desmosterol [Ligand Id: 2748] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL455876 (24-Dehydrocholesterol, Desmosterol) |
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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 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]
