fms related tyrosine kinase 3 | Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family | IUPHAR/BPS Guide to PHARMACOLOGY

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fms related tyrosine kinase 3

target has curated data in GtoImmuPdb

Target id: 1807

Nomenclature: fms related tyrosine kinase 3

Abbreviated Name: FLT3

Family: Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 993 13q12 FLT3 fms related tyrosine kinase 3
Mouse 1 1000 5 G3 Flt3 FMS-like tyrosine kinase 3
Rat - 1000 12p11 Flt3 fms-related tyrosine kinase 3
Previous and Unofficial Names
CD135 | FLK2 | STK1 | FL cytokine receptor | FMS-like tyrosine kinase 3 | Fetal liver kinase 2 | fms-related tyrosine kinase 3
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of a human Flt3 ligand-receptor ternary complex
PDB Id:  3QS7
Resolution:  4.3Å
Species:  Human
References:  54
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of FLT3
PDB Id:  1RJB
Resolution:  2.1Å
Species:  Human
References:  19
Enzyme Reaction
EC Number: 2.7.10.1
Natural/Endogenous Ligands
Fms-related tyrosine kinase 3 ligand {Sp: Human}

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
AC710 Hs Inhibition 9.3 pKd 32
pKd 9.3 (Kd 5x10-10 M) [32]
linifanib Hs Inhibition 9.2 pKd 8
pKd 9.2 (Kd 6.3x10-10 M) [8]
dovitinib Hs Inhibition 9.2 pKd 8
pKd 9.2 (Kd 6.4x10-10 M) [8]
crenolanib Hs Inhibition 9.1 pKd 21
pKd 9.1 (Kd 7.4x10-10 M) [21]
AST-487 Hs Inhibition 9.1 pKd 8
pKd 9.1 (Kd 7.9x10-10 M) [8]
quizartinib Hs Inhibition 8.8 – 8.9 pKd 6,8
pKd 8.8 – 8.9 (Kd 1.6x10-9 – 1.3x10-9 M) [6,8]
tandutinib Hs Inhibition 8.5 pKd 8
pKd 8.5 (Kd 3x10-9 M) [8]
compound 5e [PMID: 28580438] Hs Inhibition 8.4 pKd 22
pKd 8.4 (Kd 3.6x10-9 M) [22]
Description: Measured using the Z′-LYTE Kinase Assay Kit and wild type FLT3.
lestaurtinib Hs Inhibition 8.1 pKd 8
pKd 8.1 (Kd 8.5x10-9 M) [8]
midostaurin Hs Inhibition 8.0 pKd 8
pKd 8.0 (Kd 1.1x10-8 M) [8]
RG-1530 Hs Inhibition 8.0 pKd 52
pKd 8.0 (Kd 1.1x10-8 M) [52]
KW-2449 Hs Inhibition 7.8 pKd 8
pKd 7.8 (Kd 1.5x10-8 M) [8]
belizatinib Hs Inhibition 7.4 pKd 31
pKd 7.4 (Kd 4.2x10-8 M) [31]
Description: Binding affinity in vitro.
UNC4203 Hs Inhibition 7.8 pKi 67
pKi 7.8 (Ki 1.614x10-8 M) [67]
AST-487 Hs Inhibition 6.9 pKi 59
pKi 6.9 (Ki 1.2x10-7 M) [59]
Description: Inhibition of wild type FLT3
gilteritinib Hs Inhibition ~9.5 pIC50 30
pIC50 ~9.5 (IC50 ~3x10-10 M) [30]
G749 Hs Inhibition 9.4 pIC50 29
pIC50 9.4 (IC50 4x10-10 M) [29]
compound 8i [PMID: 22765894] Hs Inhibition 9.1 pIC50 65
pIC50 9.1 (IC50 8x10-10 M) [65]
compound 8h [PMID: 22765894] Hs Inhibition 9.1 pIC50 26
pIC50 9.1 (IC50 8.5x10-10 M) [26]
dorsomorphin Hs Inhibition >9.0 pIC50 33
pIC50 >9.0 (IC50 <1x10-9 M) [33]
Description: Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits
RGB-286638 Hs Inhibition 9.0 pIC50 7
pIC50 9.0 (IC50 1x10-9 M) [7]
ilorasertib Hs Inhibition 9.0 pIC50 15
pIC50 9.0 (IC50 1x10-9 M) [15]
Description: Measuring inhibition of kinase activity in a biochemical assay.
dovitinib Hs Inhibition 8.5 – 9.0 pIC50 47,53
pIC50 8.5 – 9.0 (IC50 3x10-9 – 1x10-9 M) [47,53]
compound 2c [PMID: 24900538] Hs Inhibition 8.7 pIC50 56
