betrixaban [Ligand Id: 9602] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL512351 (Betrixaban, PRT054021, Bevyxxa, PRT-054021)
  • coagulation factor X/Coagulation factor X in Human [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742]
  • 9.93
1 CHEMBL512351_lig_chart_1 Coagulation factor X Human
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  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 1 pki data point
  • 5.74
2 CHEMBL512351_lig_chart_2 HERG Human
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  • plasminogen/Plasminogen in Human [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747]
  • This target only has 0 pki data point
  • 0
3 CHEMBL512351_lig_chart_3 Plasminogen Human
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  • coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
  • This target only has 0 pki data point
  • 0
4 CHEMBL512351_lig_chart_4 Thrombin Human
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  • plasminogen activator, tissue type/Tissue-type plasminogen activator in Human [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750]
  • This target only has 0 pki data point
  • 0
5 CHEMBL512351_lig_chart_5 Tissue-type plasminogen activator Human
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  • protein C, inactivator of coagulation factors Va and VIIIa/Vitamin K-dependent protein C in Human [ChEMBL: CHEMBL4444] [GtoPdb: 2396] [UniProtKB: P04070]
  • This target only has 0 pki data point
  • 0
6 CHEMBL512351_lig_chart_6 Vitamin K-dependent protein C 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 factor 10a B 9.92 pKi 0.12 nM Ki J. Med. Chem. (2010) 53: 6243-6274 [PMID:20503967]
GtoPdb Inhibition of human factor Xa. - 9.93 pKi 0.12 nM Ki Bioorg Med Chem Lett (2009) 19: 2179-85 [PMID:19297154]
ChEMBL Inhibition of Factor 10a B 9.93 pKi 0.12 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2179-2185 [PMID:19297154]
ChEMBL Inhibition of human factor 10a using substrate S-2765 preincubated for 30 mins followed by substrate addition measured after 20 mins by micro plate reader method B 8.35 pIC50 4.5 nM IC50 Eur J Med Chem (2017) 125: 411-422 [PMID:27689724]
ChEMBL Inhibition of human factor Xa using S-2222 as substrate preincubated for 30 mins followed by substrate addition and measured for 20 mins B 8.35 pIC50 4.5 nM IC50 Bioorg Med Chem (2018) 26: 5987-5999 [PMID:30446438]
ChEMBL Inhibition of Factor 10a B 8.82 pIC50 1.5 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2179-2185 [PMID:19297154]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Binding affinity to human ERG B 5.74 pKi 1800 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2179-2185 [PMID:19297154]
ChEMBL Inhibition of human ERG expressed in HEK293 cells by patch-clamp method B 5.05 pIC50 8900 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2179-2185 [PMID:19297154]
ChEMBL Inhibition of human ERG by patch clamp assay B 5.05 pIC50 8900 nM IC50 J. Med. Chem. (2010) 53: 6243-6274 [PMID:20503967]
plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747]
ChEMBL Inhibition of plasmin B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2179-2185 [PMID:19297154]
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL Inhibition of human thrombin using acromogenic substrate S-2238 preincubated for 30 mins before substrate addition measured after 20 mins by spectrophotometry B 4.74 pIC50 18000 nM IC50 Eur. J. Med. Chem. (2015) 95: 388-399 [PMID:25839438]
ChEMBL Inhibition of human thrombin using substrate S-2238 preincubated for 30 mins followed by substrate addition measured after 20 mins by micro plate reader method B 4.74 pIC50 18000 nM IC50 Eur J Med Chem (2017) 125: 411-422 [PMID:27689724]
ChEMBL Inhibition of thrombin B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2179-2185 [PMID:19297154]
ChEMBL Inhibition of human recombinant thrombin expressed in HEK293 cells using S-2238 as substrate preincubated for 30 mins followed by substrate addition and measured for 20 mins B 7.74 pIC50 18 nM IC50 Bioorg Med Chem (2018) 26: 5987-5999 [PMID:30446438]
plasminogen activator, tissue type/Tissue-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750]
ChEMBL Inhibition of tissue plasminogen activator B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2179-2185 [PMID:19297154]
protein C, inactivator of coagulation factors Va and VIIIa/Vitamin K-dependent protein C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4444] [GtoPdb: 2396] [UniProtKB: P04070]
ChEMBL Inhibition of activated anticoagulant protein C B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2179-2185 [PMID:19297154]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]