24(S)-hydroxycholesterol [Ligand Id: 2750] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL171804 (24(S)-Hydroxychloesterol, 24(S)-Hydroxycholesterol)
1 CHEMBL171804_lig_chart_1 Glutamate NMDA receptor; GRIN1/GRIN2A HumanRat
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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
2 CHEMBL171804_lig_chart_2 Glutamate NMDA receptor; GRIN1/GRIN2B 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
3 CHEMBL171804_lig_chart_3 LXR-alpha 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 1 pki data point
  • 8
4 CHEMBL171804_lig_chart_4 Nuclear receptor ROR-gamma Human
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  • Liver X receptor-β in Human [GtoPdb: 601] [UniProtKB: P55055]
  • This target only has 0 pki data point
  • 0
5 CHEMBL171804_lig_chart_5 Liver X receptor-β Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 expressed in Xenopus laevis oocytes assessed as increase in glycine/L-glutamate-induced channel current at -80 mV holding potential by two-electrode voltage clamp method B 6.52 pEC50 300 nM EC50 J Med Chem (2019) 62: 7526-7542 [PMID:31390523]
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 6.82 pEC50 150 nM EC50 J Med Chem (2019) 62: 7526-7542 [PMID:31390523]
GluN1/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096680] [GtoPdb: 455456] [UniProtKB: P35439Q00959]
ChEMBL Positive allosteric modulation of recombinant rat GluN1/GluN2A receptor expressed in Xenopus laevis oocytes assessed as increase in glycine/L-glutamate-induced channel current at -80 mV holding potential by two-electrode voltage clamp method B 6.19 pEC50 650 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 6.28 pEC50 530 nM EC50 J Med Chem (2019) 62: 7526-7542 [PMID:31390523]
Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
GtoPdb - - 5.4 pEC50 - - - J Biol Chem (1997) 272: 3137-40 [PMID:9013544]
ChEMBL Concentration required for half maximal activity was calculated in human nuclear oxysterol receptor liver X receptor-alpha in LiSA. B 6.89 pEC50 130 nM EC50 J. Med. Chem. (2001) 44: 886-897 [PMID:11300870]
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
Liver X receptor-β in Human [GtoPdb: 601] [UniProtKB: P55055]
GtoPdb - - 5.5 pEC50 - - - J Biol Chem (1997) 272: 3137-40 [PMID:9013544]

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]