[3H]pregnenolone sulphate [Ligand Id: 6504] 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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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 (2017)
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]

ChEMBL data shown on this page come from version 35:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]