Prothrombin

A prothrombin that is encoded in the genome of human. [PRO:DNx, UniProtKB:P00734]

Synonyms

EC 3.4.21.5;
Coagulation factor II

Research

Bioassay Publications (139)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	33 (23.74)	18.2507
2000's	60 (43.17)	29.6817
2010's	40 (28.78)	24.3611
2020's	6 (4.32)	2.80

Compounds (75)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
5-(n,n-hexamethylene)amiloride	Homo sapiens (human)	IC50	10.0000	1	1
benzamidine	Homo sapiens (human)	Ki	64.9600	4	4
bis(5-amidino-2-benzimidazolyl)methane	Homo sapiens (human)	IC50	31.0000	1	1
bis(5-amidino-2-benzimidazolyl)methane	Homo sapiens (human)	Ki	238.7599	1	12
camostat	Homo sapiens (human)	IC50	0.3990	2	2
camostat	Homo sapiens (human)	Ki	3.4394	1	6
fidexaban	Homo sapiens (human)	Ki	2.0000	2	2
n(alpha)-(2-naphthylsulfonylglycyl)-4-amidinophenylalanine piperidide	Homo sapiens (human)	IC50	0.6900	1	1
nafamostat	Homo sapiens (human)	IC50	1.9000	1	1
sulfaguanidine	Homo sapiens (human)	Ki	0.0950	1	1
proflavine	Homo sapiens (human)	IC50	12.0000	1	1
catechin	Homo sapiens (human)	IC50	125.0000	1	1
isoquinoline-1,3,4-trione	Homo sapiens (human)	IC50	5.0000	1	1
diphenylcarbazone	Homo sapiens (human)	Ki	1.7000	1	1
dibrompropamidine	Homo sapiens (human)	Ki	0.9460	1	1
amiloride	Homo sapiens (human)	IC50	135.0000	2	2
captopril	Homo sapiens (human)	Ki	0.0480	1	1
1,2-di(5-amidino-2-benzofuranyl)ethane	Homo sapiens (human)	IC50	5.0000	1	1
hexamidine	Homo sapiens (human)	Ki	0.2240	1	1
inogatran	Homo sapiens (human)	IC50	7.9057	3	3
inogatran	Homo sapiens (human)	Ki	0.0114	3	3
epicatechin	Homo sapiens (human)	IC50	150.0000	1	1
p-Aminobenzamidine dihydrochloride	Homo sapiens (human)	Ki	95.0000	1	1
mci 9038	Homo sapiens (human)	IC50	0.2200	12	12
mci 9038	Homo sapiens (human)	Ki	0.0184	9	9
sivelestat	Homo sapiens (human)	IC50	2.0000	1	1
dx 9065	Homo sapiens (human)	IC50	1,366.6667	3	3
dx 9065	Homo sapiens (human)	Ki	1,334.5000	6	6
efegatran	Homo sapiens (human)	IC50	0.0351	8	8
efegatran	Homo sapiens (human)	Ki	0.0128	6	6
acetylphenylalanyl-prolyl-boroarginine	Homo sapiens (human)	Ki	0.0000	3	3
cyanidin	Homo sapiens (human)	IC50	0.2500	1	1
foy 251	Homo sapiens (human)	IC50	107.5000	1	1
homonojirimycin	Homo sapiens (human)	IC50	34.0000	1	1
l 694,458	Homo sapiens (human)	IC50	78.7600	1	1
melagatran	Homo sapiens (human)	IC50	0.5239	8	10
melagatran	Homo sapiens (human)	Ki	0.0016	4	4
pefabloc	Homo sapiens (human)	IC50	62.0000	1	1
razaxaban	Homo sapiens (human)	Ki	4.8322	9	18
dabigatran	Homo sapiens (human)	IC50	0.0046	12	12
dabigatran	Homo sapiens (human)	Ki	0.0050	7	7
sitosterol, (3beta)-isomer	Homo sapiens (human)	IC50	754.9250	4	4
sitosterol, (3beta)-isomer	Homo sapiens (human)	Ki	0.2672	1	1
bortezomib	Homo sapiens (human)	Ki	13.0000	1	1
benzamidine	Homo sapiens (human)	IC50	440.0000	1	1
benzamidine	Homo sapiens (human)	Ki	155.1385	3	13
phenylalanyl-prolyl-arginine	Homo sapiens (human)	IC50	0.0000	1	1
tosylarginine methyl ester	Homo sapiens (human)	IC50	89.0000	1	1
telaprevir	Homo sapiens (human)	IC50	1.0000	1	1
bradykinin (1-5)	Homo sapiens (human)	IC50	601.0000	1	1
silybin	Homo sapiens (human)	IC50	22.9500	2	2
quercetin	Homo sapiens (human)	IC50	15.7500	2	2
camostat mesylate	Homo sapiens (human)	IC50	31.6000	1	1
cyclotheonamide a	Homo sapiens (human)	IC50	0.7615	2	2
cyclotheonamide a	Homo sapiens (human)	Ki	0.0905	2	2
ximelagatran	Homo sapiens (human)	Ki	0.0020	1	1
otamixaban	Homo sapiens (human)	Ki	4.0000	1	1
bms 740808	Homo sapiens (human)	Ki	0.0350	2	2
napsagatran	Homo sapiens (human)	Ki	0.0003	2	2
talabostat	Homo sapiens (human)	Ki	0.0020	1	1
n,n-(4-xylylidene)bisaminoguanidine	Homo sapiens (human)	Ki	68.0000	1	1
ym 60828	Homo sapiens (human)	IC50	0.0077	1	1
ym 60828	Homo sapiens (human)	Ki	40.0000	3	3
rivaroxaban	Homo sapiens (human)	Ki	1.0000	1	1
n-alpha-(2,4,6-triisopropyl-phenylsulfonyl)-3-amidino-(l)-phenyl-alanine-4-ethoxycarbonyl-piperazide hydrochloride	Homo sapiens (human)	Ki	0.4900	2	2
dpc 423	Homo sapiens (human)	Ki	4.7321	5	10
gw 813893	Homo sapiens (human)	Ki	0.3670	2	2
l 374087	Homo sapiens (human)	Ki	0.0005	7	7
darexaban	Homo sapiens (human)	Ki	100.0000	1	1
lb 30057	Homo sapiens (human)	Ki	0.0004	6	6
darexaban glucuronide	Homo sapiens (human)	Ki	100.0000	1	1
apixaban	Homo sapiens (human)	Ki	2.3250	3	4
betrixaban	Homo sapiens (human)	IC50	11.5045	4	4
rpr 120844	Homo sapiens (human)	Ki	1.0000	1	1
n-(3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl)-3-(2-((((1,1-dimethylethyl)amino)carbonyl)amino)-3,3-dimethyl-1-oxobutyl)-6,6-dimethyl-3-azabicyclo(3.1.0)hexan-2-carboxamide	Homo sapiens (human)	IC50	1.0000	1	1
(z,z)-babch	Homo sapiens (human)	Ki	0.5050	4	4
anabaenopeptin b	Homo sapiens (human)	IC50	1.6000	1	1
dysinosin a	Homo sapiens (human)	IC50	0.0460	1	1
dysinosin a	Homo sapiens (human)	Ki	0.4510	2	2
PF-00835231	Homo sapiens (human)	IC50	10.0000	1	1
mk-7009	Homo sapiens (human)	IC50	100.0000	1	1
grassystatin a	Homo sapiens (human)	IC50	10.0000	1	1
rpx7009	Homo sapiens (human)	IC50	1,000.0000	1	1

