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

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ChEMBL ligand: CHEMBL3934885 (Friluglanstat)
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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 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]