cholesterol [Ligand Id: 2718] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL112570 (Cholest-5-en-3-ol (3.beta.)-, Cholesterin, Cholesterinum, Cholesterol, Cholestrin, Dythol, Lidinit, Lidinite, NSC-8798, Provitamin-d)
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) B 4.37 pIC50 >42657.95 nM IC50 J Med Chem (2005) 48: 5666-5674 [PMID:16134935]
CYP46A1/Cholesterol 24-hydroxylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523510] [GtoPdb: 1373] [UniProtKB: Q9Y6A2]
ChEMBL Binding affinity to full-length recombinant human CYP46A1 by spectral binding study B 6.17 pKd 670 nM Kd US-20170182047-A9. Post-Translational Regulation of Catalytic Activities of Cytochrome P450 46A1 and Uses Thereof (null)
RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
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 6.38 pEC50 418 nM EC50 ACS Med Chem Lett (2021) 12: 631-639 [PMID:33854703]
ChEMBL Agonist activity at 6xHis tagged human RORgammat LBD (262 to 507 residues) expressed in Escherichia coli BL21 (DE3) assessed as biotinylated SRC1-2 peptide coactivator recruitment by AlphaScreen assay B 7.7 pEC50 20 nM EC50 J Med Chem (2018) 61: 5794-5804 [PMID:29412659]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: increase in Daunorubicn intracellular accumulation (Daunorubicin: ? uM) in NIH-G185 cells F 5.09 pIC50 8200 nM IC50 Biochem Biophys Res Commun (2000) 276: 909-916 [PMID:11027568]

ChEMBL data shown on this page come from version 32:

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]