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 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]
