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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 |
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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 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]