Target type: biologicalprocess
A protein activation cascade that contributes to blood coagulation and consists of the interactions among high molecular weight kininogen, prekallikrein, and factor XII that lead to the activation of clotting factor X. [GOC:add, GOC:mah, GOC:pde]
The intrinsic pathway of blood coagulation is initiated by contact activation, a process triggered by exposure of blood to collagen and other negatively charged surfaces. This exposure leads to the activation of factor XII (Hageman factor), which is a zymogen (inactive precursor) circulating in the blood.
Factor XII, upon contact with collagen, undergoes a conformational change, becoming activated to factor XIIa. Factor XIIa then activates factor XI, another zymogen, transforming it into factor XIa. Factor XIa, in turn, activates factor IX, another zymogen, converting it to factor IXa.
The activation of factor IX is a key step in the intrinsic pathway. Factor IXa, along with calcium ions and phospholipid surfaces, forms a complex with factor VIIIa (activated factor VIII). This complex is known as the "tenase complex," and it functions to activate factor X, another zymogen, into factor Xa.
Factor Xa, along with calcium ions and phospholipids, forms a complex with factor Va (activated factor V). This complex is called the "prothrombinase complex," and it serves as the final enzyme in the intrinsic pathway. The prothrombinase complex converts prothrombin, a zymogen, into thrombin, a powerful enzyme that cleaves fibrinogen, a soluble protein, into fibrin, an insoluble protein.
Fibrin monomers, formed by thrombin cleavage of fibrinogen, spontaneously polymerize into long fibrin strands. These strands become crosslinked by factor XIIIa (activated factor XIII), forming a stable fibrin meshwork that traps platelets and other blood components, forming a clot.
The intrinsic pathway is a complex and tightly regulated process. It involves a cascade of enzymatic reactions, each dependent on the activation of the previous factor. This cascade allows for a rapid amplification of the coagulation response, ensuring an efficient and timely formation of a clot to stop bleeding.
The intrinsic pathway is also subject to several regulatory mechanisms, including the activation of inhibitors, such as antithrombin III, and the presence of cofactors, such as protein C and protein S. These regulatory mechanisms ensure that the coagulation process remains tightly controlled and that excessive clot formation is prevented.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Coagulation factor XII | A coagulation factor XII that is encoded in the genome of human. [PRO:DNx, UniProtKB:P00748] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| 4-methylumbelliferyl acetate | 4-methylumbelliferyl acetate : An acetate ester consiting of umbelliferone carrying a 7-O-acetyl group. | acetate ester; coumarins | plant metabolite |
| diacetyl | butane-2,3-dione : An alpha-diketone that is butane substituted by oxo groups at positions 2 and 3. It is a metabolite produced during the malolactic fermentation. | alpha-diketone | Escherichia coli metabolite; Saccharomyces cerevisiae metabolite |
| 6,7-dichloroquinoxaline-2,3-dione | quinoxaline derivative | ||
| tacrine | tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease. Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders. | acridines; aromatic amine | EC 3.1.1.7 (acetylcholinesterase) inhibitor |
| ethacridine | Ethacridine: A topically applied anti-infective agent. | acridines | |
