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 112613 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 112613 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 146709 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 146709 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 150400 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 150400 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 151492 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 151492 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 207565 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 209256 2 None 1 2 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL221141 207678 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 208792 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 210445 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 210459 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 211088 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 211598 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 210463 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 210450 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 2158 10 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
1284 2158 10 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2158 10 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2158 10 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL386958 210655 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 150488 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 150488 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 153595 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 153595 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 207679 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 211915 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 212073 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 151382 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 151382 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 112614 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 112614 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 152537 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 152537 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 112613 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 112613 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 118370 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 118370 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 112617 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 112617 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 112625 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 112625 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 209925 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 173133 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 173133 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 147133 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 147133 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 143730 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 143730 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 151492 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 151492 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 142510 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 142510 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 151244 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 151244 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 2157 27 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
1283 2157 27 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
25240297 2157 27 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL376756 2157 27 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220855 207677 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 144909 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 144909 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 118379 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 118379 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 85028 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 85028 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 152537 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 152537 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 142768 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 142768 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 173711 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 173711 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 207566 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 112621 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 112621 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 147133 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 147133 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 150175 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 150175 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 112619 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 112619 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 151244 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 151244 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 169738 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 169738 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 209918 16 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assayAgonist activity at human wild-type KISS1R expressed in HEK293 cells assessed as induction of intracellular Ca2+ mobilization after 30 mins by Fluo4 NW Ca2+ assay
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm5019675
CHEMBL3086284 209256 2 None -1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
16735781 85392 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 85392 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 143730 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 143730 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 142510 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 142510 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 150488 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 150488 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 112618 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 112618 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 145823 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 145823 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 112626 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 112626 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 118380 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 118380 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 150250 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 150250 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 152688 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 152688 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 207683 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 207681 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 210449 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 118383 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 118383 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 153470 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 153470 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 112615 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 112615 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 207680 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 2158 10 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
1284 2158 10 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2158 10 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2158 10 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
57653056 150175 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 150175 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 118381 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 118381 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 211907 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 207676 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 210488 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 210487 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 210446 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 212155 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 141527 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 141527 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 142508 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 142508 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 161326 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 161326 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 85027 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 85027 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 136434 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 136434 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 85391 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 85391 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 141498 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 141498 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 153595 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 153595 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 144909 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 144909 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 112629 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 112629 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 207563 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 112633 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 112633 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 210475 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 112623 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 112623 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 2158 10 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
1284 2158 10 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2158 10 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2158 10 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at metastin receptor expressed in HEK293 cells by measuring calcium releaseActivity at metastin receptor expressed in HEK293 cells by measuring calcium release
ChEMBL None None None None 10.1021/jm0609824
CHEMBL262577 208797 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 210444 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 3683 6 None -6 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
46700761 3683 6 None -6 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
CHEMBL3924151 3683 6 None -6 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
DB11975 3683 6 None -6 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
CHEMBL221816 207682 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 210443 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 211359 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 112620 0 None -4 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 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 112620 0 None -4 2 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL 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 112632 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 112632 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 2157 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
