HR1405-01 [Ligand Id: 11973] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL441414 (Loxoprofen trans alcohol)
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  • Cytochrome c oxidase subunit 1 in Human [ChEMBL: CHEMBL6173] [UniProtKB: P00395]
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  • Cytochrome c oxidase subunit 2 in Human [ChEMBL: CHEMBL6174] [UniProtKB: P00403]
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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 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]