Protein / target

Receptor-type tyrosine-protein kinase FLT3

FLT3P36888Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
16
Approved medicines
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Transmembrane receptor protein tyrosine kinase activity

Primary system

Immune system

Strongest disease association

hypothyroidism

Genetic evidence · score 0.93

Therapeutic maturity

Clinically validated target

16 approved medicines against this target

Druggability

Small molecule

Open Targets tractability · Approved Drug

Clinical development

16 approved · 29 in clinical development

30 linked trials

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

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.

Kinase signallingUniProt · GOImmune signallingUniProt · GOApoptosis & cell deathGO
View supporting evidence

Kinase signalling

  • ·Tyrosine-protein kinase that acts as a cell-surface receptor for the cytokine FLT3LG and…
  • ·protein tyrosine kinase activity
  • ·transmembrane receptor protein tyrosine kinase activity
  • ·peptidyl-tyrosine phosphorylation

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

Apoptosis & cell death

  • ·regulation of apoptotic process
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.

Drugs targeting this protein

3

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.

pexidartinib
Narrow target profileApprovedInhibitor

Tyrosine-protein kinase receptor FLT3 inhibitor

Appears in clinical studies involving tenosynovial giant cell tumor, diffuse type, neoplasm, Alzheimer disease, pigmented villonodular synovitis

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

gilteritinib
Narrow target profileApprovedInhibitor

Tyrosine-protein kinase receptor FLT3 inhibitor

Appears in clinical studies involving acute myeloid leukemia by FAB classification, acute myeloid leukemia, neoplasm, acute myeloid leukemia

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

sunitinib
ApprovedInhibitor

Tyrosine-protein kinase receptor FLT3 inhibitor

Appears in clinical studies involving gastrointestinal stromal tumor, renal cell carcinoma, gastrointestinal stromal tumor, neuroendocrine neoplasm

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

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

Translational evidence

Open Targets 26

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.

hypothyroidism0.93

Genetic · overall 0.57

acute myeloid leukemia0.55

Genetic · overall 0.84

neoplasm0.36

Genetic · overall 0.65

Highest-confidence therapeutic associations

Diseases where a drug acting on this target has already reached clinical development.

renal cell carcinoma0.98

Clinical · overall 0.64

hepatocellular carcinoma0.97

Clinical · overall 0.67

gastrointestinal stromal tumor0.95

Clinical · overall 0.65

primary myelofibrosis0.91

Clinical · overall 0.57

myelofibrosis0.90

Clinical · overall 0.62

Highest overall evidence

Remaining associations by Open Targets' aggregated evidence score.

cancer0.63

Pathway

acute lymphoblastic leukemia0.60

Literature

Show all associations
acute myeloid leukemia0.84
hepatocellular carcinoma0.67
gastrointestinal stromal tumor0.65
neoplasm0.65
renal cell carcinoma0.64
cancer0.63
myelofibrosis0.62
acute lymphoblastic leukemia0.60
primary myelofibrosis0.57
hypothyroidism0.57

Open Targets ranks 959 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 · 45 total

QUIZARTINIB DIHYDROCHLORIDEApproval

acute myeloid leukemia · myeloid leukemia · myelodysplastic syndrome

NINGETINIBPhase 2

non-small cell lung carcinoma · renal cell adenocarcinoma · acute myeloid leukemia

CEP-2563Phase 1
RUSERONTINIBPhase 3

acute myeloid leukemia · neoplasm

PACRITINIB CITRATEApproval

primary myelofibrosis · acquired polycythemia vera

FORETINIBPhase 2

breast cancer · gastric adenocarcinoma · renal cell carcinoma

CM-082Phase 2

mucosal melanoma · wet macular degeneration · non-small cell lung carcinoma

PACRITINIBApproval

myelofibrosis · neoplasm · myelofibrosis

AT-9283Phase 3

plasma cell myeloma · acute lymphoblastic leukemia · myelofibrosis with myeloid metaplasia

SUNITINIBApproval

gastrointestinal stromal tumor · renal cell carcinoma · gastrointestinal stromal tumor

Tractability

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 Binder

Safety liabilities

myelosuppression

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.

Show remaining trials (24)

COMPLETED · via sunitinib · NCT00357318

ClinicalTrials.gov via the drug-target graph.

Related literature

2

Papers indexed under “fms-Like Tyrosine Kinase 3” — a subject heading that covers this protein without being specific to it. Shown as context; not counted as this protein's own research activity.

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 literature, reached through a MeSH descriptor linked to this protein.

Forefront confidence

Synthesis

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.

acute myeloid leukemiaWell 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

neoplasmWell supported
0.83
agreement 0.720.94
Clinical59%Genetic30%Literature10%

Open Targets aggregate 0.65 · 3 independent evidence families

hepatocellular carcinomaWell 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 underlying per-type scores are shown above so the calculation can be checked.

What's happening now

29

Recent activity around this target, drawn from one canonical event stream. Every item is reached through 3 drugs that target this protein, so each event is news about that drug rather than about the protein directly.

  1. New publication2025-04-30
    Brain-wide microglia replacement using a nonconditioning strategy ameliorates pathology in mouse models of neurological disorders.

    Science translational medicine · 2025 · 11 citations · Europe PMC · via pexidartinib

  2. 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

  3. 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

  4. New publication2023-10-21
    Distinguishing the effects of systemic CSF1R inhibition by PLX3397 on microglia and peripheral immune cells.

    Journal of neuroinflammation · 2023 · 34 citations · Europe PMC · via pexidartinib

  5. 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

  6. Regulatory approval2021-02-11

    Approval: Sunitinib Accord (EMA)

    ema · regulatory · ema · via sunitinib

  7. New publication2021-01-05
    Microglial activation contributes to cognitive impairments in rotenone-induced mouse Parkinson's disease model.

    Journal of neuroinflammation · 2021 · 130 citations · Europe PMC · via pexidartinib

  8. New publication2020-06-21
    Liver transarterial chemoembolization and sunitinib for unresectable hepatocellular carcinoma: Results of the PRODIGE 16 study.

    Clinics and research in hepatology and gastroenterology · 2021 · 15 citations · Europe PMC · via sunitinib

  9. New publication2020-04-25
    Updated efficacy results from the JAVELIN Renal 101 trial: first-line avelumab plus axitinib versus sunitinib in patients with advanced renal cell carcinoma.

    Annals of oncology : official journal of the European Society for Medical Oncology · 2020 · 319 citations · Europe PMC · via sunitinib

  10. Regulatory approval2019-10-24

    Approval: Xospata (EMA)

    ema · regulatory · ema · via gilteritinib

  11. New publication2019-10-10
    Microglia drive APOE-dependent neurodegeneration in a tauopathy mouse model.

    The Journal of experimental medicine · 2019 · 350 citations · Europe PMC · via pexidartinib

  12. 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

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.