(R)-flurbiprofen [Ligand Id: 7340] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL190083 (E-7869, Flurbiprofen, (r)-, Flurizan, MPC-7869, R-flurbiprofen, Tarenflurbil)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL Inhibition of COX1 in human whole blood F 4.36 pIC50 44000 nM IC50 Bioorg Med Chem Lett (2006) 16: 2219-2223 [PMID:16455248]
COX-1 /Cyclooxygenase-1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4042] [GtoPdb: 1375] [UniProtKB: Q63921]
ChEMBL Concentration required to inhibit cyclooxygenase-1 in rat blood B 4.36 pIC50 44000 nM IC50 J Med Chem (2005) 48: 5705-5720 [PMID:16134939]
COX-2 /Cyclooxygenase-2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4321] [GtoPdb: 1376] [UniProtKB: Q05769]
ChEMBL Inhibition of COX2-mediated 2-arachidonoylglycerol oxygenation in LPS/IFN-gamma-stimulated mouse RAW264.7 cells assessed as 2-AG to PGE2-G/PGD2-G conversion treated 2 hrs after LPS/IFN-gamma stimulation measured after 6 hrs B 5.89 pIC50 1300 nM IC50 ACS Med Chem Lett (2012) 3: 759-763 [PMID:22984634]
presenilin 1/presenilin 2/Gamma-secretase in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094135] [GtoPdb: 2402, 2403] [UniProtKB: P49768, P49810, Q8WW43, Q92542, Q96BI3, Q9NZ42]
ChEMBL Modulation of gamma secretase (unknown origin) assessed as reduction in amyloid beta levels B 4 pIC50 100000 nM IC50 J Med Chem (2016) 59: 7719-7737 [PMID:27045975]

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]