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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 |
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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 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]