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ChEMBL ligand: CHEMBL178707 (T-226296) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]