1283 2157 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
25240297 2157 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
CHEMBL376756 2157 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b00379
1281 2157 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
1283 2157 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
25240297 2157 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
CHEMBL376756 2157 27 None -1 4 Rat 8.4 pEC50 = 8.4 Functional
Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assayAgonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
ChEMBL None None None None 10.1021/jm5005489
118707494 112630 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 112630 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 188048 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 188048 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 149193 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 149193 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 112614 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 112614 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 141531 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 141531 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 150400 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 150400 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 146933 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 146933 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 153577 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 153577 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 150250 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 150250 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 153470 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 153470 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 149193 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 149193 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 153307 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 153307 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 142703 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 142703 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 211359 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 148020 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 148020 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 96788 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 96788 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 3683 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
46700761 3683 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
CHEMBL3924151 3683 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
DB11975 3683 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assayAgonist activity at human KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
ChEMBL None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 10.1021/acs.jmedchem.6b00379
24995519 142703 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 142703 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 148020 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 148020 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 187766 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 187766 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 153307 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 153307 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 112612 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 112612 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 151382 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 151382 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 207548 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 145039 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 145039 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 112611 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 112611 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 150228 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 150228 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 112624 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 112624 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 210452 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 210473 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 151186 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 151186 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 151696 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 151696 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 149354 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 149354 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 207549 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 209926 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 152673 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 152673 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 148084 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 148084 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 112616 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 112616 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 171379 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 171379 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 211905 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 207551 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 211410 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 174274 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 174274 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 151582 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 151582 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 211926 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 210595 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 144566 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 144566 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 112622 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 112622 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 210472 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 112618 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 112618 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 10370 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 10370 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 10374 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 10374 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 10353 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 10353 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 10388 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 10388 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 10394 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 10394 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 10381 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 10381 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 10346 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 10346 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 10343 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 10343 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 10376 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 10376 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 10347 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 10347 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 10339 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 10339 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 209256 2 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Affinity Phenotypic Cellular interaction (Cell proliferation assay (cell growth inhibition in CHO/h175 cells)) EUB0000349a KISS1RAffinity Phenotypic Cellular interaction (Cell proliferation assay (cell growth inhibition in CHO/h175 cells)) EUB0000349a KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O nan
136016389 10345 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 10345 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 10893 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 10893 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 3683 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 27589480
46700761 3683 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 27589480
CHEMBL3924151 3683 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 27589480
DB11975 3683 6 None 6 2 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None CN=C(NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1c[nH]c2c1cccc2)NC(=O)[C@@H](NC(=O)NNC(=O)[C@@H](NC(=O)[C@H]([C@H](O)C)NC(=O)[C@@H](NC(=O)[C@@H]1C[C@H](CN1C(=O)[C@@H](Cc1ccc(cc1)O)NC(=O)C)O)CC(=O)N)Cc1ccccc1)CC(C)C)N 27589480
1287 2161 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
155817402 2161 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
4014 117 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18302161
4015 1492 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19934405


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
CHEMBL3086284 209256 2 None -1 3 Rat 9.8 pEC50 = 9.8 Binding
Agonist activity at rat KISS1RAgonist activity at rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2018.12.016
155551159 173379 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 173379 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 2157 27 None 1 2 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL None None None None 10.1021/jm800930w
1283 2157 27 None 1 2 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL None None None None 10.1021/jm800930w
25240297 2157 27 None 1 2 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL None None None None 10.1021/jm800930w
CHEMBL376756 2157 27 None 1 2 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membraneDisplacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane
ChEMBL None None None None 10.1021/jm800930w
1281 2157 27 None 1 2 Human 10.1 pIC50 = 10.1 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
1283 2157 27 None 1 2 Human 10.1 pIC50 = 10.1 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
25240297 2157 27 None 1 2 Human 10.1 pIC50 = 10.1 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
CHEMBL376756 2157 27 None 1 2 Human 10.1 pIC50 = 10.1 Binding
Binding affinity to human KISS1RBinding affinity to human KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
CHEMBL2151642 207544 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 2157 27 None -1 2 Rat 10.0 pIC50 = 10.0 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
1283 2157 27 None -1 2 Rat 10.0 pIC50 = 10.0 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
25240297 2157 27 None -1 2 Rat 10.0 pIC50 = 10.0 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
CHEMBL376756 2157 27 None -1 2 Rat 10.0 pIC50 = 10.0 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1016/j.bmcl.2012.08.069
58143625 124871 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 124871 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 2157 27 None 1 2 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None None 10.1021/ml1002053
1283 2157 27 None 1 2 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None None 10.1021/ml1002053
