An EC 3.4.21.* (serine endopeptidase) inhibitor that interferes with the action of thrombin (EC 3.4.21.5).
ChEBI ID: 65232
| Member | Definition | Class |
|---|---|---|
| acetylphenylalanyl-prolyl-boroarginine | A C-terminal boronic acid petide that is N-acetyl-D-phenylalanyl-L-prolyl-L-arginine in which the C-termnal carboxy group has been replaced by a borono (-B(OH)2) group. A thrombin (Factor IIa) inhibitor, thereby acting as an anticoagulant. | Ac-(D)Phe-Pro-boroArg-OH |
| bivalirudin | A synthetic peptide of 20 amino acids, comprising D-Phe, Pro, Arg, Pro, Gly, Gly, Gly, Gly, Asn, Gly, Asp, Phe, Glu, Glu, Ile, Pro, Glu, Glu, Tyr, and Leu in sequence. A congener of hirudin (a naturally occurring drug found in the saliva of the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant. | bivalirudin |
| dabigatran | An aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-carbamimidoylphenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amoino group of N-pyridin-2-yl-beta-alanine. The active metabolite of the prodrug dabigatran etexilate, it acts as an anticoagulant which is used for the prevention of stroke and systemic embolism. | dabigatran |
| dabigatran etexilate | An aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-{N'-[(hexyloxy)carbonyl]carbamimidoyl}phenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amino group of ethyl N-pyridin-2-yl-beta-alaninate. A prodrug for dabigatran, a thrombin inhibitor and anticoagulant which is used for the prevention of stroke and systemic embolism. | dabigatran etexilate |
| dabigatran etexilate | An aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-{N'-[(hexyloxy)carbonyl]carbamimidoyl}phenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amino group of ethyl N-pyridin-2-yl-beta-alaninate. A prodrug for dabigatran, a thrombin inhibitor and anticoagulant which is used for the prevention of stroke and systemic embolism. | dabigatran etexilate |
| glycyrrhizic acid | A triterpenoid saponin that is the glucosiduronide derivative of 3beta-hydroxy-11-oxoolean-12-en-30-oic acid. | glycyrrhizinic acid |
| melagatran | A member of the class of azetidines that is (2S)-azetidine 2-carboxylic acid in which the carboxylic acid has been converted to the amide corresponding to formal condensation with 4-(aminomethyl)benzenecarboximidamide and in which the hydrogen attached to the azetidine nitrogen is replaced by a (2R)-2-cyclohexyl-2-[(carboxymethyl)amino]acetyl group. | melagatran |
| procyanidin b1 | A proanthocyanidin consisting of (-)-epicatechin and (+)-catechin units joined by a bond between positions 4 and 8' respectively in a beta-configuration.. Procyanidin B1 can be found in Cinnamomum verum (Ceylon cinnamon, in the rind, bark or cortex), in Uncaria guianensis (cat's claw, in the root), and in Vitis vinifera (common grape vine, in the leaf) or in peach. | procyanidin B1 |
| ximelagatran | A member of the class of azetidines that is melagatran in which the carboxylic acid group has been converted to the corresponding ethyl ester and in which the amidine group has been converted into the corresponding amidoxime. A prodrug for melagatran, ximelagatran was the first orally available direct thrombin inhibitor to be brought to market as an anticoagulant, but was withdrawn in 2006 following reports of it causing liver damage. | ximelagatran (hydroxylamine form); ximelagatran |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 172 (2.30) | 18.7374 |
| 1990's | 395 (5.29) | 18.2507 |
| 2000's | 1,323 (17.72) | 29.6817 |
| 2010's | 4,272 (57.22) | 24.3611 |
| 2020's | 1,304 (17.47) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 707 (8.82%) | 5.53% |
| Reviews | 1,624 (20.27%) | 6.00% |
| Case Studies | 690 (8.61%) | 4.05% |
| Observational | 240 (3.00%) | 0.25% |
| Other | 4,751 (59.30%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| AR protein | Homo sapiens (human) | Potency | 18.3473 | 7 | 8 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 33.4915 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 6.0322 | 1 | 2 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 31.2268 | 1 | 2 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 6.1164 | 1 | 2 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 14.9762 | 1 | 2 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 20.9754 | 5 | 5 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 15.9663 | 3 | 3 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 14.5776 | 6 | 6 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 11.7038 | 4 | 6 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 33.4889 | 1 | 1 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 33.1734 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 6.0322 | 1 | 2 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 1.1237 | 2 | 2 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 22.3829 | 2 | 2 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 23.7101 | 1 | 1 |
| histone deacetylase 9 isoform 3 | Homo sapiens (human) | Potency | 11.8832 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 6.0322 | 1 | 2 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 6.0322 | 1 | 4 |
