edoxaban [Ligand Id: 7575] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1269025 (DU-176, Edoxaban, Lixiana)
  • coagulation factor X/Coagulation factor X in Human [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
coagulation factor X/Coagulation factor X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742]
GtoPdb - - 9.25 pKi 0.56 nM Ki J Med Chem (2010) 53: 6243-74 [PMID:20503967];
J Thromb Haemost (2008) 6: 1542-9 [PMID:18624979]
ChEMBL Inhibition of factor Xa (unknown origin) assessed as inhibition constant B 9.25 pKi 0.56 nM Ki Bioorg Med Chem Lett (2023) 80: 129127-129127 [PMID:36634753]
ChEMBL Inhibition of factor 10a B 9.25 pKi 0.56 nM Ki J Med Chem (2010) 53: 6243-6274 [PMID:20503967]
ChEMBL Inhibition of human coagulation factor 10a using Z-D-Arg-Gly-Arg-pNA.2HCl as substrate preincubated for 15 mins followed by substrate addition by UV absorption assay B 8.47 pIC50 3.4 nM IC50 Bioorg Med Chem Lett (2018) 28: 3813-3815 [PMID:30340898]
ChEMBL Inhibition of human factor Xa using Z-D-Arg-Gly-Arg-pNA.2HCl as substrate preincubated for 15 mins followed by substrate addition by UV absorption analysis B 8.47 pIC50 3.4 nM IC50 Bioorg Med Chem (2019) 27: 1320-1326 [PMID:30792102]

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]