kisspeptin-10 [Ligand Id: 1283] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL376756 (Kisspeptin-10)
  • kisspeptin receptor/Metastin receptor in Human [ChEMBL: CHEMBL5413] [GtoPdb: 266] [UniProtKB: Q969F8]
  • kisspeptin receptor/Metastin receptor in Rat [ChEMBL: CHEMBL1169599] [GtoPdb: 266] [UniProtKB: Q924U1]
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  • NPFF1 receptor/Neuropeptide FF receptor 1 in Human [ChEMBL: CHEMBL5951] [GtoPdb: 300] [UniProtKB: Q9GZQ6]
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  • NPFF2 receptor/Neuropeptide FF receptor 2 in Human [ChEMBL: CHEMBL5952] [GtoPdb: 301] [UniProtKB: Q9Y5X5]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
kisspeptin receptor/Metastin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5413] [GtoPdb: 266] [UniProtKB: Q969F8]
ChEMBL Displacement of [125]metastin from metastin receptor B 8.89 pKi 1.3 nM Ki J. Med. Chem. (2007) 50: 462-471 [PMID:17266198]
GtoPdb - - 10.4 pKi - - - Nature (2001) 411: 613-7 [PMID:11385580];
J. Biol. Chem. (2001) 276: 34631-6 [PMID:11457843]
ChEMBL Binding affinity to human KISS1R expressed in CHO cell membranes B 10.41 pKi 0.04 nM Ki J. Med. Chem. (2013) 56: 8298-8307 [PMID:24047141]
ChEMBL Displacement of radioligand from human KISS1R transfected in CHO cells B 10.46 pKi 0.04 nM Ki J. Med. Chem. (2014) 57: 6105-6115 [PMID:24918545]
ChEMBL Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay B 5.07 pIC50 8510 nM IC50 J. Med. Chem. (2013) 56: 8298-8307 [PMID:24047141]
ChEMBL Displacement of [125I]kisspeptin-15 from GPR54 B 9.92 pIC50 0.12 nM IC50 ACS Med. Chem. Lett. (2011) 2: 53-57 [PMID:24900254]
ChEMBL Binding affinity to human KISS1R B 10.09 pIC50 0.08 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 6391-6396 [PMID:22975302]
ChEMBL Displacement of [125I]kisspeptin-15 from human GPR54 expressed in CHO cell membrane B 10.15 pIC50 0.07 nM IC50 J. Med. Chem. (2008) 51: 7645-7649 [PMID:19007202]
ChEMBL Activity at metastin receptor expressed in HEK293 cells by measuring calcium release F 7.76 pEC50 17.3 nM EC50 J. Med. Chem. (2007) 50: 462-471 [PMID:17266198]
ChEMBL Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay F 9.02 pEC50 0.96 nM EC50 J. Med. Chem. (2014) 57: 6105-6115 [PMID:24918545]
ChEMBL 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 assay B 9.02 pEC50 0.96 nM EC50 J Med Chem (2016) 59: 8804-8811 [PMID:27589480]
ChEMBL Agonist activity at human GPR54 expressed in CHO cells assessed as effect on kisspeptin-10-induced response by FLIPR assay F 9.62 pEC50 0.24 nM EC50 J. Med. Chem. (2008) 51: 7645-7649 [PMID:19007202]
ChEMBL Agonist activity at human OT7T175 assessed as increase in intracellular calcium level by FLIPR assay F 10.19 pEC50 0.07 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 6328-6332 [PMID:22995619]
ChEMBL Agonist activity at human KISS1R assessed as induction of intracellular calcium mobilization by fluorometric analysis F 10.31 pEC50 0.05 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 6391-6396 [PMID:22975302]
kisspeptin receptor/Metastin receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1169599] [GtoPdb: 266] [UniProtKB: Q924U1]
GtoPdb - - 8.8 pKi - - - J. Biol. Chem. (2001) 276: 34631-6 [PMID:11457843]
ChEMBL Displacement of radioligand from rat KISS1R transfected in CHO cells B 10.06 pKi 0.09 nM Ki J. Med. Chem. (2014) 57: 6105-6115 [PMID:24918545]
ChEMBL Binding affinity to rat KISS1R B 10.24 pKi 0.06 nM Ki J. Med. Chem. (2013) 56: 8298-8307 [PMID:24047141]
ChEMBL Binding affinity to rat KISS1R B 9.96 pIC50 0.11 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 6391-6396 [PMID:22975302]
ChEMBL Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay F 8.38 pEC50 4.2 nM EC50 J. Med. Chem. (2014) 57: 6105-6115 [PMID:24918545]
ChEMBL 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 assay B 8.38 pEC50 4.2 nM EC50 J Med Chem (2016) 59: 8804-8811 [PMID:27589480]
NPFF1 receptor/Neuropeptide FF receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5951] [GtoPdb: 300] [UniProtKB: Q9GZQ6]
ChEMBL Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrs B 8.33 pIC50 4.7 nM IC50 ACS Med. Chem. Lett. (2011) 2: 53-57 [PMID:24900254]
NPFF2 receptor/Neuropeptide FF receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5952] [GtoPdb: 301] [UniProtKB: Q9Y5X5]
ChEMBL Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrs B 7.12 pIC50 76 nM IC50 ACS Med. Chem. Lett. (2011) 2: 53-57 [PMID:24900254]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]