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ChEMBL ligand: CHEMBL4858811 (Trc 253, Trc-253, TRC253) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
ChEMBL | Antagonist activity at AR wild-type (unknown origin) transfected in human LNCAP cells cotransfected with ARE-LUC incubated for 20 to 24 hrs in presence of AR agonist R1881 by steady-glo luciferase reporter gene assay | B | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (2021) 64: 909-924 [PMID:33470111] |
GtoPdb | Antagonism in LNCaP cells with WT AR | - | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (2021) 64: 909-924 [PMID:33470111] |
GtoPdb | Antagonism in LNCaP cells with F877L mutated AR | - | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2021) 64: 909-924 [PMID:33470111] |
ChEMBL | Antagonist activity at AR F877L mutant (unknown origin) transfected in human LNCAP cells cotransfected with ARE-LUC incubated for 20 to 24 hrs in presence of AR agonist R1881 by steady-glo luciferase reporter gene assay | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2021) 64: 909-924 [PMID:33470111] |
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]