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

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ChEMBL ligand: CHEMBL563 (U-27182, Strefen, Flurbiprofen, BTS 18322, Ocufen, Froben, Froben Sr, Transact, BTS-18322, Cebutid, Flubiprofen, Ansaid)
  • 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. U.S.A. (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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]