abarelix [Ligand Id: 1188] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1252 (Abarelix, Plenaxis, PPI-149, R-382, R382, R-3827, R3827)
  • GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968]
ChEMBL Competitive antagonism of GnRH-induced response in the reporter gene assay F 9.1 pKd 0.79 nM Kd J Med Chem (2001) 44: 453-467 [PMID:11462984]
GtoPdb - - 9.49 pKi 0.32 nM Ki Endocrinology (2007) 148: 857-67 [PMID:17095587]
ChEMBL Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells F 8.46 pIC50 3.5 nM IC50 J Med Chem (2001) 44: 453-467 [PMID:11462984]

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]