pIC50 8.7 (IC50 2.1x10-9 M) [56]
ENMD-2076 Hs Inhibition 8.5 pIC50 46
pIC50 8.5 (IC50 3x10-9 M) [46]
linifanib Hs Inhibition 8.4 pIC50 2
pIC50 8.4 (IC50 4x10-9 M) [2]
URMC-099 Hs Inhibition 8.4 pIC50 17
pIC50 8.4 (IC50 4x10-9 M) [17]
quizartinib Hs Inhibition 8.4 pIC50 66
pIC50 8.4 (IC50 4.2x10-9 M) [66]
mivavotinib Hs Inhibition 8.3 pIC50 28
pIC50 8.3 (IC50 4.6x10-9 M) [28]
Description: In vitro potency
AKN-028 Hs Inhibition 8.2 pIC50 11
pIC50 8.2 (IC50 6x10-9 M) [11]
sunitinib Hs Inhibition 8.2 pIC50 25
pIC50 8.2 (IC50 6.5x10-9 M) [25]
KW-2449 Hs Inhibition 8.2 pIC50 50
pIC50 8.2 (IC50 6.6x10-9 M) [50]
sitravatinib Hs Inhibition 8.1 pIC50 44
pIC50 8.1 (IC50 8x10-9 M) [44]
Description: In a biochemical enzyme activity assay.
compound 7d [PMID: 29672049] Hs Inhibition 7.9 pIC50 20
pIC50 7.9 (IC50 1.3x10-8 M) [20]
Description: In a biochemical assay.
MELK-TI Hs Inhibition 7.7 pIC50 23
pIC50 7.7 (IC50 1.8x10-8 M) [23]
Description: Measured in a MIllipore kinase screening panel assay
tafetinib Hs Inhibition 7.7 pIC50 55
pIC50 7.7 (IC50 2.08x10-8 M) [55]
Description: In a radiometric biochemical protein kinase assay.
pacritinib Hs Inhibition 7.7 pIC50 61
pIC50 7.7 (IC50 2.2x10-8 M) [61]
MK-2461 Hs Inhibition 7.7 pIC50 41
pIC50 7.7 (IC50 2.2x10-8 M) [41]
JNJ-28312141 Hs Inhibition 7.5 pIC50 36
pIC50 7.5 (IC50 3x10-8 M) [36]
merestinib Hs Inhibition 7.5 pIC50 64
pIC50 7.5 (IC50 3.1x10-8 M) [64]
Description: Inhibition of in vitro biochemical activity by EMD Millipore assay.
TG02 Hs Inhibition 7.3 – 7.7 pIC50 16,62
pIC50 7.3 – 7.7 (IC50 5.6x10-8 – 1.9x10-8 M) [16,62]
Flt-3 inhibitor II Hs Inhibition 7.5 pIC50 35
pIC50 7.5 (IC50 3.3x10-8 M) [35]
Flt-3 inhibitor Hs Inhibition 7.4 pIC50 42
pIC50 7.4 (IC50 4.2x10-8 M) [42]
SGI-1776 Hs Inhibition 7.4 pIC50 10
pIC50 7.4 (IC50 4.4x10-8 M) [10]
sorafenib Hs Inhibition 7.2 – 7.5 pIC50 60,65
pIC50 7.5 (IC50 3.3x10-8 M) [65]
pIC50 7.2 (IC50 5.8x10-8 M) [60]
Flt-3 inhibitor III Hs Inhibition 7.3 pIC50 12
pIC50 7.3 (IC50 5x10-8 M) [12]
ceritinib Hs Inhibition 7.2 pIC50 38
pIC50 7.2 (IC50 6x10-8 M) [38]
PF-562271 Hs Inhibition 7.0 pIC50 48
pIC50 7.0 (IC50 9.7x10-8 M) [48]
compound 14k [PMID: 21982499] Hs Inhibition 7.0 pIC50 45
pIC50 7.0 (IC50 1.04x10-7 M) [45]
BMS-690514 Hs Inhibition 7.0 pIC50 37
pIC50 7.0 (IC50 1.1x10-7 M) [37]
pexidartinib Hs Inhibition 6.8 pIC50 51
pIC50 6.8 (IC50 1.6x10-7 M) [51]
edicotinib Hs Inhibition 6.7 pIC50 14
pIC50 6.7 (IC50 1.9x10-7 M) [14]
tandutinib Hs Inhibition 6.7 pIC50 24
pIC50 6.7 (IC50 2.2x10-7 M) [24]
GTP-14564 Hs Inhibition 6.5 pIC50 40
pIC50 6.5 (IC50 3x10-7 M) [40]
NMS-P937 Hs Inhibition 6.3 pIC50 4
pIC50 6.3 (IC50 5.1x10-7 M) [4]
AST-487 Hs Inhibition 6.3 pIC50 1
pIC50 6.3 (IC50 5.2x10-7 M) [1]
midostaurin Hs Inhibition 6.3 pIC50 58
pIC50 6.3 (IC50 5.28x10-7 M) [58]
cediranib Hs Inhibition <6.0 pIC50 57
pIC50 <6.0 (IC50 >1x10-6 M) [57]
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 [12]. 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 [12].
G-749 inhibits FLT3 mutant D835Y with an IC50 value of 0.6nM [29].
DiscoveRx KINOMEscan® screen
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: 8,63

