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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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 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]