Details of the Target

General Information of Target

Target ID LDTP03820
Target Name Receptor-type tyrosine-protein kinase FLT3 (FLT3)
Gene Name FLT3
Gene ID 2322
Synonyms
CD135; FLK2; STK1; Receptor-type tyrosine-protein kinase FLT3; EC 2.7.10.1; FL cytokine receptor; Fetal liver kinase-2; FLK-2; Fms-like tyrosine kinase 3; FLT-3; Stem cell tyrosine kinase 1; STK-1; CD antigen CD135
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESP
EDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDL
QNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQD
ALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRE
CTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEM
STYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYE
IDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHA
ENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITE
GVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQD
NISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYD
LKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMS
ELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKE
HNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDL
NVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARDIMSDS
NYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYK
LIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDG
RVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS
Target Type
Successful
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, CSF-1/PDGF receptor subfamily
Subcellular location
Membrane
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.
TTD ID
T74312
Uniprot ID
P36888
DrugMap ID
TTGJCWZ
Ensemble ID
ENST00000241453.12
HGNC ID
HGNC:3765
ChEMBL ID
CHEMBL1974

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A549 SNV: p.N323K DBIA    Probe Info 
ABC1 SNV: p.E661V DBIA    Probe Info 
HCT116 Deletion: p.P986AfsTer27
SNV: p.V197A		 .
HEC1 SNV: p.R311W .
HEC1B SNV: p.R311W .
HT115 SNV: p.P116S DBIA    Probe Info 
ICC8 SNV: p.V317L DBIA    Probe Info 
IGR1 SNV: p.S519F .
JHH7 SNV: p.A445T .
MCC13 SNV: p.E720K .
MOLM13 Insertion: p.E598_Y599insFDFREYE DBIA    Probe Info 
MONOMAC6 SNV: p.V592A .
MV411 Insertion: p.D600_L601insHVDFREYEYD DBIA    Probe Info 
NCIH2172 SNV: p.P937H .
NCIH23 SNV: p.P738H DBIA    Probe Info 
RL952 SNV: p.E716D DBIA    Probe Info 
SAOS2 SNV: p.T382S DBIA    Probe Info 
SKNAS SNV: p.G739R DBIA    Probe Info 
SKOV3 SNV: p.S59A DBIA    Probe Info 
SNGM SNV: p.H222R DBIA    Probe Info 
TF1 SNV: p.E964G DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IA-alkyne
 Probe Info  		C241(10.00)  LDD2157  [1]
DBIA
 Probe Info  		C843(1.62)  LDD3310  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 22RV1 C843(2.50)  LDD2243  [2]
 LDCM0023  KB03 22RV1 C843(2.53)  LDD2660  [2]
 LDCM0024  KB05 COLO792 C843(1.62)  LDD3310  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Tyrosine-protein kinase ABL1 (ABL1) Tyr protein kinase family P00519
Tyrosine-protein kinase ABL2 (ABL2) Tyr protein kinase family P42684
Tyrosine-protein kinase Fyn (FYN) Tyr protein kinase family P06241
Tyrosine-protein kinase Lck (LCK) Tyr protein kinase family P06239
Tyrosine-protein kinase SYK (SYK) Tyr protein kinase family P43405
Other
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Adapter molecule crk (CRK) CRK family P46108
Crk-like protein (CRKL) CRK family P46109
Growth factor receptor-bound protein 10 (GRB10) GRB7/10/14 family Q13322
Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) PI3K p85 subunit family P27986
NF-kappa-B essential modulator (IKBKG) . Q9Y6K9
Ras GTPase-activating protein 1 (RASA1) . P20936

