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

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ChEMBL ligand: CHEMBL599 (UHAC-62XX, N-1539, UH-AC 62XX, Anjeso, Mobic, Meloxicam, UH-AC-62 XX, Qmiiz odt, N1539, 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 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 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 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]