ketoprofen [Ligand Id: 4795] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL571 (19583RP, Actron, Actron ketoprofen, Alrheumat, Aneol, Axorid, Capisten, Fenoket 200, Hydratropic acid, m-benzoyl-, IDEA-033, Iso-k, Jomethid xl, Ketocid 200, Ketonal, Ketoprofen, Ketorin, Ketotard 200 xl, Ketovail, Ketozip 200 xl, Larafen, Larafen cr, Nexcede, NSC-758144, Orudis, Orudis 100, Orudis kt, Oruvail, Oruvail 100, Oruvail 150, Oruvail 200, Oruvail im, Powergel, R.P. 19583, R.P. 19,583, RP-19583, (rs)-ketoprofen, RU-4733, Sector, Tiloket, Tiloket cr, Valket 200 retard)
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • Organic anion transporter 1/Solute carrier family 22 member 6 in Human [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8]
  • Organic anion transporter 1/Solute carrier family 22 member 6 in Rat [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956]
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  • Organic anion transporter 2/Solute carrier family 22 member 7 in Rat [ChEMBL: CHEMBL2073671] [GtoPdb: 1026] [UniProtKB: Q5RLM2]
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  • SMCT1 in Human [GtoPdb: 922] [UniProtKB: Q8N695]
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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]
GtoPdb Inhibition of COX1 in human whole blood. - 6.48 pIC50 330 nM IC50 Bioorg Med Chem Lett (2008) 18: 4655-7 [PMID:18667313]
ChEMBL Inhibition of COX1 in human whole blood B 6.48 pIC50 330 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 4655-4657 [PMID:18667313]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 7.85 pIC50 14 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL In vitro inhibition of cyclooxygenase-1 via inhibition of TXB2 generation in the presence of 1 uM arachidonic acid in human platelet F 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 533-537 [PMID:11844666]
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979]
ChEMBL Inhibition of purified ovine COX1 pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay B 6.1 pIC50 800 nM IC50 ACS Med. Chem. Lett. (2014) 5: 983-988 [PMID:25221653]
ChEMBL Inhibition of Ovine COX-1 preincubated for 15 mins by fluorescence analysis B 7.17 pIC50 67 nM IC50 ACS Med. Chem. Lett. (2015) 6: 1086-1090 [PMID:26487917]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL Inhibition of human recombinant COX2 pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay B 5.42 pIC50 3800 nM IC50 ACS Med. Chem. Lett. (2014) 5: 983-988 [PMID:25221653]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) B 6.11 pIC50 785 nM IC50 DrugMatrix in vitro pharmacology data
GtoPdb Inhibition of COX2 in human whole blood. - 6.16 pIC50 690 nM IC50 Bioorg Med Chem Lett (2008) 18: 4655-7 [PMID:18667313]
ChEMBL Inhibition of COX2 in human whole blood B 6.16 pIC50 690 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 4655-4657 [PMID:18667313]
ChEMBL Inhibition of recombinant human COX-2 preincubated for 15 mins by fluorescence analysis B 7.21 pIC50 61 nM IC50 ACS Med. Chem. Lett. (2015) 6: 1086-1090 [PMID:26487917]
ChEMBL In vitro inhibition of PGE-2 generation by LPS-stimulated monocytes isolated from human blood. F 7.59 pIC50 26 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 533-537 [PMID:11844666]
Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208]
ChEMBL Inhibition of ovine COX2 assessed as reduction in PGH2 production by enzyme immunoassay B 6.74 pIC50 180 nM IC50 Bioorg Med Chem (2018) 26: 4113-4126 [PMID:29980364]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR (unknown origin) using tyrosine 4 as substrate by fluorescence analysis B 5 pIC50 >10000 nM IC50 ACS Med. Chem. Lett. (2015) 6: 1086-1090 [PMID:26487917]
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 6-Carboxyfluorescein uptake in OAT1-expressing CHO cells F 5.85 pIC50 1400 nM IC50 Anal. Biochem. (2000) 283: 49-55 [PMID:10929807]
ChEMBL TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells F 5.89 pIC50 1300 nM IC50 J. Pharmacol. Exp. Ther. (2000) 295: 10-15 [PMID:10991954]
Organic anion transporter 1/Solute carrier family 22 member 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956]
ChEMBL TP_TRANSPORTER: inhibition of MTX uptake in Xenopus laevis oocytes F 6.3 pIC50 500 nM IC50 Eur. J. Pharmacol. (2000) 409: 31-36 [PMID:11099697]
Organic anion transporter 2/Solute carrier family 22 member 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073671] [GtoPdb: 1026] [UniProtKB: Q5RLM2]
ChEMBL TP_TRANSPORTER: inhibition of Salicylate uptake in Oat2-expressing LLC PK1 cells F 5.74 pKi 1840 nM Ki Jpn. Pharmacol. Ther. (2001) 29: S101-S104
SMCT1 in Human [GtoPdb: 922] [UniProtKB: Q8N695]
GtoPdb - - 3.92 pIC50 119000 nM IC50 Pharm Res (2006) 23: 1209-16 [PMID:16729224]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]