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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 |
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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] |
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]