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