meloxicam [Ligand Id: 7220] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL599 (Acticam, Anjeso, Contacera, Coxicam, Emdocam, Flexicam, Inflacam, Loxicom, Melfax, Melosus, Melovem, Meloxicam, Meloxidolor, Meloxidyl, Meloxivet, Meloxoral, Metacam, Mobic, Movatec, N-1539, N1539, Qmiiz odt, Recocam, Revitacam, Rheumocam, UH-AC 62XX, UH-AC-62 XX, UHAC-62XX, Vivlodex)
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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 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 4.44 pIC50 36600 nM IC50 J Med Chem (1997) 40: 980-989 [PMID:9083488]
GtoPdb - - 4.44 pIC50 36600 nM IC50 J Med Chem (1997) 40: 980-9 [PMID:9083488]
ChEMBL Inhibition of human recombinant COX1 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated for 10 mins measured after substrate addition by microplate reader based enzyme immunoassay B 4.51 pIC50 31200 nM IC50 Bioorg Med Chem (2020) 28: 115526-115526 [PMID:32354672]
ChEMBL Concentration that caused a 50% decrease in the maximal inhibition of Prostaglandin G/H synthase 1 activity as measured by PGE-2 production. B 5.66 pIC50 2200 nM IC50 Bioorg Med Chem Lett (1998) 8: 1181-1186 [PMID:9871731]
ChEMBL In vitro for its inhibitory activity against human whole blood Prostaglandin G/H synthase 1 B 5.85 pIC50 1400 nM IC50 Bioorg Med Chem Lett (1999) 9: 1773-1778 [PMID:10406640]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 5.88 pIC50 1319 nM IC50 DrugMatrix in vitro pharmacology data
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979]
ChEMBL Inhibition of ovine COX1 after 5 mins by enzyme immuno assay B 4.71 pIC50 19400 nM IC50 Medchemcomm (2015) 6: 283-299
ChEMBL Inhibition of sheep seminal vesicle COX-1 assessed as reduction in oxygen consumption using arachidonic acid as substrate incubated for 12 mins followed by substrate addition measured for 2 mins B 6 pIC50 1000 nM IC50 Bioorg Med Chem (2017) 25: 316-326 [PMID:27842798]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL Inhibition of COX2 (unknown origin) assessed as suppression of PGG2 conversion to PGH2 incubated fro 2 mins by TMPD based colorimetric assay B 4.24 pIC50 57300 nM IC50 Bioorg Med Chem (2019) 27: 3918-3928 [PMID:31345747]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) B 6.03 pIC50 938 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 2 B 6.15 pIC50 700 nM IC50 Bioorg Med Chem Lett (1999) 9: 1773-1778 [PMID:10406640]
ChEMBL Concentration of drug that causes a 50% decrease in the maximal inhibition of Prostaglandin G/H synthase 2 activity as measured by PGE-2 production B 6.31 pIC50 490 nM IC50 J Med Chem (1997) 40: 980-989 [PMID:9083488]
GtoPdb - - 6.31 pIC50 490 nM IC50 J Med Chem (1997) 40: 980-9 [PMID:9083488]
ChEMBL Inhibition of human recombinant COX2 assessed as reduction in PGH2 formation using arachidonic acid as substrate preincubated for 10 mins measured after substrate addition by microplate reader based enzyme immunoassay B 6.48 pIC50 330 nM IC50 Bioorg Med Chem (2020) 28: 115526-115526 [PMID:32354672]
ChEMBL Concentration that caused a 50% decrease in the maximal inhibition of Prostaglandin G/H synthase 2 activity as measured by PGE-2 production. B 6.8 pIC50 160 nM IC50 Bioorg Med Chem Lett (1998) 8: 1181-1186 [PMID:9871731]
Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208]
ChEMBL Inhibition of ovine COX2 after 5 mins by enzyme immuno assay B 5.86 pIC50 1370 nM IC50 Medchemcomm (2015) 6: 283-299
COX-2 /Cyclooxygenase-2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4321] [GtoPdb: 1376] [UniProtKB: Q05769]
ChEMBL Inhibition of mouse COX-2 expressed in baculovirus infected Sf21 insect cells assessed as reduction in oxygen consumption using arachidonic acid as substrate incubated for 12 mins followed by substrate addition measured for 2 mins B 6.82 pIC50 151.36 nM IC50 Bioorg Med Chem (2017) 25: 316-326 [PMID:27842798]

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]