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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 34:
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]