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fms related receptor tyrosine kinase 1

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Target id: 1812

Nomenclature: fms related receptor tyrosine kinase 1

Abbreviated Name: VEGFR-1

Family: Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1338 13q12.3 FLT1 fms related receptor tyrosine kinase 1
Mouse 1 1333 5 87.01 cM Flt1 FMS-like tyrosine kinase 1
Rat 1 1336 12p11 Flt1 Fms related receptor tyrosine kinase 1
Previous and Unofficial Names Click here for help
fms related tyrosine kinase 1 | FMS-related tyrosine kinase 1 | fms-related tyrosine kinase 1 | vascular endothelial growth factor receptor 1
Database Links Click here for help
Alphafold P17948 (Hs), P35969 (Mm), P53767 (Rn)
BRENDA 2.7.10.1
CATH/Gene3D 2.60.40.10
ChEMBL Target CHEMBL1868 (Hs), CHEMBL3516 (Mm)
DrugBank Target P17948 (Hs)
Ensembl Gene ENSG00000102755 (Hs), ENSMUSG00000029648 (Mm), ENSRNOG00000000940 (Rn)
Entrez Gene 2321 (Hs), 14254 (Mm), 54251 (Rn)
Human Protein Atlas ENSG00000102755 (Hs)
KEGG Enzyme 2.7.10.1
KEGG Gene hsa:2321 (Hs), mmu:14254 (Mm), rno:54251 (Rn)
OMIM 165070 (Hs)
Pharos P17948 (Hs)
RefSeq Nucleotide NM_001159920 (Hs), NM_010228 (Mm), NM_019306 (Rn)
RefSeq Protein NP_001153392 (Hs), NP_034358 (Mm), NP_062179 (Rn)
UniProtKB P17948 (Hs), P35969 (Mm), P53767 (Rn)
Wikipedia FLT1 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of VEGFR1 (FLT1) in complex with N-(4-Chlorophenyl)-2-((pyridin-4-ylmethyl)amino)benzamide.
PDB Id:  3HNG
Resolution:  2.7Å
Species:  Human
References: 
Enzyme Reaction Click here for help
EC Number: 2.7.10.1
Natural/Endogenous Ligands Click here for help
VEGFA {Sp: Human}
VEGFB {Sp: Human}

