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) |
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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 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]
