vipoglanstat [Ligand Id: 12209] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3694493 (GS-248, Vipoglanstat)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mPGES1/Prostaglandin E synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684]
ChEMBL Enzyme Assay: The aim of this assay is to determine the affinity of a test compound for the mPGES-1 enzyme. 47 ul of recombinant human mPGES-1 (0.5 ug protein/well) containing microsomal suspension in a buffer containing GSH, (2.5 mmol/L L-Glutathione reduced, dissolved in 0.1 mol/L Phosphat Buffer pH 7.4) is dispensed in a 384-well plate and thereafter 1 ul of the test compound(s) is/are added and incubated for 25 minutes at room temperature. The enzyme reaction is started by the addition of 2 ul PGH2 (final conc. 2 uM) dissolved in water-free Diglyme. After 60 seconds the reaction is terminated by addition of a stop solution containing FeCl2 (10 uL 0.074 mol/l FeCl2). The samples are diluted between 1:25 in PBS (Phosphate Buffered Saline). 10 ul of the diluted samples are transferred to 384-well low volume plate. B 8.7 pIC50 2 nM IC50 US-8759537-B2. 3H-imidazo [4, 5-C] pyridine-6-carboxamides as anti-inflammatory agents (2014)
GtoPdb - - 8.7 pIC50 2 nM IC50 WO2012022793A1. New compounds (2012)

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]