lumiracoxib [Ligand Id: 2897] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL404108 (COX-189, Lumiracoxib, Prexige) |
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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 | Inhibition of COX1 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2007) 50: 1425-1441 [PMID:17341061] |
| ChEMBL | Inhibition of COX1 | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2012) 55: 2932-2942 [PMID:22236250] |
| COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
| GtoPdb | - | - | 6.49 | pKi | 320 | nM | Ki | J Biol Chem (2007) 282: 16379-90 [PMID:17434872] |
| ChEMBL | Inhibition of human COX2 preincubated before addition of [1-14C]arachidonic acid | B | 6.49 | pKi | 320 | nM | Ki | J Biol Chem (2007) 282: 16379-16390 [PMID:17434872] |
| ChEMBL | Inhibition of COX2 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2012) 55: 2932-2942 [PMID:22236250] |
| ChEMBL | Inhibition of human COX2 mediated PGE2 production in human whole blood | B | 6.85 | pIC50 | 140 | nM | IC50 | J Biol Chem (2007) 282: 16379-16390 [PMID:17434872] |
| ChEMBL | Inhibition of COX2 (unknown origin) | B | 6.85 | pIC50 | 140 | nM | IC50 | Medchemcomm (2015) 6: 2081-2123 |
| ChEMBL | Inhibition of human COX2 mediated PGE2 production in IL-1-beta-induced human dermal fibroblast cells | B | 6.89 | pIC50 | 130 | nM | IC50 | J Biol Chem (2007) 282: 16379-16390 [PMID:17434872] |
| ChEMBL | Inhibition of human COX2 for 17 mins pre-incubated before addition of [1-14C]arachidonic acid | B | 6.97 | pIC50 | 107 | nM | IC50 | J Biol Chem (2007) 282: 16379-16390 [PMID:17434872] |
| ChEMBL | Inhibition of COX-2 (unknown origin) | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1516-1520 [PMID:26898334] |
| ChEMBL | Inhibition of COX2 | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2007) 50: 1425-1441 [PMID:17341061] |
| COX-2 /Cyclooxygenase-2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4321] [GtoPdb: 1376] [UniProtKB: Q05769] | ||||||||
| ChEMBL | Inhibition of purified mouse COX-2 assessed as inhibition of PGE2-G/PGD2-G formation preincubated for 3 mins before 2-AG substrate addition measured after 30 seconds by LC-MS-MS method | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5860-5864 [PMID:24060487] |
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]
