pregnenolone sulphate [Ligand Id: 4290] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1179605 |
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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] |
| 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 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]
