7β-hydroxycholesterol [Ligand Id: 4352] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL497834 (7Beta-Hydroxycholesterol)
  • NPC1 like intracellular cholesterol transporter 1/Niemann-Pick C1-like protein 1 in Human [ChEMBL: CHEMBL2027] [GtoPdb: 2629] [UniProtKB: Q9UHC9]
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  • RAR-related orphan receptor-α/Nuclear receptor ROR-alpha in Human [ChEMBL: CHEMBL5868] [GtoPdb: 598] [UniProtKB: P35398]
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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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  • GPR183 in Human [GtoPdb: 81] [UniProtKB: P32249]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 5.47 pEC50 3400 nM EC50 Bioorg Med Chem Lett (2014) 24: 3480-3485 [PMID:24928400]
RAR-related orphan receptor-α/Nuclear receptor ROR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5868] [GtoPdb: 598] [UniProtKB: P35398]
ChEMBL Displacement of 25-[3H]hydroxycholesterol from GST-tagged ROR alpha ligand binding domain (unknown origin) expressed in Escherichia coli BL21 gold (DE3) cells by radioligand competition assay B 7.92 pKi 12 nM Ki Medchemcomm (2013) 4: 764-776
RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
ChEMBL Displacement of 25-[3H]hydroxycholesterol from GST-tagged ROR gamma ligand binding domain (unknown origin) expressed in Escherichia coli BL21 gold (DE3) cells by radioligand competition assay B 8 pKi 10 nM Ki Medchemcomm (2013) 4: 764-776
GPR183 in Human [GtoPdb: 81] [UniProtKB: P32249]
GtoPdb - - 5.75 pEC50 1763 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]