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Protein / target

Receptor-type tyrosine-protein kinase FLT3

Encoded byFLT3P36888Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
16
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Transmembrane receptor protein tyrosine kinase

Strongest disease association

Hypothyroidism

Via encoding gene FLT3 · Genetic evidence · score 0.93

Therapeutic position

Established drug target

Small molecules and antibodies

Research activity

Emerging research

2 papers · latest 2019

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

Tyrosine-protein kinase that acts as a cell-surface receptor for the cytokine FLT3LG and regulates differentiation, proliferation and survival of hematopoietic progenitor cells and of dendritic cells.

View complete UniProt function annotation

Tyrosine-protein kinase that acts as a cell-surface receptor for the cytokine FLT3LG and regulates differentiation, proliferation and survival of hematopoietic progenitor cells and of dendritic cells. Promotes phosphorylation of SHC1 and AKT1, and activation of the downstream effector MTOR. Promotes activation of RAS signaling and phosphorylation of downstream kinases, including MAPK1/ERK2 and/or MAPK3/ERK1. Promotes phosphorylation of FES, FER, PTPN6/SHP, PTPN11/SHP-2, PLCG1, and STAT5A and/or STAT5B. Activation of wild-type FLT3 causes only marginal activation of STAT5A or STAT5B. Mutations that cause constitutive kinase activity promote cell proliferation and resistance to apoptosis via the activation of multiple signaling pathways

Subcellular location

MembraneEndoplasmic reticulum lumen
Domains and Gene Ontology detail (37)

Domains & features

Ig-like C2-typeProtein kinase

Gene Ontology

  • Cendoplasmic reticulum lumen
  • Cendosome membrane
  • Cplasma membrane
  • Creceptor complex
  • FATP binding
  • Fcytokine receptor activity
  • Fgrowth factor binding
  • Fnuclear glucocorticoid receptor binding
  • Fphosphatidylinositol 3-kinase activator activity
  • Fprotein tyrosine kinase activity
  • Fprotein-containing complex binding
  • Ftransmembrane receptor protein tyrosine kinase activity

993 aa · 113 kDa · 2 isoforms

Biological roles

Reactome v97

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Cell proliferation & survivalGO · ReactomeReceptor tyrosine kinase signallingGOCell migrationGOOncogenic signallingReactomeImmune signallingUniProt · GO
View supporting evidence

Cell proliferation & survival

  • ·positive regulation of cell population proliferation
  • ·PIP3 activates AKT signaling
  • ·PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling

Receptor tyrosine kinase signalling

  • ·transmembrane receptor protein tyrosine kinase activity
  • ·cell surface receptor protein tyrosine kinase signaling pathway

Cell migration

  • ·cell migration

Oncogenic signalling

  • ·Constitutive Signaling by Aberrant PI3K in Cancer

Immune signalling

  • ·Tyrosine-protein kinase that acts as a cell-surface receptor for the cytokine FLT3LG and…
  • ·cytokine receptor activity
  • ·B cell differentiation
  • ·cellular response to cytokine stimulus
View underlying pathways (25)

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Interaction neighbourhood

STRING v12.0

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.

FLT3LGKITLGCEBPAGRB2STAT3STAT5ASTAT5BSPI1PIK3CAPIK3R1FLT3

10 strongest partners — larger node and heavier line mean higher confidence

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

4 medicines · 7 areas

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.

Carcinoma, Renal Cell1 medicine
Gastrointestinal Stromal Tumors1 medicine
Leukemia, Myeloid, Acute1 medicine
Mastocytosis1 medicine
Mastocytosis, Systemic1 medicine
Neuroendocrine Tumors1 medicine

16 medicines meet Open Targets' target-level approved-medicine definition; the 4 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

4

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.

pexidartinib
Narrow target profileApprovedInhibitor

Tyrosine-protein kinase receptor FLT3 inhibitor

Indicated for Neoplasms

Direct interaction with this protein · 1 of 3 recorded protein targets — narrow recorded profile

gilteritinib
Narrow target profileApprovedInhibitor

Tyrosine-protein kinase receptor FLT3 inhibitor

Indicated for Neoplasms

Direct interaction with this protein · 1 of 2 recorded protein targets — narrow recorded profile

sunitinib
ApprovedInhibitor

Tyrosine-protein kinase receptor FLT3 inhibitor

Indicated for Carcinoma, Renal Cell, Gastrointestinal Stromal Tumors, Neuroendocrine Tumors, Neoplasms

Direct interaction with this protein · 1 of 9 recorded protein targets — broad pharmacology

midostaurin
ApprovedInhibitor

Tyrosine-protein kinase receptor FLT3 inhibitor

Indicated for Leukemia, Myeloid, Acute, Mastocytosis, Mastocytosis, Systemic, Neoplasms

Direct interaction with this protein · 1 of 16 recorded protein targets — broad pharmacology

ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.

Translational evidence

Open Targets 26

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 FLT3

Gene-level evidence surfaced through the gene FLT3that 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.

