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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 |
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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]