piroxicam [Ligand Id: 7273] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL527 (Pirozip 10, Larapam, Feldene 20, Piroflam 20, Brexidol, Feldene p, CP-16171, Kentene, Pirozip 20, Piroxicam, Flamatrol, CP-16,171, NSC-666076, Feldene, Piroflam 10)
  • 5-LOX/Arachidonate 5-lipoxygenase in Rat [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
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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 3/Solute carrier family 22 member 8 in Human [ChEMBL: CHEMBL1641348] [GtoPdb: 1027] [UniProtKB: Q8TCC7]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-LOX/Arachidonate 5-lipoxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
ChEMBL Inhibition of 5-lipoxygenase from rat peritoneal neutrophils after oral administration B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1988) 31: 1453-1462 [PMID:3133478]
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL Inhibition of COX-1 (unknown origin) using arachidonic acid as substrate preincubated for 2 mins followed by substrate addition in presence of TMPD by spectrophotometric analysis B 4.07 pIC50 85113.8 nM IC50 Bioorg Med Chem (2017) 25: 316-326 [PMID:27842798]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 5.88 pIC50 1313 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Concentration of drug that causes a 50% decrease in the maximal inhibition of Prostaglandin G/H synthase 1 activity as measured by PGE-2 production (''++'' indicates 80-90% inhibition) B 5.89 pIC50 1300 nM IC50 J. Med. Chem. (1997) 40: 980-989 [PMID:9083488]
GtoPdb - - 5.89 pIC50 1300 nM IC50 J Med Chem (1997) 40: 980-9 [PMID:9083488]
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979]
ChEMBL Tested for inhibitory activity against Prostaglandin G/H synthase 1 from ovine B 4.68 pIC50 21000 nM IC50 J. Med. Chem. (1995) 38: 3895-3901 [PMID:7562922]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
GtoPdb - - 3.66 pIC50 218000 nM IC50 J Med Chem (1995) 38: 3895-901 [PMID:7562922]
ChEMBL Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate preincubated for 2 mins followed by substrate addition in presence of TMPD by spectrophotometric analysis relative to control B 4.05 pIC50 89125.09 nM IC50 Bioorg Med Chem (2017) 25: 316-326 [PMID:27842798]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
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 Ochratoxin A uptake in OAT1-expressing S2 cells F 4.7 pKi 19800 nM Ki Life Sci. (2001) 69: 2123-2135 [PMID:11669456]
ChEMBL TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells F 4.69 pIC50 20500 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 PAH uptake in Xenopus laevis oocytes F 4.28 pKi 52000 nM Ki Mol. Pharmacol. (1999) 55: 847-854 [PMID:10220563]
Organic anion transporter 3/Solute carrier family 22 member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641348] [GtoPdb: 1027] [UniProtKB: Q8TCC7]
ChEMBL TP_TRANSPORTER: inhibition of Ochratoxin A uptake in OAT3-expressing S2 cells F 5.31 pKi 4880 nM Ki Life Sci. (2001) 69: 2123-2135 [PMID:11669456]

ChEMBL data shown on this page come from version 28:

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]