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) |
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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 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]
