desmosterol [Ligand Id: 2748] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL455876 (24-Dehydrocholesterol, Desmosterol)
  • RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
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  • Liver X receptor-β in Human [GtoPdb: 601] [UniProtKB: P55055]
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  • Liver X receptor-α in Human [GtoPdb: 602] [UniProtKB: Q13133]
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  • Farnesoid X receptor-β in Mouse [GtoPdb: 604]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
ChEMBL Agonist activity at Gal4-fused RORgammat DNA binding domain (unknown origin) expressed in 293T cells assessed as SRC1 coactivator recruitment in presence of ursolic acid by TR-FRET assay B 7.1 pEC50 80 nM EC50 J Med Chem (2018) 61: 5794-5804 [PMID:29412659]
ChEMBL Orthosteric agonist activity at recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as increase in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment incubated for 60 mins by TR-FRET assay B 7.32 pEC50 48 nM EC50 ACS Med Chem Lett (2021) 12: 631-639 [PMID:33854703]
Liver X receptor-β in Human [GtoPdb: 601] [UniProtKB: P55055]
GtoPdb - - 5.85 pKi 1400 nM Ki J Biol Chem (2006) 281: 27816-26 [PMID:16857673]
Liver X receptor-α in Human [GtoPdb: 602] [UniProtKB: Q13133]
GtoPdb - - 5.54 pKi 2900 nM Ki J Biol Chem (2006) 281: 27816-26 [PMID:16857673]
Farnesoid X receptor-β in Mouse [GtoPdb: 604]
GtoPdb - - 5 pEC50 - - - Mol Cell Biol (2003) 23: 864-72 [PMID:12529392]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]