Protein / target
Antithrombin-III
Protein at a glance
Biological role
Serine-type endopeptidase inhibitor activity
Primary system
Haematologic system
Strongest disease association
Reduced antithrombin III activity
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
10 approved · 2 in clinical development
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
Most important serine protease inhibitor in plasma that regulates the blood coagulation cascade (PubMed:15140129, PubMed:15853774). AT-III inhibits thrombin, matriptase-3/TMPRSS7, as well as factors IXa, Xa and XIa (PubMed:15140129). Its inhibitory activity is greatly enhanced in the presence of heparin
Subcellular location
Domains and Gene Ontology detail (13)Hide
Gene Ontology
- Cblood microparticle
- Cendoplasmic reticulum lumen
- Cextracellular exosome
- Cextracellular matrix
- Cextracellular region
- Cextracellular space
- Cplasma membrane
- Fheparin binding
- Fidentical protein binding
- Fprotease binding
- Fserine-type endopeptidase inhibitor activity
- Pblood coagulation
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
View supporting evidenceHide supporting evidence
Haemostasis
- ·Most important serine protease inhibitor in plasma that regulates the blood coagulation…
- ·blood coagulation
- ·regulation of blood coagulation
- ·Fibrin formation
Proteolysis
- ·Most important serine protease inhibitor in plasma that regulates the blood coagulation…
- ·protease binding
Kinase signalling
- ·Post-translational protein phosphorylation
Cell adhesion
- ·extracellular matrix
View underlying pathways (6)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Drugs targeting this protein
Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.
Antithrombin-III activator
Antithrombin-III activator
ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.
Translational evidence
Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.
Strongest genetic associations
Human genetic evidence — the most direct causal link between this target and a disease.
Highest-confidence therapeutic associations
Diseases where a drug acting on this target has already reached clinical development.
Show all associationsHide all associations
Open Targets ranks 1,117 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.
Known drugs · 12 total
Venous thrombosis · Thromboembolism · deep vein thrombosis
deep vein thrombosis · Recurrent thrombophlebitis · venous thromboembolism
deep vein thrombosis · venous thromboembolism · Recurrent thrombophlebitis
deep vein thrombosis · venous thromboembolism · Venous thrombosis
pulmonary embolism · deep vein thrombosis
hemophilia · hemophilia A · hemophilia B
Recurrent thrombophlebitis · blood coagulation disease · venous thromboembolism
blood coagulation disease · thrombotic disease · myocardial infarction
Recurrent thrombophlebitis · Thrombocytopenia
Recurrent thrombophlebitis · myocardial infarction · angina unstable
Tractability
Safety liabilities
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.
Show remaining trials (24)Hide
ClinicalTrials.gov via the drug-target graph.
Forefront confidence
Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.
This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.
What's happening now
Recent activity around this target, drawn from one canonical event stream. Every item is reached through 2 drugs that target this protein, so each event is news about that drug rather than about the protein directly.
- New publicationAmerican Society of Hematology 2021 guidelines on the use of anticoagulation for thromboprophylaxis in patients with COVID-19.
- New publicationApixaban for the Treatment of Venous Thromboembolism Associated with Cancer.
- New publicationEdoxaban for the Treatment of Cancer-Associated Venous Thromboembolism.
- Regulatory approval
Approval: Inhixa (EMA)
- New publicationPredicting the risk of venous thromboembolism in patients hospitalized with heart failure.
- New publicationD-dimer as a predictor of venous thromboembolism in acutely ill, hospitalized patients: a subanalysis of the randomized controlled MAGELLAN trial.
- New publicationRivaroxaban for thromboprophylaxis in acutely ill medical patients.
- New publicationPrediction and prevention of thromboembolic events with enoxaparin in cancer patients with elevated tissue factor-bearing microparticles: a randomized-controlled phase II trial (the Microtec study).
- New publicationRivaroxaban versus enoxaparin for thromboprophylaxis after total knee arthroplasty (RECORD4): a randomised trial.
- New publicationLow-molecular-weight heparin versus a coumarin for the prevention of recurrent venous thromboembolism in patients with cancer.
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.