LG190178 [Ligand Id: 2787] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL197589 (LG-190178)
  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
  • Androgen receptor/Androgen Receptor in Mouse [ChEMBL: CHEMBL3056] [GtoPdb: 628] [UniProtKB: P19091]
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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 human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity by luciferase and beta-galactosidase reporter gene assay B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2013) 21: 1643-1651 [PMID:23462715]
Androgen receptor/Androgen Receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3056] [GtoPdb: 628] [UniProtKB: P19091]
ChEMBL Androgen antagonistic activity as inhibitory concentration against testosterone-induced SC-3 cell proliferation F 7.72 pIC50 19 nM IC50 Bioorg Med Chem Lett (2005) 15: 4327-4331 [PMID:16019211]
Vitamin D receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1977] [GtoPdb: 605] [UniProtKB: P11473]
GtoPdb - - 6.82 pKi - - - Chem Biol (1999) 6: 265-75 [PMID:10322128]
ChEMBL Agonist activity at VDR (unknown origin) by reporter gene assay B 7.4 pEC50 40 nM EC50 Bioorg Med Chem (2013) 21: 1643-1651 [PMID:23462715]
Vitamin D receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5601] [UniProtKB: P48281]
ChEMBL Activation of VDR in mouse ASZ001 cells assessed as change in Cyp24A1 mRNA expression after 48 hrs by q-PCR analysis B 8.11 pEC50 7.7 nM EC50 Eur J Med Chem (2019) 162: 495-506 [PMID:30471551]

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]