| benzophenone | benzophenone : The simplest member of the class of benzophenones, being formaldehyde in which both hydrogens are replaced by phenyl groups. | benzophenones | photosensitizing agent; plant metabolite |
| gabexate | Gabexate: A serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin. | benzoate ester | |
| nafamostat | nafamostat: inhibitor of trypsin, plasmin, pancreatic kallikrein, plasma kallikrein & thrombin; strongly inhibits esterolytic activities of C1r & C1 esterase complement-mediated hemolysis; antineoplastic | benzoic acids; guanidines | |
| quinone | 1,4-benzoquinone : The simplest member of the class of 1,4-benzoquinones, obtained by the formal oxidation of hydroquinone to the corresponding diketone. It is a metabolite of benzene. benzoquinone : The simplest members of the class of benzoquinones, consisting of cyclohexadiene which is substituted by two oxo groups. quinone : Compounds having a fully conjugated cyclic dione structure, such as that of benzoquinones, derived from aromatic compounds by conversion of an even number of -CH= groups into -C(=O)- groups with any necessary rearrangement of double bonds (polycyclic and heterocyclic analogues are included). | 1,4-benzoquinones | cofactor; human xenobiotic metabolite; mouse metabolite |
| acenaphthenequinone | acenaphthoquinone : An orthoquinone that is the 1,2-dioxo derivative of acenaphthene. | orthoquinones | chain carrier; epitope |
| 9,10-phenanthrenequinone | 9,10-phenanthrenequinone: structure | phenanthrenes | |
| 5-bromoisatin | indoles | anticoronaviral agent | |
| isatin | tribulin: endogenous MONOAMINE OXIDASE inhibitory activity extractable into ethyl acetate found in brain and many mammalian tissues and fluids; ISATIN is a major component; produced in excess following alcohol withdrawal; | indoledione | EC 1.4.3.4 (monoamine oxidase) inhibitor; plant metabolite |
| chloranil | Chloranil: A quinone fungicide used for treatment of seeds and foliage. tetrachloro-1,4-benzoquinone : A member of the class of 1,4-benzoquiones that is 1,4-benzoquinone in which all four hydrogens are substituted by chlorines. | 1,4-benzoquinones; organochlorine compound | EC 2.7.1.33 (pantothenate kinase) inhibitor; metabolite |
| benzoin | benzoins; secondary alpha-hydroxy ketone | EC 3.1.1.1 (carboxylesterase) inhibitor | |
| dibenzoylmethane | dibenzoylmethane : A beta-diketone that is acetylacetone (acac) in which both methyl groups have been replaced by phenyl groups. It is a minor constituent of the root extract of licorice (Glycyrrhiza glabra) and exhibits antimutagenic and anticancer effects. | aromatic ketone; beta-diketone | antimutagen; antineoplastic agent; metabolite |
| benzil | benzil : An alpha-diketone that is ethane-1,2-dione substituted by phenyl groups at positions 1 and 2 respectively. benzil: structure | alpha-diketone; aromatic ketone | |
| 1,3-cyclohexanedione | 1,3-cyclohexanedione: structure cyclohexane-1,3-dione : A cyclohexanedione carrying oxo substituents at positions 1 and 3. | beta-diketone; cyclohexanedione | |
| dibromsalicil | dibromsalicil: brominated salicyclic acid deriv; antiplaque antiseptic | ||
| 1,2-naphthoquinone | 1,2-naphthoquinone : The parent structure of the family of 1,2-naphthoquinones, in which the oxo groups of the quinone moiety are at positions 1 and 2 of the naphthalene ring. It is a metabolite of naphthalene and is found in diesel exhaust particles. naphthalene-1,2-dione: structure given in first source | 1,2-naphthoquinones | aryl hydrocarbon receptor agonist; carcinogenic agent |