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
benzamidine	Homo sapiens (human)	Kd	405.0000	2	2
triiodothyronine	Homo sapiens (human)	EC50	0.0029	3	3
catechin	Homo sapiens (human)	Kd	49.2000	1	1
glutamic acid	Homo sapiens (human)	EC50	7.4000	1	1
epicatechin	Homo sapiens (human)	Kd	5,190.0000	1	1
p-Aminobenzamidine dihydrochloride	Homo sapiens (human)	Kd	78.0000	1	1
mci 9038	Homo sapiens (human)	Kd	0.0024	1	1
acetylphenylalanyl-prolyl-boroarginine	Homo sapiens (human)	Kd	0.0000	1	1
cyanidin	Homo sapiens (human)	Kd	0.0078	1	1
melagatran	Homo sapiens (human)	Kd	0.0013	1	1
silybin	Homo sapiens (human)	Kd	18.6000	1	1
quercetin	Homo sapiens (human)	Kd	0.0387	1	1

Drugs with Other Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
camptothecin	Homo sapiens (human)	MIC	100.0000	1	1
etoposide	Homo sapiens (human)	MIC	0.1000	1	1
telaprevir	Homo sapiens (human)	IC90	1.0000	1	1
bms-262084	Homo sapiens (human)	Selectivity	2.6250	1	1
n-(3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl)-3-(2-((((1,1-dimethylethyl)amino)carbonyl)amino)-3,3-dimethyl-1-oxobutyl)-6,6-dimethyl-3-azabicyclo(3.1.0)hexan-2-carboxamide	Homo sapiens (human)	IC90	1.4000	1	1
mk-7009	Homo sapiens (human)	IC90	100.0000	1	1

