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 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 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]