25240297 2157 27 None 1 2 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None None 10.1021/ml1002053
CHEMBL376756 2157 27 None 1 2 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None None 10.1021/ml1002053
25138123 178668 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 178668 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 178668 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 178668 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 80351 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 80351 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 80344 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 80344 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 80344 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 80344 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 80348 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 80348 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 80352 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 80352 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 80351 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 80351 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 80352 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 80352 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 124876 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 124876 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 80348 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 80348 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 173298 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 173298 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 207544 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 80353 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 80353 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 80350 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 80350 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 80353 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 80353 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 80350 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 80350 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 80347 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 80347 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 80345 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 80345 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 80347 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 80347 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 80345 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 80345 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 80343 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 80343 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 80342 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 80342 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 80349 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 80349 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 124870 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 124870 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 141802 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 141802 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 141802 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 141802 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 80346 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 80346 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 80346 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 80346 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 80349 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 80349 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 124872 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 124872 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 169738 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 169738 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 80342 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 80342 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 10485 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 10485 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 10558 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 10558 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 10584 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 10584 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 10617 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 10617 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 10828 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 10828 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 10388 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 10388 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 10708 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 10708 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 10345 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 10345 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 10336 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 10336 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 10350 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 10350 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 10340 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 10340 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 10708 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 10708 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 10648 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 10648 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 10382 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 10382 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 10649 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 10649 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 10824 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 10824 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 10893 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 10893 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 10338 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 10338 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 10355 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 10355 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 10583 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 10583 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 10637 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 10637 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 207088 4 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None CN(C)c1cccc2c(S(=O)(=O)N3CCC[C@H]3C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)cccc12 10.1021/ml1002053
136016478 10613 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 10613 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 10612 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 10612 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 10636 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 10636 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 10876 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 10876 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 80350 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 80350 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 10479 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 10479 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 10347 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 10347 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 80341 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 80341 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 80343 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 80343 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 10884 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 10884 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 14235 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 14235 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 14235 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 10484 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 10484 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 10370 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 10370 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 10365 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 10365 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 10694 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 10694 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 188330 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 188330 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 14265 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 14265 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 14265 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 10616 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 10616 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 10618 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 10618 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 80341 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 80341 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 10893 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 10893 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 10343 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 10343 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 10343 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 10343 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 10638 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 10638 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 10680 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 10680 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 10376 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 10376 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 10337 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 10337 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 124874 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 124874 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 124876 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 124876 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 171903 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 171903 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 172183 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 172183 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 10342 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 10342 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 10389 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 10389 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 10354 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 10354 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 10374 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 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 10374 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [125I]metastin(40-54) from human GPR54 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 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 124877 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 124877 