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
RG-1530 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pKd 29
⤷ pKd 8.1 (Kd 9x10-9 M) [29]
compound 25 [PMID: 17935989] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pKi 27
⤷ pKi 6.4 (Ki 4.4x10-7 M) [27]
tivozanib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.7 pIC50 21
⤷ pIC50 9.7 (IC50 2.1x10-10 M) [21]
foretinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.1 pIC50 21
⤷ pIC50 9.1 (IC50 8x10-10 M) [21]
VEGF receptor tyrosine kinase inhibitor III Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.0 pIC50 9
⤷ pIC50 9.0 (IC50 1x10-9 M) [9]
ilorasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.0 pIC50 12
⤷ pIC50 9.0 (IC50 1x10-9 M) [12]
Description: Measuring inhibition of kinase activity in a biochemical assay.
motesanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pIC50 21
⤷ pIC50 8.7 (IC50 2x10-9 M) [21]
SU-14813 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.7 pIC50 24
⤷ pIC50 8.7 (IC50 2x10-9 M) [24]
tinengotinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.6 pIC50 33
⤷ pIC50 8.6 (IC50 2.4x10-9 M) [33]
linifanib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.5 pIC50 1
⤷ pIC50 8.5 (IC50 3x10-9 M) [1]
CEP-11981 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.5 pIC50 16
⤷ pIC50 8.5 (IC50 3x10-9 M) [16]
catequentinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 8.4 pIC50 7
⤷ pIC50 8.4 (IC50 4x10-9 M) [7]
Description: In vitro activity
cediranib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.3 pIC50 31
⤷ pIC50 8.3 (IC50 5x10-9 M) [31]
dovitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 – 8.5 pIC50 25,30
⤷ pIC50 8.0 – 8.5 (IC50 1x10-8 – 3x10-9 M) [25,30]
sitravatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.2 pIC50 23
⤷ pIC50 8.2 (IC50 6x10-9 M) [23]
Description: In a biochemical enzyme activity assay.
compound 8h [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 17
⤷ pIC50 8.1 (IC50 7.2x10-9 M) [17]
semaxanib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pIC50 6
⤷ pIC50 8.1 (IC50 8x10-9 M) [6]
OSI-930 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 11
⤷ pIC50 8.1 (IC50 8x10-9 M) [11]
ibcasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 36
⤷ pIC50 8.1 (IC50 8x10-9 M) [36]
Description: Inhibition in a biochemical assay.
pazopanib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.0 pIC50 13
⤷ pIC50 8.0 (IC50 1x10-8 M) [13]
MK-2461 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 pIC50 22
⤷ pIC50 8.0 (IC50 1x10-8 M) [22]
dorsomorphin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.0 pIC50 20
⤷ pIC50 8.0 (IC50 1.1x10-8 M) [20]
Description: Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits
lucitanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.9 pIC50 35
⤷ pIC50 7.9 (IC50 1.2x10-8 M) [35]
compound 8i [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.5 – 7.7 pIC50 17,34
⤷ pIC50 7.7 (IC50 2x10-8 M) [17]
pIC50 7.5 (IC50 2.9x10-8 M) [34]
nintedanib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 15
⤷ pIC50 7.5 (IC50 3.1x10-8 M) [15]
Cdk1/2 inhibitor III Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 19
⤷ pIC50 7.5 (IC50 3.2x10-8 M) [19]
fruquintinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.5 pIC50 26
⤷ pIC50 7.5 (IC50 3.3x10-8 M) [26]
Description: Evaluated in a [32]p-ATP incorporation assay
pexmetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.3 pIC50 4
⤷ pIC50 7.3 (IC50 4.7x10-8 M) [4]
vatalanib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 18
⤷ pIC50 6.8 (IC50 1.4x10-7 M) [18]
brivanib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pIC50 5
⤷ pIC50 6.4 (IC50 3.8x10-7 M) [5]
ZM-306416 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.7 – 6.5 pIC50 3,14
⤷ pIC50 5.7 – 6.5 (IC50 2x10-6 – 3.3x10-7 M) [3,14]
pexidartinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.1 pIC50 28
⤷ pIC50 6.1 (IC50 8.8x10-7 M) [28]
Inhibitor Comments
Note that pazopanib is a multi-target kinase inhibitor. See for [13] futher affinity data.
Compound 25 [PMID 17935989] is a CHK1 inhibitor and interacts with VEGFR1 as an off-target. Inhibiton of CHK1 is >100 times more potent than inhibition of VEGFR1 [...].
DiscoveRx KINOMEscan® screen Click here for help
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: 8,32
Key to terms and symbols Click column headers to sort
Target used in screen: FLT1
Ligand Sp. Type Action Value Parameter
cediranib Small molecule or natural product Hs Inhibitor Inhibition 9.1 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 8.3 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.2 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition 8.1 pKd
vatalanib Small molecule or natural product Hs Inhibitor Inhibition 8.0 pKd
brivanib Small molecule or natural product Hs Inhibitor Inhibition 8.0 pKd
motesanib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 7.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
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: 2,10
Key to terms and symbols Click column headers to sort
Target used in screen: Flt1/FLT1(VEGFR1)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
PDK1/Akt/Flt dual pathway inhibitor Small molecule or natural product Hs Inhibitor Inhibition 3.1 115.0 89.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 0.0 -0.5
TWS119 Small molecule or natural product Hs Inhibitor Inhibition 8.6 0.0 0.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 11.4 0.0 -1.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 13.3 7.0 4.0
Gö 6983 Small molecule or natural product Hs Inhibitor Inhibition 22.0 2.0 0.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 23.2 0.0 0.0
VEGF receptor tyrosine kinase inhibitor II Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 24.8 0.0 2.0
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 26.2
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 27.2
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Chemotaxis & migration
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling
Immuno Process:  Immune system development

References

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How to cite this page

Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family: fms related receptor tyrosine kinase 1. Last modified on 04/02/2022. Accessed on 10/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1812.