Protein / target
Antithrombin-III
Protein at a glance
Biological role
Serine-type endopeptidase inhibitor
Strongest disease association
Hereditary antithrombin deficiency
Therapeutic position
Established drug target
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
Most important serine protease inhibitor in plasma that regulates the blood coagulation cascade.
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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.
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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
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.
Approved medicines with mapped indications
Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.
10 medicines meet Open Targets' target-level approved-medicine definition; the 2 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.
Antithrombin-III activator
Indicated for Thrombosis, Venous Thromboembolism, Venous Thrombosis
Antithrombin-III activator
Indicated for Myocardial Infarction, Pulmonary Embolism, Thrombosis, Venous Thromboembolism
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Translational evidence
Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.
Strongest disease associations · via encoding gene SERPINC1
Gene-level evidence surfaced through the gene SERPINC1 that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.
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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 per-type scores above show the calculation.
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Drug development
12 compounds recorded · 10 approved · 2 in clinical development
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Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.
Tractability
Small molecules — Emerging
Antibodies — Emerging
Protein degraders — Emerging
Other modalities — Strong
View underlying tractability evidence (8)Hide
Raw Open Targets tractability assessment buckets, by modality.
Safety-related annotations
Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.
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. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.
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ClinicalTrials.gov via the drug-target graph.
What's happening now
Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 2 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.
- 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.