JNJ-63576253 [Ligand Id: 12709] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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] |
| ChEMBL | Antagonist activity at Androgen receptor in human LNCaP cells measured by transcriptional reporter assay | B | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (2022) 65: 8772-8797 [PMID:35786895] |
| 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 | Antagonist activity at Androgen receptor F877L mutant in human LNCaP cells measured by transcriptional reporter assay | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2022) 65: 8772-8797 [PMID:35786895] |
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]
