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

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ChEMBL ligand: CHEMBL1760248
  • MCH1 receptor/Melanin-concentrating hormone receptor 1 in Human [ChEMBL: CHEMBL344] [GtoPdb: 280] [UniProtKB: Q99705]
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  • Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
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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]
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]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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]

ChEMBL data shown on this page come from version 36:

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]