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 10617 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 10617 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 124875 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 124875 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 181418 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 181418 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 10661 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 10661 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 124873 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 124873 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 187766 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 187766 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 10484 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 10484 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 209268 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 10383 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 10383 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 124878 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 124878 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 169638 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 169638 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 10485 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 10485 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 10828 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 10828 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 10377 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 10377 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 10375 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 10375 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 124875 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 124875 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 188048 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 188048 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 10353 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 10353 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 10394 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 10394 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 10369 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 10369 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 10894 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 10894 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 10381 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 10381 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 10381 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 10381 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 10616 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 10616 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 10614 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 10614 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 10339 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 10339 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 10618 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 10618 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 209256 2 None 1 3 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
1486 3271 23 None - 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/ml1002053
53320361 3271 23 None - 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/ml1002053
CHEMBL1672380 3271 23 None - 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]kisspeptin-15 from GPR54Displacement of [125I]kisspeptin-15 from GPR54
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/ml1002053
1281 2157 27 None 1 2 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None None 10.1021/jm401056w
1283 2157 27 None 1 2 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None None 10.1021/jm401056w
25240297 2157 27 None 1 2 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None None 10.1021/jm401056w
CHEMBL376756 2157 27 None 1 2 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assayInhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay
ChEMBL None None None None 10.1021/jm401056w
CHEMBL2151642 207544 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 10387 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 10387 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 80344 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 80344 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 10590 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 10590 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 14211 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 14211 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 14211 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 10346 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 10346 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 10356 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 10356 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 209633 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 112631 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 112631 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 112621 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 112621 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 209254 0 None 1 2 Human 10.5 pKi = 10.5 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087927 209264 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 112630 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 112630 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 2157 27 None 1 2 Human 10.5 pKi = 10.5 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
1283 2157 27 None 1 2 Human 10.5 pKi = 10.5 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
25240297 2157 27 None 1 2 Human 10.5 pKi = 10.5 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
CHEMBL376756 2157 27 None 1 2 Human 10.5 pKi = 10.5 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
118707485 112620 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 112620 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 112628 3 None 1 2 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314224 112628 3 None 1 2 Human 10.4 pKi = 10.4 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
118707484 112619 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 112619 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 112633 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 112633 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 2157 27 None 1 2 Human 10.4 pKi = 10.4 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None None 10.1021/jm401056w
1283 2157 27 None 1 2 Human 10.4 pKi = 10.4 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None None 10.1021/jm401056w
25240297 2157 27 None 1 2 Human 10.4 pKi = 10.4 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None None 10.1021/jm401056w
CHEMBL376756 2157 27 None 1 2 Human 10.4 pKi = 10.4 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None None 10.1021/jm401056w
118707492 112627 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 112627 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 209261 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 209262 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 209264 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 209249 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 209261 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 207544 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 80344 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 80344 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 209254 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 209244 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 112613 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 112613 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 209266 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 2157 27 None -1 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1021/jm401056w
1283 2157 27 None -1 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1021/jm401056w
25240297 2157 27 None -1 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1021/jm401056w
CHEMBL376756 2157 27 None -1 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None None 10.1021/jm401056w
CHEMBL3085809 209249 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 209262 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 2157 27 None 1 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting methodDisplacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
1283 2157 27 None 1 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting methodDisplacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
25240297 2157 27 None 1 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting methodDisplacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
CHEMBL376756 2157 27 None 1 2 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting methodDisplacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
CHEMBL3086283 209255 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 80344 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 80344 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 112628 3 None -1 2 Rat 10.2 pKi = 10.2 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3314224 112628 3 None -1 2 Rat 10.2 pKi = 10.2 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL 1298 33 19 14 -1.0 CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm5005489
CHEMBL3085804 209244 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 112611 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 112611 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 209266 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 112619 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 112619 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 80352 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 80352 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 209253 0 None 1 2 Human 10.1 pKi = 10.1 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087926 209263 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 112612 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 112612 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 112630 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 112630 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 112633 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 112633 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 2157 27 None -1 2 Rat 10.1 pKi = 10.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
1283 2157 27 None -1 2 Rat 10.1 pKi = 10.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
25240297 2157 27 None -1 2 Rat 10.1 pKi = 10.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
CHEMBL376756 2157 27 None -1 2 Rat 10.1 pKi = 10.1 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None None 10.1021/jm5005489
CHEMBL3086284 209256 2 None 1 3 Human 10.1 pKi = 10.1 Binding
Affinity Biochemical interaction (Binding assay (used membrane fraction of human KISS1R-expressing cells)) EUB0000349a KISS1RAffinity Biochemical interaction (Binding assay (used membrane fraction of human KISS1R-expressing cells)) EUB0000349a KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O nan
CHEMBL3086284 209256 2 None 1 3 Human 10.1 pKi = 10.1 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