Enables

This protein enables 8 target(s):

Target	Category	Definition
lipopolysaccharide binding	molecular function	Binding to a lipopolysaccharide. [PMID:11079463]
serine-type endopeptidase activity	molecular function	Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a catalytic mechanism that involves a catalytic triad consisting of a serine nucleophile that is activated by a proton relay involving an acidic residue (e.g. aspartate or glutamate) and a basic residue (usually histidine). [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE]
signaling receptor binding	molecular function	Binding to one or more specific sites on a receptor molecule, a macromolecule that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:bf, GOC:ceb, ISBN:0198506732]
calcium ion binding	molecular function	Binding to a calcium ion (Ca2+). [GOC:ai]
protein binding	molecular function	Binding to a protein. [GOC:go_curators]
growth factor activity	molecular function	The function that stimulates a cell to grow or proliferate. Most growth factors have other actions besides the induction of cell growth or proliferation. [ISBN:0815316194]
heparin binding	molecular function	Binding to heparin, a member of a group of glycosaminoglycans found mainly as an intracellular component of mast cells and which consist predominantly of alternating alpha-(1->4)-linked D-galactose and N-acetyl-D-glucosamine-6-sulfate residues. [GOC:jl, ISBN:0198506732]
thrombospondin receptor activity	molecular function	Combining with thrombospondin and transmitting the signal to initiate a change in cell activity. [GOC:BHF, GOC:signaling, GOC:vk]

Located In

This protein is located in 7 target(s):

Target	Category	Definition
extracellular region	cellular component	The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators]
extracellular space	cellular component	That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684]
endoplasmic reticulum lumen	cellular component	The volume enclosed by the membranes of the endoplasmic reticulum. [ISBN:0198547684]
Golgi lumen	cellular component	The volume enclosed by the membranes of any cisterna or subcompartment of the Golgi apparatus, including the cis- and trans-Golgi networks. [GOC:mah]
plasma membrane	cellular component	The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
extracellular exosome	cellular component	A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894]
blood microparticle	cellular component	A phospholipid microvesicle that is derived from any of several cell types, such as platelets, blood cells, endothelial cells, or others, and contains membrane receptors as well as other proteins characteristic of the parental cell. Microparticles are heterogeneous in size, and are characterized as microvesicles free of nucleic acids. [GOC:BHF, GOC:mah, PMID:16373184]

Active In

This protein is active in 2 target(s):

Target	Category	Definition
collagen-containing extracellular matrix	cellular component	An extracellular matrix consisting mainly of proteins (especially collagen) and glycosaminoglycans (mostly as proteoglycans) that provides not only essential physical scaffolding for the cellular constituents but can also initiate crucial biochemical and biomechanical cues required for tissue morphogenesis, differentiation and homeostasis. The components are secreted by cells in the vicinity and form a sheet underlying or overlying cells such as endothelial and epithelial cells. [GOC:BHF, GOC:rph, PMID:21123617]
extracellular space	cellular component	That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684]

Involved In

This protein is involved in 33 target(s):

