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ChEMBL ligand: CHEMBL1252 (R-382, R3827, R-3827, Plenaxis, PPI-149, R382, Abarelix) |
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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 28:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]