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ChEMBL ligand: CHEMBL1252 (Abarelix, Plenaxis, PPI-149, R-382, R382, R-3827, R3827) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]