Target	Category	Definition
positive regulation of protein phosphorylation	biological process	Any process that activates or increases the frequency, rate or extent of addition of phosphate groups to amino acids within a protein. [GOC:hjd]
proteolysis	biological process	The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah]
acute-phase response	biological process	An acute inflammatory response that involves non-antibody proteins whose concentrations in the plasma increase in response to infection or injury of homeothermic animals. [ISBN:0198506732]
cell surface receptor signaling pathway	biological process	The series of molecular signals initiated by an extracellular ligand binding to a receptor located on the cell surface. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:signaling]
G protein-coupled receptor signaling pathway	biological process	The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor]
blood coagulation	biological process	The sequential process in which the multiple coagulation factors of the blood interact, ultimately resulting in the formation of an insoluble fibrin clot; it may be divided into three stages: stage 1, the formation of intrinsic and extrinsic prothrombin converting principle; stage 2, the formation of thrombin; stage 3, the formation of stable fibrin polymers. [PMID:30700128]
positive regulation of cell population proliferation	biological process	Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators]
regulation of cell shape	biological process	Any process that modulates the surface configuration of a cell. [GOC:dph, GOC:go_curators, GOC:tb]
response to wounding	biological process	Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating damage to the organism. [GOC:go_curators]
negative regulation of platelet activation	biological process	Any process that decreases the rate or frequency of platelet activation. Platelet activation is a series of progressive, overlapping events triggered by exposure of the platelets to subendothelial tissue. [GOC:BHF, GOC:dph, GOC:tb]
platelet activation	biological process	A series of progressive, overlapping events triggered by exposure of the platelets to subendothelial tissue. These events include shape change, adhesiveness, aggregation, and release reactions. When carried through to completion, these events lead to the formation of a stable hemostatic plug. [http://www.graylab.ac.uk/omd/]
regulation of blood coagulation	biological process	Any process that modulates the frequency, rate or extent of blood coagulation. [GOC:mah]
positive regulation of blood coagulation	biological process	Any process that activates or increases the frequency, rate or extent of blood coagulation. [GOC:mah]
positive regulation of cell growth	biological process	Any process that activates or increases the frequency, rate, extent or direction of cell growth. [GOC:go_curators]
positive regulation of insulin secretion	biological process	Any process that activates or increases the frequency, rate or extent of the regulated release of insulin. [GOC:mah]
positive regulation of collagen biosynthetic process	biological process	Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of collagen, any of a group of fibrous proteins of very high tensile strength that form the main component of connective tissue in animals. [GOC:mah]
fibrinolysis	biological process	A process that solubilizes fibrin in the bloodstream of a multicellular organism, chiefly by the proteolytic action of plasmin. [GOC:jl, PMID:15842654]
negative regulation of proteolysis	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of the hydrolysis of a peptide bond or bonds within a protein. [GOC:go_curators]
positive regulation of receptor signaling pathway via JAK-STAT	biological process	Any process that activates or increases the frequency, rate or extent of the JAK-STAT signaling pathway activity. [GOC:bf]
negative regulation of astrocyte differentiation	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of astrocyte differentiation. [GOC:vp, PMID:15139015]
positive regulation of release of sequestered calcium ion into cytosol	biological process	Any process that activates or increases the frequency, rate or extent of the release into the cytosolic compartment of calcium ions sequestered in the endoplasmic reticulum or mitochondria. [GOC:ai]
regulation of cytosolic calcium ion concentration	biological process	Any process involved in the maintenance of an internal steady state of calcium ions within the cytosol of a cell or between the cytosol and its surroundings. [GOC:ai, GOC:mah, GOC:rph]
cytolysis by host of symbiont cells	biological process	The killing by an organism of a cell in its symbiont organism by means of the rupture of cell membranes and the loss of cytoplasm. The symbiont is defined as the smaller of the organisms involved in a symbiotic interaction. [GOC:add]
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	biological process	Any process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai]
negative regulation of fibrinolysis	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of fibrinolysis, an ongoing process that solubilizes fibrin, resulting in the removal of small blood clots. [GOC:ai]
antimicrobial humoral immune response mediated by antimicrobial peptide	biological process	An immune response against microbes mediated by anti-microbial peptides in body fluid. [PMID:15761415, PMID:24287494]
neutrophil-mediated killing of gram-negative bacterium	biological process	The directed killing of a gram-negative bacterium by a neutrophil. [GOC:add, ISBN:0781765196]
positive regulation of lipid kinase activity	biological process	Any process that increases the frequency, rate or extent of lipid kinase activity, the catalysis of the transfer of a phosphate group, usually from ATP, to a simple or complex lipid. [GOC:dph, GOC:tb]
negative regulation of cytokine production involved in inflammatory response	biological process	Any process that stops, prevents or reduces the frequency, rate or extent of cytokine production involved in inflammatory response. [GOC:TermGenie]
positive regulation of protein localization to nucleus	biological process	Any process that activates or increases the frequency, rate or extent of protein localization to nucleus. [GOC:TermGenie]
positive regulation of phospholipase C-activating G protein-coupled receptor signaling pathway	biological process	Any process that activates or increases the frequency, rate or extent of phospholipase C-activating G protein-coupled receptor signaling pathway. [GOC:BHF, GOC:TermGenie]
ligand-gated ion channel signaling pathway	biological process	The series of molecular signals initiated by activation of a ligand-gated ion channel on the surface of a cell. The pathway begins with binding of an extracellular ligand to a ligand-gated ion channel and ends with a molecular function that directly regulates a downstream cellular process, e.g. transcription. [GOC:bhm, PMID:25869137]
positive regulation of reactive oxygen species metabolic process	biological process	Any process that activates or increases the frequency, rate or extent of reactive oxygen species metabolic process. [GOC:mah]