An EC 3.4.21.* (serine endopeptidase) inhibitor that interferes with the action of coagulation factor Xa (EC 3.4.21.6).
ChEBI ID: 68581
| Member | Definition | Class |
|---|---|---|
| apixaban | A pyrazolopyridine that is 7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide substituted at position 1 by a 4-methoxyphenyl group and at position 6 by a 4-(2-oxopiperidin-1-yl)phenyl group. It is used for the prevention and treatment of thromboembolic diseases. | apixaban |
| betrixaban | A secondary carboxamide obtained by formal condensation of the carboxy group of 4-(N,N-dimethylcarbamimidoyl)benzoic acid with the amino group of 2-amino-N-(5-chloropyridin-2-yl)-5-methoxybenzamide. A synthetic anticoagulant compound that targets activated factor Xa in the coagulation cascade. | betrixaban |
| edoxaban | A monocarboxylic acid amide that is used (as its tosylate monohydrate) for the treatment of deep vein thrombosis and pulmonary embolism. | edoxaban |
| pd 0348292 | A member of the class of pyrrolidines that is (2R,4R)-N(1)-(p-chlorophenyl)-4-methoxypyrrolidine-1,2-dicarboxamide in which the nitrogen of the 2-carbamoyl group has been substituted by a 2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl group. It is a synthetic organic anticoagulant compound that targets activated factor Xa in the coagulation cascade. | eribaxaban |
| rivaroxaban | A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-chlorothiophene-2-carboxylic acid with the amino group of 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one. An anticoagulant used for prophylaxis of venous thromboembolism in patients with knee or hip replacement surgery. | rivaroxaban |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 147 (2.39) | 29.6817 |
| 2010's | 3,963 (64.46) | 24.3611 |
| 2020's | 2,038 (33.15) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 1,023 (12.54%) | 5.53% |
| Reviews | 1,960 (24.02%) | 6.00% |
| Case Studies | 783 (9.60%) | 4.05% |
| Observational | 430 (5.27%) | 0.25% |
| Other | 3,964 (48.58%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 3.7908 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 37.9083 | 1 | 1 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 0.0209 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 3.7908 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 3.7908 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 3.7908 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 3.7908 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Chain A, Activated Factor Xa Heavy Chain | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
| Chain A, Coagulation factor X (EC 3.4.21.6) (Stuart factor) (Stuart-Prower factor) | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
| Coagulation factor X | Homo sapiens (human) | IC50 | 0.0274 | 17 | 18 |
| Coagulation factor X | Homo sapiens (human) | Ki | 0.1244 | 15 | 25 |
| Coagulation factor X | Oryctolagus cuniculus (rabbit) | Ki | 0.0002 | 1 | 1 |
| Coagulation factor XII | Homo sapiens (human) | IC50 | 33.0000 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Plasminogen | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 8.9000 | 2 | 2 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | Ki | 1.8000 | 1 | 1 |
| Prothrombin | Homo sapiens (human) | IC50 | 11.5045 | 4 | 4 |
| Prothrombin | Homo sapiens (human) | Ki | 2.0600 | 4 | 5 |
| Suppressor of tumorigenicity 14 protein | Homo sapiens (human) | Ki | 3.3500 | 1 | 1 |
| Tissue-type plasminogen activator | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Trypsin-1 | Homo sapiens (human) | Ki | 4.2000 | 1 | 1 |
| Trypsin-2 | Homo sapiens (human) | Ki | 4.2000 | 1 | 1 |
| Trypsin-3 | Homo sapiens (human) | Ki | 4.2000 | 1 | 1 |
| Vitamin K-dependent protein C | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Chain A, Coagulation factor X, heavy chain | Homo sapiens (human) | Kd | 0.0003 | 1 | 1 |