| 1-acetylisatin | 1-acetylisatin: structure in first source | indoledione | |
| 1-phenyl-1,2-propanedione | 1-phenyl-1,2-propanedione : An alpha-diketone that consists of 1-phenylpropane bearing keto substituents at positions 1 and 2. It is found in coffee. 1-phenyl-1,2-propanedione: an oxoglutarate carrier antagonist | alpha-diketone; aromatic ketone | plant metabolite |
| 2,3-pentanedione | pentane-2,3-dione : An alpha-diketone that is pentane substituted at the 2- and 3-positions by oxo groups. | alpha-diketone; methyl ketone | flavouring agent |
| 5-methylisatin | 5-methylisatin: structure in first source | ||
| n-methylisatin | N-methylisatin: structure given in first source | ||
| 9-amino-6-chloro-2-methoxyacridine | |||
| acetylacetone | acetylacetone : A beta-diketone that is pentane in which the hydrogens at positions 2 and 4 are replaced by oxo groups. | beta-diketone | |
| 5-Methoxyisatin | indoles | anticoronaviral agent | |
| 3-methyl-1,2-cyclopentanedione | 3-methyl-1,2-cyclopentanedione: a peroxynitrite scavenger isolated from coffee extract; structure in first source | cyclic ketone | |
| 4-benzoylbenzoic acid | 4-carboxybenzophenone: a photosensitizer agent | ||
| 1,10-phenanthroline-5,6-dione | 1,10-phenanthroline-5,6-dione: has antineoplastic, intercalating, and trypanocidal activities; structure given in first source | ||
| 2-chloranil | |||
| 3,5-di-tert-butyl-1,2-benzoquinone | |||
| 5-Chloro-1H-indole-2,3-dione | indoles | anticoronaviral agent | |
| 5-iodoisatin | 5-iodoisatin: structure in first source | indoles | anticoronaviral agent |
| 2,2-dimethoxy-2-phenylacetophenone | |||
| anisoin | |||
| hydrobenzoin | hydrobenzoin: structure in first source | ethanediol | |
| gidazepam | gidazepam: prodrug for 7-bromo-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepine-2-one | ||
| 1,3-indandione | 1,2-indanedione: use for detection of latent fingerprints on porous surfaces; structure in first source | ||
| dabigatran | 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: A THROMBIN inhibitor which acts by binding and blocking thrombogenic activity and the prevention of thrombus formation. It is used to reduce the risk of stroke and systemic EMBOLISM in patients with nonvalvular atrial fibrillation. | aromatic amide; benzimidazoles; beta-alanine derivative; carboxamidine; pyridines | anticoagulant; EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor; EC 3.4.21.5 (thrombin) inhibitor |
| 5-Fluoroisatin | indoles | anticoronaviral agent | |
| N-malonylanthranilic acid | dicarboxylic acid monoamide | ||
| 2-[2-[4-(2-fluorophenyl)-1-piperazinyl]-2-oxoethyl]-1,1-dioxo-1,2-benzothiazol-3-one | piperazines | ||
| 1-(4-fluorophenyl)-2-[[4-(2-furanylmethyl)-5-(phenoxymethyl)-1,2,4-triazol-3-yl]thio]ethanone | aromatic ketone | ||
| (4-Methyl-2-oxochromen-7-yl) furan-2-carboxylate | coumarins | anticoronaviral agent | |
| 3,4,5-trimethoxybenzoic acid [(3,5-dimethyl-4-oxo-1-cyclohexa-2,5-dienylidene)amino] ester | trihydroxybenzoic acid | ||
| 5-bromo-N-(4-propan-2-ylphenyl)-2-furancarboxamide | aromatic amide; furans | ||
| 2-furancarboxylic acid (2-acetyl-1-benzothiophen-3-yl) ester | carboxylic ester | ||
| (5-amino-3-phenyl-1,2,4-triazol-1-yl)-(2-methoxyphenyl)methanone | triazoles | ||
| (3-amino-1,2,4-triazol-4-yl)-(2,5-dimethylphenyl)methanone | benzoic acids | ||
