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ChEMBL ligand: CHEMBL512351 (Betrixaban, Betrixaban maleate, Bevyxxa, PRT-054021, PRT054021) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]