24(S), 25-epoxycholesterol [Ligand Id: 2751] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL434302 (24(S), 25-Epoxycholesterol, 24(S),25-Epoxycholesterol)
  • Liver X receptor-α/LXR-alpha in Human [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
ChEMBL Binding affinity to human LXRalpha B 4.7 pEC50 >20000 nM EC50 J. Med. Chem. (2016) 59: 3264-3271 [PMID:26990539]
ChEMBL Effective concentration in LXR alpha-Gal4 receptor gene assay B 5.52 pEC50 3000 nM EC50 J. Med. Chem. (2002) 45: 1963-1966 [PMID:11985463]
ChEMBL Activity against LXR alpha transiently transfected in HEK293 cells B 6.3 pEC50 500 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 1638-1642 [PMID:16386417]
ChEMBL Concentration required for half maximal activity was calculated in human nuclear oxysterol receptor liver X receptor-alpha in LiSA. B 6.34 pEC50 460 nM EC50 J. Med. Chem. (2001) 44: 886-897 [PMID:11300870]
GtoPdb - - 6.5 pEC50 - - - Proc Natl Acad Sci USA (1999) 96: 266-71 [PMID:9874807];
J Biol Chem (1997) 272: 3137-40 [PMID:9013544];
Nat Chem Biol (2013) 9: 126-33 [PMID:23292650]
ChEMBL Agonist activity at LXRalpha ligand binding domain by FRET based SRC1 recruitment assay B 6.55 pEC50 280 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL Agonist activity at human LXRalpha coexpressed in African green monkey CV1 cells by Gal4 responsive reporter gene assay B 6.93 pEC50 117 nM EC50 J. Med. Chem. (2016) 59: 3264-3271 [PMID:26990539]
ChEMBL Ligand-dependent recruitment of steroid receptor co-activator 1 (SRC1) to Liver X receptor-alpha B 7.02 pEC50 95 nM EC50 J. Med. Chem. (2002) 45: 1963-1966 [PMID:11985463]
Liver X receptor-β/LXR-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4093] [GtoPdb: 601] [UniProtKB: P55055]
ChEMBL Binding to human LXRbeta B 4.7 pEC50 >20000 nM EC50 J. Med. Chem. (2016) 59: 3264-3271 [PMID:26990539]
ChEMBL Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay F 6.4 pEC50 400 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL Agonist activity at LXRbeta ligand binding domain by FRET based SRC1 recruitment assay B 6.54 pEC50 286 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL Agonist activity at human LXRbeta coexpressed in African green monkey CV1 cells by Gal4 responsive reporter gene assay B 6.77 pEC50 168 nM EC50 J. Med. Chem. (2016) 59: 3264-3271 [PMID:26990539]
GtoPdb - - 7.04 pEC50 - - - J Biol Chem (1997) 272: 3137-40 [PMID:9013544];
Nat Chem Biol (2013) 9: 126-33 [PMID:23292650]

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]