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]
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  • coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
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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]
ChEMBL Inhibition of factor Xa (unknown origin) assessed as inhibition constant B 10.1 pKi 0.08 nM Ki Bioorg Med Chem Lett (2023) 80: 129127-129127 [PMID:36634753]
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]
ChEMBL Inhibition of factor Xa (unknown origin) B 8.65 pIC50 2.26 nM IC50 Bioorg Med Chem Lett (2023) 80: 129127-129127 [PMID:36634753]
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 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]