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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