| Interferon beta | Homo sapiens (human) | Potency | 6.0322 | 1 | 2 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 27.5404 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 33.4889 | 2 | 2 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 26.7797 | 2 | 2 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 29.8470 | 1 | 1 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 33.0156 | 2 | 3 |
| polyprotein | Zika virus | Potency | 33.1734 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 11.8832 | 1 | 1 |
| progesterone receptor | Homo sapiens (human) | Potency | 13.3332 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 13.4216 | 2 | 2 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 9.3826 | 2 | 2 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 22.6142 | 2 | 2 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 22.6142 | 2 | 2 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 29.8816 | 1 | 2 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 29.8493 | 1 | 1 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 30.1065 | 1 | 1 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 28.2240 | 2 | 2 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 23.7101 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Alpha-synuclein | Homo sapiens (human) | IC50 | 7.3000 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Beta-glucuronidase | Escherichia coli K-12 | IC50 | 12.1500 | 1 | 1 |
| Beta-glucuronidase | Rattus norvegicus (Norway rat) | IC50 | 97.2100 | 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 |
| Canalicular multispecific organic anion transporter 1 | Rattus norvegicus (Norway rat) | Ki | 1.3750 | 2 | 2 |
| Cationic trypsin | Bos taurus (cattle) | IC50 | 0.0112 | 1 | 1 |
| Chain H, Prothrombin | Homo sapiens (human) | Ki | 0.0040 | 1 | 2 |
| Coagulation factor VII | Homo sapiens (human) | IC50 | 3.3000 | 1 | 1 |
| Coagulation factor X | Homo sapiens (human) | IC50 | 18.5333 | 2 | 3 |
| Coagulation factor X | Homo sapiens (human) | Ki | 3.0600 | 4 | 4 |
| Coagulation factor XI | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| Coagulation factor XII | Homo sapiens (human) | IC50 | 33.0000 | 1 | 1 |
| Corticosteroid 11-beta-dehydrogenase isozyme 1 | Homo sapiens (human) | IC50 | 0.0115 | 3 | 3 |
| Corticosteroid 11-beta-dehydrogenase isozyme 1 | Mus musculus (house mouse) | IC50 | 0.0135 | 3 | 3 |
| Corticosteroid 11-beta-dehydrogenase isozyme 2 | Homo sapiens (human) | IC50 | 0.0007 | 3 | 3 |
| Disintegrin and metalloproteinase domain-containing protein 17 | Homo sapiens (human) | IC50 | 17.3000 | 1 | 2 |
| Glycogen phosphorylase, muscle form | Oryctolagus cuniculus (rabbit) | IC50 | 822.0000 | 1 | 1 |
| Multidrug and toxin extrusion protein 1 | Homo sapiens (human) | IC50 | 8.1000 | 1 | 1 |
| Multidrug and toxin extrusion protein 2 | Homo sapiens (human) | IC50 | 25.3000 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 1 |
| Pancreatic alpha-amylase | Sus scrofa (pig) | IC50 | 200.0000 | 1 | 1 |
| Plasminogen | Homo sapiens (human) | IC50 | 3.0600 | 1 | 2 |
| Plasminogen | Homo sapiens (human) | Ki | 1.3983 | 3 | 3 |
| Prothrombin | Homo sapiens (human) | IC50 | 0.2406 | 20 | 22 |
| Prothrombin | Homo sapiens (human) | Ki | 0.0029 | 15 | 15 |
| Ribosyldihydronicotinamide dehydrogenase [quinone] | Homo sapiens (human) | IC50 | 10.5000 | 2 | 2 |
| Ribosyldihydronicotinamide dehydrogenase [quinone] | Homo sapiens (human) | Ki | 60.0000 | 1 | 1 |
| Serine protease hepsin | Homo sapiens (human) | Ki | 0.8350 | 1 | 1 |
| Solute carrier family 22 member 2 | Homo sapiens (human) | IC50 | 4.7000 | 1 | 1 |
| Solute carrier organic anion transporter family member 1B1 | Homo sapiens (human) | Ki | 15.9000 | 1 | 1 |
| Solute carrier organic anion transporter family member 1B2 | Rattus norvegicus (Norway rat) | Ki | 6.1000 | 1 | 1 |
| Solute carrier organic anion transporter family member 1B3 | Homo sapiens (human) | Ki | 12.5000 | 1 | 1 |
| Tissue-type plasminogen activator | Homo sapiens (human) | Ki | 15.9233 | 3 | 3 |
| Trypsin-1 | Homo sapiens (human) | IC50 | 0.0119 | 1 | 2 |
| Trypsin-1 | Homo sapiens (human) | Ki | 0.0227 | 5 | 5 |
| Trypsin-2 | Homo sapiens (human) | IC50 | 0.0119 | 1 | 2 |
| Trypsin-2 | Homo sapiens (human) | Ki | 0.0349 | 3 | 3 |
| Trypsin-3 | Homo sapiens (human) | IC50 | 0.0119 | 1 | 2 |
| Trypsin-3 | Homo sapiens (human) | Ki | 0.0349 | 3 | 3 |
| Tyrosine-protein phosphatase non-receptor type 1 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Urokinase-type plasminogen activator | Homo sapiens (human) | Ki | 6.3000 | 1 | 1 |
| Vitamin K-dependent protein C | Homo sapiens (human) | IC50 | 1.3000 | 1 | 1 |
| Vitamin K-dependent protein C | Homo sapiens (human) | Ki | 20.9300 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Corticosteroid 11-beta-dehydrogenase isozyme 1 | Homo sapiens (human) | EC50 | 0.0100 | 1 | 1 |
| Corticosteroid 11-beta-dehydrogenase isozyme 1 | Mus musculus (house mouse) | EC50 | 0.0080 | 1 | 1 |
| Corticosteroid 11-beta-dehydrogenase isozyme 2 | Homo sapiens (human) | EC50 | 0.0010 | 1 | 1 |
| High mobility group protein B1 | Homo sapiens (human) | Kd | 122.5000 | 4 | 4 |
| Prothrombin | Homo sapiens (human) | Kd | 0.0007 | 2 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| High mobility group protein B1 | Mus musculus (house mouse) | ED50 | 70.0000 | 1 | 1 |