pregnenolone sulphate [Ligand Id: 4290] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1179605
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  • GluN2A/Glutamate [NMDA] receptor subunit epsilon 1 in Human [ChEMBL: CHEMBL1972] [GtoPdb: 456] [UniProtKB: Q12879]
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  • GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Human [ChEMBL: CHEMBL1904] [GtoPdb: 457] [UniProtKB: Q13224]
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  • GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Human [ChEMBL: CHEMBL4109] [GtoPdb: 458] [UniProtKB: Q14957]
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  • GluN2D/Glutamate [NMDA] receptor subunit epsilon 4 in Human [ChEMBL: CHEMBL2591] [GtoPdb: 459] [UniProtKB: O15399]
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  • glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415]
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  • glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416]
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  • glycine receptor β subunit in Human [GtoPdb: 427] [UniProtKB: P48167]
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  • TRPM3 in Human [GtoPdb: 495] [UniProtKB: Q9HCF6]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CYP46A1/Cholesterol 24-hydroxylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523510] [GtoPdb: 1373] [UniProtKB: Q9Y6A2]
ChEMBL Inhibition of full-length recombinant human CYP46A1 assessed as cholesterol hydroxylation using cholesterol as substrate in presence of NADPH cytochrome P450 oxidoreductase by gas chromatography-mass spectrometry B 5.6 pKi 2500 nM Ki US-20170182047-A9. Post-Translational Regulation of Catalytic Activities of Cytochrome P450 46A1 and Uses Thereof (null)
GluN2A/Glutamate [NMDA] receptor subunit epsilon 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1972] [GtoPdb: 456] [UniProtKB: Q12879]
ChEMBL Positive allosteric modulation of EGFP-fused human GluN2A receptor expressed in HEK293T cells assessed as increase in glycine-induced channel current by two electrode voltage clamp method B 4.47 pEC50 34000 nM EC50 J Med Chem (2018) 62: 3-23 [PMID:29446949]
ChEMBL Positive allosteric modulation of GluN2A receptor (unknown origin) expressed in xenopus laevis oocytes assessed as increase in glycine-induced channel current by two electrode voltage clamp method B 4.68 pEC50 21000 nM EC50 J Med Chem (2018) 62: 3-23 [PMID:29446949]
GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1904] [GtoPdb: 457] [UniProtKB: Q13224]
ChEMBL Positive allosteric modulation of EGFP-fused human GluN2B receptor expressed in HEK293T cells assessed as increase in glycine-induced channel current by two electrode voltage clamp method B 4.2 pEC50 63000 nM EC50 J Med Chem (2018) 62: 3-23 [PMID:29446949]
ChEMBL Positive allosteric modulation of GluN2B receptor (unknown origin) expressed in xenopus laevis oocytes assessed as increase in glycine-induced channel current by two electrode voltage clamp method B 4.48 pEC50 33000 nM EC50 J Med Chem (2018) 62: 3-23 [PMID:29446949]
GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4109] [GtoPdb: 458] [UniProtKB: Q14957]
ChEMBL Positive allosteric modulation of EGFP-fused human GluN2C receptor expressed in HEK293T cells assessed as increase in glycine-induced channel current by two electrode voltage clamp method B 4.08 pEC50 83000 nM EC50 J Med Chem (2018) 62: 3-23 [PMID:29446949]
GluN2D/Glutamate [NMDA] receptor subunit epsilon 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2591] [GtoPdb: 459] [UniProtKB: O15399]
ChEMBL Positive allosteric modulation of EGFP-fused human GluN2D receptor expressed in HEK293T cells assessed as increase in glycine-induced channel current by two electrode voltage clamp method B 4.11 pEC50 78000 nM EC50 J Med Chem (2018) 62: 3-23 [PMID:29446949]
glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415]
GtoPdb - - 5.7 pKi 1900 nM Ki
glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416]
GtoPdb - - 5.3 pKi 5500 nM Ki
glycine receptor β subunit in Human [GtoPdb: 427] [UniProtKB: P48167]
GtoPdb - - 5 pKi 10100 nM Ki
GtoPdb - - 5.6 pKi 2700 nM Ki
TRPM3 in Human [GtoPdb: 495] [UniProtKB: Q9HCF6]
GtoPdb - - 4.9 pEC50 - - - Nat Cell Biol (2008) 10: 1421-30 [PMID:18978782]

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]