Key to terms and symbols Click column headers to sort
Target used in screen: FLT3
Ligand Sp. Type Action Value Parameter
sunitinib Hs Inhibitor Inhibition 9.4 pKd
SU-14813 Hs Inhibitor Inhibition 9.3 pKd
linifanib Hs Inhibitor Inhibition 9.2 pKd
dovitinib Hs Inhibitor Inhibition 9.2 pKd
tamatinib Hs Inhibitor Inhibition 9.1 pKd
AST-487 Hs Inhibitor Inhibition 9.1 pKd
foretinib Hs Inhibitor Inhibition 9.1 pKd
quizartinib Hs Inhibitor Inhibition 8.9 pKd
staurosporine Hs Inhibitor Inhibition 8.5 pKd
tandutinib Hs Inhibitor Inhibition 8.5 pKd
Target used in screen: FLT3(D835H)
Ligand Sp. Type Action Value Parameter
tamatinib Hs Inhibitor Inhibition 9.2 pKd
lestaurtinib Hs Inhibitor Inhibition 9.2 pKd
foretinib Hs Inhibitor Inhibition 8.9 pKd
staurosporine Hs Inhibitor Inhibition 8.7 pKd
JNJ-28312141 Hs Inhibitor Inhibition 8.6 pKd
linifanib Hs Inhibitor Inhibition 8.6 pKd
quizartinib Hs Inhibitor Inhibition 8.4 pKd
sunitinib Hs Inhibitor Inhibition 8.4 pKd
NVP-TAE684 Hs Inhibitor Inhibition 8.3 pKd
AST-487 Hs Inhibitor Inhibition 8.3 pKd
Target used in screen: FLT3(D835Y)
Ligand Sp. Type Action Value Parameter
tamatinib Hs Inhibitor Inhibition 9.4 pKd
lestaurtinib Hs Inhibitor Inhibition 9.2 pKd
JNJ-28312141 Hs Inhibitor Inhibition 8.8 pKd
foretinib Hs Inhibitor Inhibition 8.7 pKd
NVP-TAE684 Hs Inhibitor Inhibition 8.7 pKd
sunitinib Hs Inhibitor Inhibition 8.6 pKd
staurosporine Hs Inhibitor Inhibition 8.6 pKd
dovitinib Hs Inhibitor Inhibition 8.3 pKd
SU-14813 Hs Inhibitor Inhibition 8.2 pKd
fedratinib Hs Inhibitor Inhibition 8.2 pKd
Target used in screen: FLT3(ITD)
Ligand Sp. Type Action Value Parameter
tamatinib Hs Inhibitor Inhibition 9.3 pKd
sunitinib Hs Inhibitor Inhibition 9.0 pKd
lestaurtinib Hs Inhibitor Inhibition 8.8 pKd
SU-14813 Hs Inhibitor Inhibition 8.7 pKd
staurosporine Hs Inhibitor Inhibition 8.6 pKd
foretinib Hs Inhibitor Inhibition 8.6 pKd
dovitinib Hs Inhibitor Inhibition 8.4 pKd
JNJ-28312141 Hs Inhibitor Inhibition 8.4 pKd
NVP-TAE684 Hs Inhibitor Inhibition 8.1 pKd
linifanib Hs Inhibitor Inhibition 8.1 pKd
Target used in screen: FLT3(K663Q)
Ligand Sp. Type Action Value Parameter
