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ChEMBL ligand: CHEMBL441414 (Loxoprofen trans alcohol) |
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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 | Inhibitory activity against recombinant human prostaglandin G/H synthase 1 | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1201-1203 [PMID:14980665] |
ChEMBL | Inhibitory potency against Prostaglandin G/H synthase 1 in human whole blood assay | B | 6.55 | pIC50 | 280 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1201-1203 [PMID:14980665] |
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
ChEMBL | Inhibitory activity against recombinant human Prostaglandin G/H synthase 2 | B | 6.41 | pIC50 | 390 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1201-1203 [PMID:14980665] |
GtoPdb | - | - | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1201-3 [PMID:14980665] |
ChEMBL | Inhibitory potency against cyclooxygenase-2 in human whole blood assay | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1201-1203 [PMID:14980665] |
Cytochrome c oxidase subunit 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6173] [UniProtKB: P00395] | ||||||||
ChEMBL | Inhibition of human recombinant COX-1 using [1-14C] arachidonic acid as substrate preincubated for 15 mins followed by substrate addition | B | 5.83 | pIC50 | 1470 | nM | IC50 | Eur J Med Chem (2022) 235: 114258-114258 [PMID:35339101] |
ChEMBL | Inhibition of human recombinant COX-1 using arachidonic acid as substrate preincubated for 15 mins followed by substrate addition and measured after 5 mins | B | 6.3 | pIC50 | 500 | nM | IC50 | Eur J Med Chem (2022) 235: 114258-114258 [PMID:35339101] |
ChEMBL | Inhibition of COX-1 in human whole blood assessed as reduction in thromboxane B2 production by immunoassay | B | 6.55 | pIC50 | 280 | nM | IC50 | Eur J Med Chem (2022) 235: 114258-114258 [PMID:35339101] |
Cytochrome c oxidase subunit 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6174] [UniProtKB: P00403] | ||||||||
ChEMBL | Inhibition of human recombinant COX-2 using arachidonic acid as substrate preincubated for 15 mins followed by substrate addition and measured after 5 mins | B | 6.41 | pIC50 | 390 | nM | IC50 | Eur J Med Chem (2022) 235: 114258-114258 [PMID:35339101] |
ChEMBL | Inhibition of COX-2 in LPS-stimulated human whole blood assessed as reduction in PGE2 production by immunoassay | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2022) 235: 114258-114258 [PMID:35339101] |
ChEMBL | Inhibition of human recombinant COX-2 using [1-14C] arachidonic acid as substrate preincubated for 15 mins followed by substrate addition | B | 7.59 | pIC50 | 26 | nM | IC50 | Eur J Med Chem (2022) 235: 114258-114258 [PMID:35339101] |
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]