ChEMBL ligand: CHEMBL376756 (Human metastin 45-54, Kisspeptin-10, Kisspeptin-10 (human))
kisspeptin receptor/Metastin receptor in Human [ChEMBL: CHEMBL5413] [GtoPdb: 266] [UniProtKB: Q969F8] kisspeptin receptor/Metastin receptor in Rat [ChEMBL: CHEMBL1169599] [GtoPdb: 266] [UniProtKB: Q924U1] There should be some charts here, you may need to enable JavaScript!
NPFF1 receptor/Neuropeptide FF receptor 1 in Human [ChEMBL: CHEMBL5951] [GtoPdb: 300] [UniProtKB: Q9GZQ6] There should be some charts here, you may need to enable JavaScript!
NPFF2 receptor/Neuropeptide FF receptor 2 in Human [ChEMBL: CHEMBL5952] [GtoPdb: 301] [UniProtKB: Q9Y5X5] There should be some charts here, you may need to enable JavaScript!

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]
ChEMBL	Displacement of [125I]-Kp-10 from human Kiss1 receptor by TopCount scintillation counting method	B	10.21	pKi	0.06	nM	Ki	J Med Chem (2021) 64: 7555-7564 [PMID:34008968]
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 expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay	F	9.02	pEC50	0.96	nM	EC50	J Med Chem (2016) 59: 8804-8811 [PMID:27589480]
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 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 KISS1R expressed 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	F	10.06	pEC50	0.09	nM	EC50	Bioorg Med Chem Lett (2019) 29: 654-658 [PMID:30598349]
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	F	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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]