soticlestat [Ligand Id: 11517] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4298172 (OV-935, OV935, Soticlestat, TAK-935, TAK935)
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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 CH24H expressing human 293-F cells for 15 minutes using [14C] cholesterol as substrate and measured after 5 hrs by trypan blue staining based thin-layer chromatography B 8.13 pIC50 7.4 nM IC50 J Med Chem (2022) 65: 3343-3358 [PMID:35166541]
ChEMBL Inhibition of full length N-terminal his6-tagged human CH24H (28 to 494 residues) expressed in Escherichia coli DH5alpha using [14C] cholesterol as substrate preincubated for 15 mins followed by substrate addition and measured after 5 min in presence of beta-NADPH B 8.13 pIC50 7.4 nM IC50 J Med Chem (2021) 64: 12228-12244 [PMID:34387987]
GtoPdb Inhibition of catalytic activity of human CH24H in vitro. - 8.35 pIC50 4.5 nM IC50 Sci Rep (2020) 10: 17081 [PMID:33051477]

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]