| 3-[[(5-bromo-2-furanyl)-oxomethyl]amino]-2-methylbenzoic acid | aromatic amide; furans | ||
| 2-[[4-(4-methylphenyl)sulfonyl-1-piperazinyl]methyl]-4-propan-2-ylphenol | sulfonamide | ||
| 3-(1-piperidinylsulfonyl)-N-(2-thiazolyl)benzamide | sulfonamide | ||
| 2-[[2-(3,4-dimethylanilino)-2-oxoethyl]thio]acetamide | anilide | ||
| 2-furanyl-[4-(4-phenoxyphenyl)sulfonyl-1-piperazinyl]methanone | aromatic ether | ||
| N-(4-fluorophenyl)-3-([1,2,4]triazolo[4,3-a]quinolin-1-ylthio)propanamide | quinolines | ||
| LSM-32435 | triazolopyrimidines | ||
| 1-[1-ethyl-6-methyl-4-(4-phenyl-1-piperazinyl)-2-sulfanylidene-5-pyrimidinyl]ethanone | piperazines | ||
| 1-[(3,4-dichlorophenyl)methyl]indole-2,3-dione | indoles | ||
| 2-[[cyclohexyl(oxo)methyl]amino]acetic acid [2-(4-cyanoanilino)-2-oxoethyl] ester | depsipeptide | ||
| 6-(4-bromophenyl)-3-methyl-1-[2-(2H-tetrazol-5-yl)ethyl]-4-(trifluoromethyl)pyrazolo[3,4-b]pyridine | phenylpyridine | ||
| 2-ethoxy-N-[4-(2-pyrimidinylsulfamoyl)phenyl]acetamide | sulfonamide | ||
| 3-[[(4-tert-butylphenyl)-oxomethyl]amino]-1H-1,2,4-triazole-5-carboxylic acid methyl ester | benzamides | ||
| 3-(methoxymethyl)-2-benzofurancarboxylic acid [4-amino-6-(2-methylanilino)-1,3,5-triazin-2-yl]methyl ester | benzofurans | ||
| 3-chloro-1-(4-methoxyphenyl)-4-(3-methyl-1-piperidinyl)pyrrole-2,5-dione | maleimides | ||
| 2-[3-(2-chloro-6-fluorophenyl)-5-methyl-4-isoxazolyl]-5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazole | (trifluoromethyl)benzenes | ||
| N-[2-furanyl-(8-hydroxy-7-quinolinyl)methyl]-2-methylpropanamide | hydroxyquinoline | ||
| 4-(1-methyl-3-indolyl)-N-propan-2-ylbutanamide | indoles | ||
| 1-(2,1,3-benzothiadiazol-4-ylsulfonyl)-N-(6-methyl-1,3-benzothiazol-2-yl)-3-piperidinecarboxamide | benzothiadiazole | ||
| 1-cyclopentyl-N-[2-(3,4-dihydro-1H-isoquinolin-2-yl)ethyl]-5-oxo-3-pyrrolidinecarboxamide | isoquinolines | ||
| 4-[2-(1-cyclohexenyl)ethyl]-1-cyclohexyl-3-pyridin-4-ylpiperazine-2,5-dione | piperazines; pyridines | ||
| N-(3-acetylphenyl)-3,5-dimethyl-4-isoxazolesulfonamide | aromatic ketone | ||
| N-[1-(cyclohexylamino)-2-methyl-1-oxobutan-2-yl]-N-(2-furanylmethyl)-2-pyridinecarboxamide | organonitrogen compound; organooxygen compound | ||
| N-(2-methylphenyl)-1-phenazinecarboxamide | phenazines | ||
| 5-Nitroisatin | indoles | anticoronaviral agent | |
| 1-(3,4-dihydro-1H-isoquinolin-2-yl)-2-[[5-methyl-2-(4-methylphenyl)-4-oxazolyl]methylsulfonyl]ethanone | 1,3-oxazoles | ||
| phenylalanyl-prolyl-arginine methyl chloride | phenylalanyl-prolyl-arginine methyl chloride: selective affinity label for thrombin; RN given refers to parent (L-Pro-D-Phe-(S))-isomer | ||
| 1-(3-methoxyphenyl)-3-[2-(methylthio)phenyl]urea | ureas | ||
| 5-Chloro-3-pyridinyl 2-furoate | carboxylic ester | anticoronaviral agent | |
| rivaroxaban | 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: A morpholine and thiophene derivative that functions as a FACTOR XA INHIBITOR and is used in the treatment and prevention of DEEP-VEIN THROMBOSIS and PULMONARY EMBOLISM. It is also used for the prevention of STROKE and systemic embolization in patients with non-valvular ATRIAL FIBRILLATION, and for the prevention of atherothrombotic events in patients after an ACUTE CORONARY SYNDROME. | aromatic amide; lactam; monocarboxylic acid amide; morpholines; organochlorine compound; oxazolidinone; thiophenes | anticoagulant; EC 3.4.21.6 (coagulation factor Xa) inhibitor |
| N-[4-(6-chloro-5-nitro-1H-benzimidazol-2-yl)phenyl]acetamide | benzimidazoles |