apixaban [Ligand Id: 6390] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL231779 (Apixaban, BMS-562247, BMS-562247-01, Eliquis)
  • coagulation factor X/Coagulation factor X in Human [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742]
  • Coagulation factor X in Rabbit [ChEMBL: CHEMBL5062] [UniProtKB: O19045]
  • 9.77
1 CHEMBL231779_lig_chart_1 Coagulation factor X HumanRabbit
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  • coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
  • 5.51
2 CHEMBL231779_lig_chart_2 Thrombin Human
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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]
ChEMBL Inhibition of human factor 10a B 10.1 pKi 0.08 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 4419-4427 [PMID:17588746]
ChEMBL Binding affinity to human F10a B 10.1 pKi 0.08 nM Ki J. Med. Chem. (2007) 50: 5339-5356 [PMID:17914785]
ChEMBL Inhibition of human factor 10a B 10.1 pKi 0.08 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2845-2849 [PMID:18424044]
ChEMBL Inhibition of Factor 10a B 10.1 pKi 0.08 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2179-2185 [PMID:19297154]
ChEMBL Binding affinity to human coagulation factor 10a B 10.1 pKi 0.08 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 462-468 [PMID:19046881]
ChEMBL Inhibition of human factor 10a B 10.1 pKi 0.08 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 1373-1377 [PMID:20100660]
ChEMBL Inhibition of factor 10a B 10.1 pKi 0.08 nM Ki J. Med. Chem. (2010) 53: 6243-6274 [PMID:20503967]
ChEMBL Inhibition of purified human factor Xa B 10.1 pKi 0.08 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 3341-3345 [PMID:24951330]
GtoPdb - - 10.1 pKi 0.08 nM Ki J Thromb Haemost (2008) 6: 820-9 [PMID:18315548]
ChEMBL Inhibition of human coagulation factor 10a assessed as reduction in p-nitroaniline cleavage from pefachrome substrate preincubated for 10 mins followed by substrate addition measured after 20 mins B 6.64 pIC50 230 nM IC50 Bioorg Med Chem (2016) 24: 5646-5661 [PMID:27663548]
ChEMBL Inhibition of human F10a assessed as decrease in p-nitroaniline cleavage from pefachrome F10a preincubated for 10 mins followed by substrate addition measured after 20 mins B 6.68 pIC50 210 nM IC50 Bioorg Med Chem (2017) 25: 2800-2810 [PMID:28389110]
Coagulation factor X in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5062] [UniProtKB: O19045]
ChEMBL Binding affinity to rabbit F10a B 9.77 pKi 0.17 nM Ki J. Med. Chem. (2007) 50: 5339-5356 [PMID:17914785]
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL Inhibition of human thrombin B 5.51 pKi 3100 nM Ki J. Med. Chem. (2007) 50: 5339-5356 [PMID:17914785]
ChEMBL Inhibition of human factor 2a B 5.51 pKi 3100 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 1373-1377 [PMID:20100660]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]