T-226296 [Ligand Id: 1314] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL178707 (T-226296)
  • MCH1 receptor/Melanin-concentrating hormone receptor 1 in Human [ChEMBL: CHEMBL344] [GtoPdb: 280] [UniProtKB: Q99705]
  • MCH1 receptor/Melanin-concentrating hormone receptor 1 in Rat [ChEMBL: CHEMBL1075228] [GtoPdb: 280] [UniProtKB: P97639]
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1 CHEMBL178707_lig_chart_1 Melanin-concentrating hormone receptor 1 HumanRat
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
MCH1 receptor/Melanin-concentrating hormone receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL344] [GtoPdb: 280] [UniProtKB: Q99705]
ChEMBL Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells B 7.42 pKi 38 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 3754-3759 [PMID:17448659]
ChEMBL Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells B 8.26 pKi 5.5 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 999-1004 [PMID:15686900]
ChEMBL Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader F 6.06 pIC50 872 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 4879-4882 [PMID:15341943]
ChEMBL Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes B 7.07 pIC50 85 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 4879-4882 [PMID:15341943]
ChEMBL Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting F 7.37 pIC50 43 nM IC50 Bioorg. Med. Chem. (2011) 19: 5539-5552 [PMID:21856163]
ChEMBL Antagonist activity at MCH1R by [35S]GTPgammaS binding assay F 7.72 pIC50 19 nM IC50 J. Med. Chem. (2009) 52: 2076-2089 [PMID:19290642]
ChEMBL Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting B 7.85 pIC50 14 nM IC50 Bioorg. Med. Chem. (2011) 19: 5539-5552 [PMID:21856163]
ChEMBL Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells B 8.26 pIC50 5.5 nM IC50 Bioorg. Med. Chem. (2011) 19: 6261-6273 [PMID:21975069]
ChEMBL Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells B 8.26 pIC50 5.5 nM IC50 J. Med. Chem. (2004) 47: 3962-3971 [PMID:15267235]
ChEMBL Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay F 8.26 pIC50 5.5 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 6166-6171 [PMID:19773162]
ChEMBL Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay B 8.26 pIC50 5.5 nM IC50 Bioorg. Med. Chem. (2011) 19: 883-893 [PMID:21190859]
GtoPdb - - 8.3 pIC50 5.01 nM IC50 Eur J Pharmacol (2002) 438: 129-35 [PMID:11909603]
MCH1 receptor/Melanin-concentrating hormone receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075228] [GtoPdb: 280] [UniProtKB: P97639]
ChEMBL Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting B 7.62 pIC50 24 nM IC50 Bioorg. Med. Chem. (2011) 19: 5539-5552 [PMID:21856163]

ChEMBL data shown on this page come from version 28:

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]