sunitinib Hs Inhibitor Inhibition 9.7 pKd
AST-487 Hs Inhibitor Inhibition 9.3 pKd
tamatinib Hs Inhibitor Inhibition 9.2 pKd
SU-14813 Hs Inhibitor Inhibition 9.1 pKd
foretinib Hs Inhibitor Inhibition 9.1 pKd
dovitinib Hs Inhibitor Inhibition 9.0 pKd
linifanib Hs Inhibitor Inhibition 8.9 pKd
tandutinib Hs Inhibitor Inhibition 8.8 pKd
midostaurin Hs Inhibitor Inhibition 8.7 pKd
quizartinib Hs Inhibitor Inhibition 8.7 pKd
Target used in screen: FLT3(N841I)
Ligand Sp. Type Action Value Parameter
lestaurtinib Hs Inhibitor Inhibition 8.9 pKd
tamatinib Hs Inhibitor Inhibition 8.8 pKd
foretinib Hs Inhibitor Inhibition 8.8 pKd
staurosporine Hs Inhibitor Inhibition 8.7 pKd
AST-487 Hs Inhibitor Inhibition 8.6 pKd
sunitinib Hs Inhibitor Inhibition 8.6 pKd
linifanib Hs Inhibitor Inhibition 8.6 pKd
quizartinib Hs Inhibitor Inhibition 8.4 pKd
tozasertib Hs Inhibitor Inhibition 8.4 pKd
dovitinib Hs Inhibitor Inhibition 8.3 pKd
Target used in screen: FLT3(R834Q)
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 9.7 pKd
AST-487 Hs Inhibitor Inhibition 9.1 pKd
tamatinib Hs Inhibitor Inhibition 8.4 pKd
quizartinib Hs Inhibitor Inhibition 8.3 pKd
lestaurtinib Hs Inhibitor Inhibition 8.1 pKd
dovitinib Hs Inhibitor Inhibition 8.1 pKd
foretinib Hs Inhibitor Inhibition 8.0 pKd
sunitinib Hs Inhibitor Inhibition 8.0 pKd
midostaurin Hs Inhibitor Inhibition 7.9 pKd
linifanib Hs Inhibitor Inhibition 7.8 pKd
Target used in screen: FLT3-autoinhibited
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 9.0 pKd
sunitinib Hs Inhibitor Inhibition 8.8 pKd
AST-487 Hs Inhibitor Inhibition 6.9 pKd
lestaurtinib Hs Inhibitor Inhibition 6.7 pKd
quizartinib Hs Inhibitor Inhibition 6.4 pKd
midostaurin Hs Inhibitor Inhibition 6.2 pKd
tandutinib Hs Inhibitor Inhibition 6.1 pKd
tozasertib Hs Inhibitor Inhibition 6.1 pKd
sorafenib Hs Inhibitor Inhibition 6.0 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
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: 3,13

Key to terms and symbols Click column headers to sort
Target used in screen: Flt3/FLT3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
SB 218078 Hs Inhibitor Inhibition 0.2 24.0 3.0
dorsomorphin