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Target id: 1807
Nomenclature: fms related receptor tyrosine kinase 3
Abbreviated Name: FLT3
Family: Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 1 | 993 | 13q12.2 | FLT3 | fms related receptor tyrosine kinase 3 | |
Mouse | 1 | 1000 | 5 G3 | Flt3 | FMS-like tyrosine kinase 3 | |
Rat | - | 1000 | 12p11 | Flt3 | Fms related receptor tyrosine kinase 3 |
Previous and Unofficial Names ![]() |
CD135 | Fetal liver kinase 2 | FL cytokine receptor | FLK2 | FMS-like tyrosine kinase 3 | fms-related tyrosine kinase 3 | fms related tyrosine kinase 3 | STK1 |
Database Links ![]() |
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Alphafold | P36888 (Hs), Q00342 (Mm) |
BRENDA | 2.7.10.1 |
CATH/Gene3D | 2.60.40.10 |
ChEMBL Target | CHEMBL1974 (Hs), CHEMBL2034796 (Mm) |
DrugBank Target | P36888 (Hs) |
Ensembl Gene | ENSG00000122025 (Hs), ENSMUSG00000042817 (Mm), ENSRNOG00000054764 (Rn) |
Entrez Gene | 2322 (Hs), 14255 (Mm), 140635 (Rn) |
Human Protein Atlas | ENSG00000122025 (Hs) |
KEGG Enzyme | 2.7.10.1 |
KEGG Gene | hsa:2322 (Hs), mmu:14255 (Mm), rno:140635 (Rn) |
OMIM | 136351 (Hs) |
Orphanet | ORPHA138366 (Hs) |
Pharos | P36888 (Hs) |
RefSeq Nucleotide | NM_004119 (Hs), NM_010229 (Mm), NM_001100822 (Rn) |
RefSeq Protein | NP_004110 (Hs), NP_034359 (Mm), NP_001094292 (Rn) |
UniProtKB | P36888 (Hs), Q00342 (Mm) |
Wikipedia | FLT3 (Hs) |
Selected 3D Structures ![]() |
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Enzyme Reaction ![]() |
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Natural/Endogenous Ligands ![]() |
Fms-related tyrosine kinase 3 ligand {Sp: Human} |
Download all structure-activity data for this target as a CSV file
Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Inhibitor Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Cyclin-dependent kinase 1 (CDK1) which shares a phenylalanine gate keeper residue in the analogous position to that in FLT3, is significantly inhibited by Flt-3 inhibitor III but with a much lower IC50 value of 2100μM [18]. c-Kit and KDR (VEGFR-2) which contain a cysteine residue at the position corresponding to Cys828 important in the binding pocket of FLT3, are also inhibited by this compound, with IC50 values of 260 and 910μM respectively [18]. G-749 inhibits FLT3 mutant D835Y with an IC50 value of 0.6nM [36]. |
Other Binding Ligands | |||||||||||||||||||||||||||||||||||||||||||||||||||
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DiscoveRx KINOMEscan® screen ![]() |
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A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform. http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan Reference: 13,73 |
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Target used in screen: FLT3 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Target used in screen: FLT3(D835H) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Target used in screen: FLT3(D835Y) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Target used in screen: FLT3(ITD) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Target used in screen: FLT3(K663Q) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Target used in screen: FLT3(N841I) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Target used in screen: FLT3(R834Q) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Target used in screen: FLT3-autoinhibited | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen ![]() |
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A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service. A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform. http://www.millipore.com/techpublications/tech1/pf3036 http://www.reactionbiology.com/webapps/main/pages/kinase.aspx Reference: 3,19 |
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Target used in screen: Flt3/FLT3 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immunopharmacology Comments |
FLT3 is the receptor for the cytokine Flt3 ligand (FLT3LG). Flt3 ligand is a growth factor akin to stem cell factor and colony stimulating factor 1, and is essential for hematopoietic progenitor cell development and expansion of both myeloid and lymphoid lineages. It is one of the growth factor receptors targeted by the chemotherapeutic tyrosine kinase inhibitor sorafenib. Results from mouse experiments suggest that Flt3 ligand is effective in treating sepsis, by potentiating innate immune functions of dendritic cells and neutrophils and improving T cell function [53]. |
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Tissue Distribution ![]() |
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Physiological Functions ![]() |
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Physiological Consequences of Altering Gene Expression ![]() |
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Clinically-Relevant Mutations and Pathophysiology ![]() |
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Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family: fms related receptor tyrosine kinase 3. Last modified on 14/08/2024. Accessed on 24/03/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1807.