The Drug(s) Related To This Target

Approved
Click To Hide/Show 15 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Brigatinib Small molecular drug DB12267
Fedratinib Small molecular drug DB12500
Fostamatinib Small molecular drug DB12010
Intedanib Small molecular drug D09HNV
Lestaurtinib Small molecular drug D0V9WF
Midostaurin Small molecular drug D07NVU
Nintedanib Small molecular drug DB09079
Ponatinib Small molecular drug D0H0EQ
Sorafenib Small molecular drug DB00398
Sunitinib Small molecular drug DB01268
Tivozanib Small molecular drug DB11800
Zidovudine Small molecular drug D01XYJ
Gilteritinib . D04KZY
Pexidartinib . D09TAB
Pralsetinib . DB15822
Phase 3
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ac220 Small molecular drug D07KYT
Pacritinib Small molecular drug D0PN8H
Phase 2
Click To Hide/Show 9 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bms-690514 Small molecular drug D0R6UV
Famitinib Small molecular drug D0Z6MT
Ff-10101 Small molecular drug D28HJI
Hm43239 Small molecular drug DI1VM3
Mk-2461 Small molecular drug D00DRL
Sel24 Small molecular drug D0V2ZC
Cdx-301 . D0Q8CV
Sel-24 . D0X8ID
Tak-659 . D06KTJ
Phase 1
Click To Hide/Show 9 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Amg 427 Antibody D91CMX
Imc-eb10 Antibody D07ZNF
Fn-1501 Small molecular drug DKCU40
Kw-2449 Small molecular drug D00ABO
Mrx-2843 Small molecular drug D10LNV
Ski-g-801 Small molecular drug DIA08F
4sc-203 . D07UUB
Ff-10101-01 . D0YQ9I
Ki23819 . D0D1HS
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Mc-2001 . D04GFO
Investigative
Click To Hide/Show 31 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(1h-indol-2-yl)(5-methoxy-1h-indol-2-yl)Methanone Small molecular drug D09OLH
(1h-indol-2-yl)(5-phenoxy-1h-indol-2-yl)Methanone Small molecular drug D0G0KQ
(1h-indol-2-yl)(6-methoxy-1h-indol-2-yl)Methanone Small molecular drug D0D7ZL
(5-fluoro-1h-indol-2-yl)-(1h-indol-2-yl)Methanone Small molecular drug D0H7MF
(5-hydroxy-1h-indol-2-yl)(1h-indol-2-yl)Methanone Small molecular drug D0XS9E
(Benzo[B]Furan-2-yl)-(1h-indol-2-yl)Methanone Small molecular drug D0I7QX
2-(3,4-dimethoxybenzamido)Thiophene-3-carboxamide Small molecular drug D0ZO8Z
4-(4-aminophenyl)-1h-indazol-3yl-amine Small molecular drug D0Y9GK
Akn-028 Small molecular drug D0D0TQ
Amuvatinib Small molecular drug DB12742
Ast-487 Small molecular drug D0N7AJ
Bis(5-acetoxybenzo[B]Furan-2-yl)Methanone Small molecular drug D0L0MZ
Bis(5-aminobenzo[B]Furan-2-yl)Methanone Small molecular drug D07AXL
Bis(5-hydroxybenzo[B]Furan-2-yl)Methanone Small molecular drug D02OBA
Bis(6-hydroxybenzo[B]Furan-2-yl)Methanone Small molecular drug D03VAA
Bis(Benzo[B]Furan-2-yl)Methanone Small molecular drug D0Z3DW
Bis-(5-hydroxy-1h-indol-2-yl)-methanone Small molecular drug D0I3XZ
Di(1h-indol-2-yl)Methanone Small molecular drug D0G5YI
G749 Small molecular drug D0N3XP
Gtp-14564 Small molecular drug D0UN9O
In1479 Small molecular drug D0X1JO
Jnj-28312141 Small molecular drug D0Y4BL
N-[4-(3-amino-1h-indazol-4-yl)Phenyl]Benzamide Small molecular drug D0X6KS
Pmid21982499c14k Small molecular drug D06UKS
Pmid22765894c8h Small molecular drug D0C2GE
Pmid24900538c2c Small molecular drug D0E7VO
Quizartinib Small molecular drug DB12874
Tcs-359 Small molecular drug D0X7JK
Urmc-099 Small molecular drug D07ADX
Linifanib . DB06080
Xl999 . DB05014
Patented
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Carboxamide Derivative 4 Small molecular drug D0MX7B
Pyridine Derivative 18 Small molecular drug D0AK1F
Discontinued
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ag1295 Small molecular drug D06GBK
Su5614 Small molecular drug D01MIP
Tandutinib Small molecular drug D0IT6Q

References

1 From chemoproteomic-detected amino acids to genomic coordinates: insights into precise multi-omic data integration. Mol Syst Biol. 2021 Feb;17(2):e9840. doi: 10.15252/msb.20209840.
Mass spectrometry data entry: PXD022151
2 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840