25-hydroxycholesterol [Ligand Id: 2885] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL169046 (25-Hydroxycholesterol)
  • Alpha-crystallin B chain in Human [ChEMBL: CHEMBL3621022] [UniProtKB: P02511]
  • This target only has 0 pki data point
  • 0
1 CHEMBL169046_lig_chart_1 Alpha-crystallin B chain Human
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  • GluN1/GluN2A/Glutamate NMDA receptor; GRIN1/GRIN2A in Human [ChEMBL: CHEMBL1907604] [GtoPdb: 455456] [UniProtKB: Q05586Q12879]
  • This target only has 0 pki data point
  • 0
2 CHEMBL169046_lig_chart_2 Glutamate NMDA receptor; GRIN1/GRIN2A Human
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  • GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human [ChEMBL: CHEMBL1907603] [GtoPdb: 455457] [UniProtKB: Q05586Q13224]
  • This target only has 0 pki data point
  • 0
3 CHEMBL169046_lig_chart_3 Glutamate NMDA receptor; GRIN1/GRIN2B Human
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  • hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035]
  • This target only has 0 pki data point
  • 0
4 CHEMBL169046_lig_chart_4 HMG-CoA reductase Human
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  • Liver X receptor-α/LXR-alpha in Human [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
  • This target only has 0 pki data point
  • 0
5 CHEMBL169046_lig_chart_5 LXR-alpha Human
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  • NPC1 like intracellular cholesterol transporter 1/Niemann-Pick C1-like protein 1 in Human [ChEMBL: CHEMBL2027] [GtoPdb: 2629] [UniProtKB: Q9UHC9]
  • This target only has 0 pki data point
  • 0
6 CHEMBL169046_lig_chart_6 Niemann-Pick C1-like protein 1 Human
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  • RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
  • This target only has 0 pki data point
  • 0
7 CHEMBL169046_lig_chart_7 Nuclear receptor ROR-gamma Human
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  • Sterol regulatory element-binding protein 2 in Human [ChEMBL: CHEMBL1795166] [UniProtKB: Q12772]
  • This target only has 0 pki data point
  • 0
8 CHEMBL169046_lig_chart_8 Sterol regulatory element-binding protein 2 Human
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  • GPR183 in Human [GtoPdb: 81] [UniProtKB: P32249]
  • This target only has 0 pki data point
  • 0
9 CHEMBL169046_lig_chart_9 GPR183 Human
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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: 455456] [UniProtKB: Q05586Q12879]
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: 455457] [UniProtKB: Q05586Q13224]
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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]