25-hydroxycholesterol [Ligand Id: 2885] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL169046 (25-Hydroxycholesterol) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Alpha-crystallin B chain in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3621022] [UniProtKB: P02511] | ||||||||
| ChEMBL | Inhibition of alpha-crystallin B R120G mutant (unknown origin)-induced intracellular protein aggregation expressed in human HeLa cells or HLE-B3 cells incubated for 6 to 8 hrs by fluorescence microscopy relative to untreated control | B | 6.49 | pEC50 | 320 | nM | EC50 | J Med Chem (2018) 61: 8693-8706 [PMID:30153006] |
| GluN1/GluN2A/Glutamate NMDA receptor; GRIN1/GRIN2A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907604] [GtoPdb: 455, 456] [UniProtKB: Q05586, Q12879] | ||||||||
| ChEMBL | Positive allosteric modulation of recombinant human GluN1/GluN2A receptor stably expressed in HEK293 cells assessed as increase in glycine/L-glutamate-induced channel current at -70 mV holding potential by IonWork two-electrode voltage clamp method | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2019) 62: 7526-7542 [PMID:31390523] |
| GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907603] [GtoPdb: 455, 457] [UniProtKB: Q05586, Q13224] | ||||||||
| ChEMBL | Positive allosteric modulation of recombinant human GluN1/GluN2B receptor stably expressed in HEK293 cells assessed as increase in glycine/L-glutamate-induced channel current at -70 mV holding potential by IonWork two-electrode voltage clamp method | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2019) 62: 7526-7542 [PMID:31390523] |
| hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035] | ||||||||
| ChEMBL | Tested for its inhibitory activity against HMG-CoA reductase transcription in HepG2 cells | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (1994) 37: 2343-2351 [PMID:8057282] |
| ChEMBL | Induction of human HMGCR-dCat-ELuc degradation expressed in HEK293 cells assessed as reduction in luciferase activity after 4 hrs by luciferase reporter assay | B | 6.2 | pEC50 | 630 | nM | EC50 | Bioorg Med Chem (2020) 28: 115298-115298 [PMID:31902650] |
| integrin, beta 3 subunit (platelet glycoprotein IIIa, antigen CD61)/integrin, alpha V subunit/Integrin alpha-V/beta-3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907598] [GtoPdb: 2457, 2453] [UniProtKB: P05106, P06756] | ||||||||
| ChEMBL | Binding affinity to human integrin alphavbeta3 by surface plasmon resonance method | B | 7.96 | pKd | 10.9 | nM | Kd | J Med Chem (2020) 63: 5675-5696 [PMID:31999923] |
| Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133] | ||||||||
| ChEMBL | Concentration required for half maximal activity was calculated in human nuclear oxysterol receptor liver X receptor-alpha in LiSA. | B | 5.94 | pEC50 | 1160 | nM | EC50 | J Med Chem (2001) 44: 886-897 [PMID:11300870] |
| NPC1 like intracellular cholesterol transporter 1/Niemann-Pick C1-like protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2027] [GtoPdb: 2629] [UniProtKB: Q9UHC9] | ||||||||
| ChEMBL | Binding affinity to FLAG/tGFP-tagged NPC1 I1061T mutant (unknown origin) expressed in HEK293 cells assessed as localization after 24 hrs by fluorescence microscopy | B | 5.48 | pEC50 | 3300 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 3480-3485 [PMID:24928400] |
| 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 human His6-tagged ROR gamma ligand binding domain (residues 262 to 507) expressed in Escherichia coli BL21 (DE3) cells assessed as increase in recruitment of coactivator peptide by AlphaScreen biochemical assay | B | 7.7 | pEC50 | 20 | nM | EC50 | Medchemcomm (2013) 4: 764-776 |
| ChEMBL | Displacement of [3H]25-hydroxycholesterol from human RORc-LBD expressed in bacterial expression system after 3 hrs by scintillation counting analysis | B | 7.7 | pEC50 | 20 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 5769-5776 [PMID:25453817] |
| 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] |
| ChEMBL | Activity at 6His-tagged human RORgamma LBD (262 to 507 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as induction of biotinylated SRC1 co-activator peptide recruitment by alphascreen assay | B | 7.7 | pEC50 | 20 | nM | EC50 | Bioorg Med Chem Lett (2016) 26: 4387-4393 [PMID:27542308] |
| Sterol regulatory element-binding protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795166] [UniProtKB: Q12772] | ||||||||
| ChEMBL | Inhibition of SREBP2 activation expressed in CHO-K1 cells co-transfected with pSRE-Luc plasmid assessed as inhibition of luciferase expression after 20 hrs by luciferase reporter gene assay | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2011) 54: 4923-4927 [PMID:21561152] |
| GPR183 in Human [GtoPdb: 81] [UniProtKB: P32249] | ||||||||
| GtoPdb | - | - | 6.9 | pEC50 | 127 | nM | EC50 | Nature (2011) 475: 519-23 [PMID:21796211] |
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]
