ChEMBL ligand: CHEMBL1179605
CYP46A1/Cholesterol 24-hydroxylase in Human [ChEMBL: CHEMBL4523510] [GtoPdb: 1373] [UniProtKB: Q9Y6A2] There should be some charts here, you may need to enable JavaScript!
GluN2A/Glutamate [NMDA] receptor subunit epsilon 1 in Human [ChEMBL: CHEMBL1972] [GtoPdb: 456] [UniProtKB: Q12879] There should be some charts here, you may need to enable JavaScript!
GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Human [ChEMBL: CHEMBL1904] [GtoPdb: 457] [UniProtKB: Q13224] There should be some charts here, you may need to enable JavaScript!
GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Human [ChEMBL: CHEMBL4109] [GtoPdb: 458] [UniProtKB: Q14957] There should be some charts here, you may need to enable JavaScript!
GluN2D/Glutamate [NMDA] receptor subunit epsilon 4 in Human [ChEMBL: CHEMBL2591] [GtoPdb: 459] [UniProtKB: O15399] There should be some charts here, you may need to enable JavaScript!
glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415] There should be some charts here, you may need to enable JavaScript!
glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416] There should be some charts here, you may need to enable JavaScript!
glycine receptor β subunit in Human [GtoPdb: 427] [UniProtKB: P48167] There should be some charts here, you may need to enable JavaScript!
TRPM3 in Human [GtoPdb: 495] [UniProtKB: Q9HCF6] There should be some charts here, you may need to enable JavaScript!

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 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]