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 (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 34:

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]