friluglanstat [Ligand Id: 12888] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3934885
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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]
GtoPdb Inhibition of PGE2 production in A549 epithelial cells - 7.89 pIC50 12.9 nM IC50 US9216968B2. Heterocyclic derivative and pharmaceutical drug (2015)
GtoPdb Inhibition of mPGES1 in microsomes isolated from CHO-K1 cells transiently expressing human mPGES1 - 8.18 pIC50 6.6 nM IC50 US9216968B2. Heterocyclic derivative and pharmaceutical drug (2015)
ChEMBL Inhibition Assay: mPGES-1 microsome fractions were prepared from CHO-K1 cells transiently transfected with plasmid encoding the human mPGES-1cDNA. Microsomes were diluted with potassium phosphate buffer containing reduced glutathione (pH7.4), and DMSO containing test compound or DMSO alone was added (such that DMSO final concentration would be 1% in each) and incubated at 4° C. for 20 minutes. Then, the enzymatic reactions were initiated by the addition of PGH2 substrate (final concentration 1 μM) and incubated at 4° C. for 60 seconds. The reaction was terminated by the addition of a citrate solution (final citrate concentration 50 mM) containing ferric chloride (final concentration 1 mg/mL). PGE2 production in the enzyme reaction aliquot was measured using HTRF kit (Cisbio International, catalogue #62P2APEC). B 8.18 pIC50 6.6 nM IC50 US-9216968-B2. Heterocyclic derivative and pharmaceutical drug (2015)

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]