Leukemia, Myeloid, Acute
0.98Well supported

Clinical evidence dominant · Open Targets 0.84

Hypothyroidism
0.93Well supported

Genetic evidence dominant · Open Targets 0.57

Neoplasms
0.90Well supported

Clinical evidence dominant · Open Targets 0.65

Carcinoma, Hepatocellular
0.82Well supported

Clinical evidence dominant · Open Targets 0.67

Myelofibrosis
0.82Well supported

Clinical evidence dominant · Open Targets 0.62

View evidence synthesis (5)
Leukemia, Myeloid, AcuteWell supported
0.98
agreement 0.901.00
Clinical28%Somatic mutation22%Genetic21%Pathway13%Animal model10%Literature6%Genetic literaturedup

Open Targets aggregate 0.84 · 6 independent evidence families · 1 not counted as duplicate

HypothyroidismWell supported
0.93
agreement 0.791.00
Genetic99%Literature1%

Open Targets aggregate 0.57 · 2 independent evidence families

NeoplasmsWell supported
0.90
agreement 0.800.99
Clinical45%Pathway25%Genetic23%Literature8%

Open Targets aggregate 0.65 · 4 independent evidence families

Carcinoma, HepatocellularWell supported
0.82
agreement 0.700.94
Clinical66%Somatic mutation27%Literature7%

Open Targets aggregate 0.67 · 3 independent evidence families

MyelofibrosisWell supported
0.82
agreement 0.710.92
Clinical58%Somatic mutation25%Animal model15%Literature2%

Open Targets aggregate 0.62 · 4 independent evidence families

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.

Show all associations
Leukemia, Myeloid, Acute0.84
Carcinoma, Hepatocellular0.67
Gastrointestinal Stromal Tumors0.65
Neoplasms0.65
Carcinoma, Renal Cell0.64
Myelofibrosis0.62
Precursor Cell Lymphoblastic Leukemia-Lymphoma0.60
Primary myelofibrosis0.57
Hypothyroidism0.57

Drug development

45 compounds recorded · 16 approved · 29 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 4 drugs that target this protein in Forefront's canonical graph (4 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (10)
QUIZARTINIB DIHYDROCHLORIDEApproval
NINGETINIBPhase 2
CEP-2563Phase 1
RUSERONTINIBPhase 3
PACRITINIB CITRATEApproval
FORETINIBPhase 2
CM-082Phase 2
PACRITINIBApproval
AT-9283Phase 3
SUNITINIBApproval

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 moleculesStrong

Approved Drug and Structure with Ligand support this modality.

AntibodiesSupported

Phase 1 Clinical and GO CC high conf support this modality.

Protein degradersEmerging

Feasibility evidence (literature and uniprot ubiquitination) — no clinical-stage drug of this modality recorded.

Other modalitiesStrong

Advanced Clinical support this modality.

View underlying tractability evidence (13)
SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Med-Quality PocketSM · Druggable FamilyAB · Phase 1 ClinicalAB · GO CC high confAB · UniProt SigP or TMHMMPR · LiteraturePR · UniProt UbiquitinationPR · Database UbiquitinationPR · Small Molecule BinderOC · Advanced Clinical

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

myelosuppressionClinPGx

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

30

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.

View all trials (26)

RECRUITING · via gilteritinib · NCT03013998

ACTIVE_NOT_RECRUITING · via sunitinib · NCT02465060

ACTIVE_NOT_RECRUITING · via sunitinib · NCT01396408

ClinicalTrials.gov via the drug-target graph.

What's happening now

12

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 3 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.

  1. New publication2024-05-03
    Machine-learning and mechanistic modeling of metastatic breast cancer after neoadjuvant treatment.

    PLoS computational biology · 2024 · 10 citations · Europe PMC · via sunitinib

  2. New publication2024-01-05
    Genomic profiling in GIST: Implications in clinical outcome and future challenges.

    Neoplasia (New York, N.Y.) · 2024 · 20 citations · Europe PMC · via sunitinib

  3. New publication2021-03-01
    Nivolumab plus Cabozantinib versus Sunitinib for Advanced Renal-Cell Carcinoma.

    The New England journal of medicine · 2021 · 1,297 citations · Europe PMC · via sunitinib

  4. Regulatory approval2021-02-11

    Approval: Sunitinib Accord (EMA)

    ema · regulatory · ema · via sunitinib

  5. Regulatory approval2019-10-24

    Approval: Xospata (EMA)

    ema · regulatory · ema · via gilteritinib

  6. New publication2019-10-01
    Gilteritinib or Chemotherapy for Relapsed or Refractory <i>FLT3</i>-Mutated AML.

    The New England journal of medicine · 2019 · 966 citations · Europe PMC · via gilteritinib

  7. New publication2019-02-16
    Pembrolizumab plus Axitinib versus Sunitinib for Advanced Renal-Cell Carcinoma.

    The New England journal of medicine · 2019 · 2,427 citations · Europe PMC · via sunitinib

  8. New publication2018-03-21
    Nivolumab plus Ipilimumab versus Sunitinib in Advanced Renal-Cell Carcinoma.

    The New England journal of medicine · 2018 · 3,404 citations · Europe PMC · via sunitinib

  9. Regulatory approval2017-09-18

    Approval: Rydapt (EMA)

    ema · regulatory · ema · via midostaurin

  10. New publication2016-06-01
    Efficacy and Safety of Midostaurin in Advanced Systemic Mastocytosis.

    The New England journal of medicine · 2016 · 371 citations · Europe PMC · via midostaurin

  11. Regulatory approval2006-07-19

    Approval: Sutent (EMA)

    ema · regulatory · ema · via sunitinib

  12. New publication2005-12-05
    Activity of SU11248, a multitargeted inhibitor of vascular endothelial growth factor receptor and platelet-derived growth factor receptor, in patients with metastatic renal cell carcinoma.

    Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2006 · 1,110 citations · Europe PMC · via sunitinib

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.

Research activity

2 papers · to 2019

Papers linked directly to this protein. This is the protein's own literature — descriptor-derived papers are kept separate below.

Most cited

Perl AE · The New England journal of medicine · 2019

Krause DS · The New England journal of medicine · 2005

Recent

Gilteritinib or Chemotherapy for Relapsed or Refractory <i>FLT3</i>-Mutated AML.

Perl AE · The New England journal of medicine · 2019

Tyrosine kinases as targets for cancer therapy.

Krause DS · The New England journal of medicine · 2005

Europe PMC papers linked directly to this protein.