118707496 112632 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 112632 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 80352 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 80352 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 209263 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 209268 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 112617 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 112617 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 209256 2 None -1 3 Rat 10.0 pKi = 10 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3086286 209258 0 None 1 2 Human 10.0 pKi = 10.0 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087931 209268 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 207544 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 209255 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 209256 2 None 1 3 Human 10.0 pKi = 10.0 Binding
Displacement of radioligand from human KISS1R transfected in CHO cellsDisplacement of radioligand from human KISS1R transfected in CHO cells
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
118707493 112629 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 112629 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 80350 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 80350 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 80353 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 80353 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 209246 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 209252 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 209265 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 80350 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 80350 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 80353 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 80353 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 209265 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 112626 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 112626 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 209252 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 209258 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 112611 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 112611 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 209246 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 209256 2 None -1 3 Rat 9.9 pKi = 9.9 Binding
Displacement of radioligand from rat KISS1R transfected in CHO cellsDisplacement of radioligand from rat KISS1R transfected in CHO cells
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm5005489
CHEMBL3086281 209253 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 209248 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 112632 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 112632 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 209247 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 209247 0 None -1 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human KISS1R expressed in CHO cell membranesBinding affinity to human KISS1R expressed in CHO cell membranes
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3085811 209251 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 209257 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 112622 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 112622 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 209248 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 209250 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 209251 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 209267 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 209257 0 None -1 2 Rat 9.6 pKi = 9.6 Binding
Binding affinity to rat KISS1RBinding affinity to rat KISS1R
ChEMBL None None None CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm401056w
CHEMBL3087930 209267 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 209250 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 209245 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 209245 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 210487 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 112626 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 112626 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 2158 10 None -6 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1284 2158 10 None -6 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2158 10 None -6 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2158 10 None -6 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1281 2157 27 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1283 2157 27 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
25240297 2157 27 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL376756 2157 27 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL262577 208797 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 207679 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 2158 10 None -6 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1284 2158 10 None -6 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2158 10 None -6 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2158 10 None -6 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL221141 207678 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 208792 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 210445 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 210452 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 210459 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 211088 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 211598 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 210463 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 210472 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 212155 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 207676 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 211905 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 207682 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 211926 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 210488 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 207677 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 211359 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 210475 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 210444 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 210655 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 210449 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 112622 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 112622 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 210443 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 11743 21 None -8 12 Human 5.4 pKi = 5.4 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1021/jm0609824
8478 11743 21 None -8 12 Human 5.4 pKi = 5.4 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1021/jm0609824
CHEMBL1182210 11743 21 None -8 12 Human 5.4 pKi = 5.4 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1021/jm0609824
CHEMBL221753 11743 21 None -8 12 Human 5.4 pKi = 5.4 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1021/jm0609824
CHEMBL435315 211915 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 207683 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 207680 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 212073 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 2158 10 None -6 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
1284 2158 10 None -6 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL220853 2158 10 None -6 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL373467 2158 10 None -6 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
ChEMBL None None None None 10.1021/jm0609824
CHEMBL434382 211907 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 82826 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 82826 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 211410 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 211359 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 210595 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 207681 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 210450 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 210473 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 210446 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 2157 27 None 1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1283 2157 27 None 1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
25240297 2157 27 None 1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL376756 2157 27 None 1 2 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
2335 11743 21 None -8 12 Human 8.3 pKi = 8.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
8478 11743 21 None -8 12 Human 8.3 pKi = 8.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
CHEMBL1182210 11743 21 None -8 12 Human 8.3 pKi = 8.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
CHEMBL221753 11743 21 None -8 12 Human 8.3 pKi = 8.3 Binding
Displacement of [125]metastin from metastin receptorDisplacement of [125]metastin from metastin receptor
Drug Central 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 None
1286 2160 0 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
155817401 2160 0 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1289 2165 0 None - 1 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
155817403 2165 0 None - 1 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
101134421 2158 10 None -6 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1284 2158 10 None -6 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL220853 2158 10 None -6 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL373467 2158 10 None -6 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
101134421 2158 10 None 6 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1284 2158 10 None 6 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL220853 2158 10 None 6 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL373467 2158 10 None 6 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1285 2159 0 None -1 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1288 2164 0 None -2 2 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1281 2157 27 None -1 2 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1283 2157 27 None -1 2 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
25240297 2157 27 None -1 2 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL376756 2157 27 None -1 2 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1285 2159 0 None 1 2 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1288 2164 0 None 2 2 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1288 2164 0 None 2 2 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1281 2157 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1281 2157 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
1283 2157 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
1283 2157 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
25240297 2157 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
25240297 2157 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843
CHEMBL376756 2157 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11385580
CHEMBL376756 2157 27 None 1 2 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11457843