flurbiprofen [Ligand Id: 4194] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL563 (Ansaid, BTS 18,322, BTS-18322, Cebutid, Flubiprofen, Flurbiprofen, Froben, Froben sr, NSC-757037, Ocufen, Strefen, Transact, U-27,182, U-27182)
  • Aldo-keto reductase family 1 member C1 in Human [ChEMBL: CHEMBL5905] [UniProtKB: Q04828]
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  • Aldo-keto reductase family 1 member C2 in Human [ChEMBL: CHEMBL5847] [UniProtKB: P52895]
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  • AKR1C3/Aldo-keto-reductase family 1 member C3 in Human [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
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  • Aldo-keto reductase family 1 member C4 in Human [ChEMBL: CHEMBL4999] [UniProtKB: P17516]
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  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
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  • fatty acid binding protein 2/Fatty acid binding protein intestinal in Human [ChEMBL: CHEMBL4879] [GtoPdb: 2532] [UniProtKB: P12104]
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  • fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
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  • Organic anion transporter 1/Solute carrier family 22 member 6 in Human [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8]
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  • ASIC1 in Rat [GtoPdb: 684] [UniProtKB: P55926]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Aldo-keto reductase family 1 member C1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5905] [UniProtKB: Q04828]
ChEMBL Inhibition of human recombinant N-terminal His6-tagged AKR1C1 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis B 4 pIC50 >100000 nM IC50 J Med Chem (2012) 55: 7746-7758 [PMID:22877157]
Aldo-keto reductase family 1 member C2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5847] [UniProtKB: P52895]
ChEMBL Inhibition of human recombinant N-terminal His6-tagged AKR1C2 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis B 4.49 pIC50 32500 nM IC50 J Med Chem (2012) 55: 7746-7758 [PMID:22877157]
AKR1C3/Aldo-keto-reductase family 1 member C3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
ChEMBL Inhibition of human recombinant N-terminal His6-tagged AKR1C3 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis B 5.81 pIC50 1560 nM IC50 J Med Chem (2012) 55: 7746-7758 [PMID:22877157]
Aldo-keto reductase family 1 member C4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4999] [UniProtKB: P17516]
ChEMBL Inhibition of human recombinant N-terminal His6-tagged AKR1C4 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis B 4 pIC50 >100000 nM IC50 J Med Chem (2012) 55: 7746-7758 [PMID:22877157]
Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
ChEMBL Inhibition of FAAH in Sprague-Dawley rat brain homogenates preincubated for 10 mins followed by addition of substrate measured after 30 mins by liquid scintillation counting B 4 pIC50 >100000 nM IC50 Eur J Med Chem (2016) 109: 216-237 [PMID:26774927]
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL Inhibition of COX-1 (unknown origin) B 5.7 pIC50 1995.26 nM IC50 Bioorg Med Chem (2017) 25: 316-326 [PMID:27842798]
GtoPdb - - 7.12 pIC50 75 nM IC50 Proc Natl Acad Sci USA (1999) 96: 7563-8 [PMID:10377455]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 7.68 pIC50 21 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of COX1 B 8 pIC50 10 nM IC50 J Med Chem (2007) 50: 1425-1441 [PMID:17341061]
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979]
ChEMBL Binding affinity of compound towards prostaglandin G/H synthase 1 was evaluated B 6 pKi 1000 nM Ki Bioorg Med Chem Lett (2004) 14: 667-671 [PMID:14741265]
ChEMBL Inhibition of ovine COX1 B 6.3 pIC50 500 nM IC50 Bioorg Med Chem (2010) 18: 2204-2218 [PMID:20188577]
ChEMBL Inhibition of ovine COX1 assessed as production of PGF2-alpha preincubated with compound followed by the addition of 5 uM arachidonic acid as substrate by enzyme immunoassay B 6.82 pIC50 150 nM IC50 Eur J Med Chem (2016) 109: 216-237 [PMID:26774927]
ChEMBL Reversible competitive inhibition of prostaglandin G/H synthase 1 B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2004) 14: 667-671 [PMID:14741265]
ChEMBL In vitro inhibitory activity against Prostaglandin G/H synthase 1 in sheep B 7.96 pIC50 11 nM IC50 Bioorg Med Chem Lett (1999) 9: 307-312 [PMID:10091674]
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 6.77 pIC50 170 nM IC50 J Med Chem (2005) 48: 5705-5720 [PMID:16134939]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL Inhibition of COX-2 (unknown origin) B 5.7 pIC50 1995.26 nM IC50 Bioorg Med Chem (2017) 25: 316-326 [PMID:27842798]
ChEMBL Inhibition of recombinant human COX2 assessed as production of PGF2-alpha preincubated with compound followed by the addition of 5 uM arachidonic acid as substrate by enzyme immunoassay B 5.97 pIC50 1060 nM IC50 Eur J Med Chem (2016) 109: 216-237 [PMID:26774927]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) B 6.44 pIC50 359 nM IC50 DrugMatrix in vitro pharmacology data
GtoPdb - - 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (1999) 9: 307-12 [PMID:10091674]
ChEMBL In vitro inhibitory activity against Prostaglandin G/H synthase 2 (COX-2) in human B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (1999) 9: 307-312 [PMID:10091674]
ChEMBL Inhibition of COX2 B 8 pIC50 10 nM IC50 J Med Chem (2007) 50: 1425-1441 [PMID:17341061]
COX-2 /Cyclooxygenase-2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4321] [GtoPdb: 1376] [UniProtKB: Q05769]
ChEMBL Inhibition of mouse COX2 B 6.3 pIC50 500 nM IC50 Bioorg Med Chem (2010) 18: 2204-2218 [PMID:20188577]
fatty acid binding protein 2/Fatty acid binding protein intestinal in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879] [GtoPdb: 2532] [UniProtKB: P12104]
ChEMBL Displacement of 1-anilinonaphthalene-8-sulphonic acid from I-FABP B 4.59 pKi 26000 nM Ki J Med Chem (2008) 51: 3755-3764 [PMID:18533710]
fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
ChEMBL Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay B 5.93 pKi 1180 nM Ki J Med Chem (2008) 51: 3755-3764 [PMID:18533710]
Organic anion transporter 1/Solute carrier family 22 member 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8]
ChEMBL TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells F 5.82 pIC50 1500 nM IC50 J Pharmacol Exp Ther (2000) 295: 10-15 [PMID:10991954]
ASIC1 in Rat [GtoPdb: 684] [UniProtKB: P55926]
GtoPdb - - 3.5 pIC50 350000 nM IC50 J Neurosci (2001) 21: 8026-33 [PMID:11588175]

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]