pyrrolidine MCHR1 antagonist 1 [Ligand Id: 7756] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1760248
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  • MCH1 receptor/Melanin-concentrating hormone receptor 1 in Human [ChEMBL: CHEMBL344] [GtoPdb: 280] [UniProtKB: Q99705]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of [3H]-dofetilide from human ERG expressed in human HEK293 cells after 90 mins by scintillation counting B 5.08 pIC50 8240 nM IC50 Bioorg Med Chem Lett (2011) 21: 2460-2467 [PMID:21414780]
MCH1 receptor/Melanin-concentrating hormone receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL344] [GtoPdb: 280] [UniProtKB: Q99705]
GtoPdb - - 7.22 pIC50 60 nM IC50 Bioorg Med Chem Lett (2011) 21: 2460-7 [PMID:21414780]
ChEMBL Displacement of [125I]-MCH from MCHR1 after 2 hrs by scintillation counting B 7.24 pIC50 57 nM IC50 Bioorg Med Chem Lett (2011) 21: 2460-2467 [PMID:21414780]
ChEMBL Antagonist activity at MCHR1 by aequorin bioluminescence assay F 7.6 pIC50 25 nM IC50 Bioorg Med Chem Lett (2011) 21: 2460-2467 [PMID:21414780]

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]