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kinase insert domain receptor

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Target not currently curated in GtoImmuPdb

Target id: 1813

Nomenclature: kinase insert domain receptor

Abbreviated Name: VEGFR-2

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

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1356 4q12 KDR kinase insert domain receptor
Mouse 1 1367 5 40.23 cM Kdr kinase insert domain protein receptor
Rat 1 1343 14p11 Kdr kinase insert domain receptor
Previous and Unofficial Names Click here for help
CD309 | fetal liver kinase 1 | FLK1 | FLK4 | kinase insert domain receptor (a type III receptor tyrosine kinase) | vascular endothelial growth factor receptor 2
Database Links Click here for help
Alphafold
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the kinase domain of human vascular endothelial growth factor receptor 2.
PDB Id:  1VR2
Resolution:  2.4Å
Species:  Human
References:  47
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of VEGFR2 (juxtamembrane and kinase domains) in complex with axitinib.
PDB Id:  4AG8
Ligand:  axitinib
Resolution:  2.0Å
Species:  Human
References:  46
Enzyme Reaction Click here for help
EC Number: 2.7.10.1
Natural/Endogenous Ligands Click here for help
VEGFA {Sp: Human}
VEGFC {Sp: Human}
VEGFE {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
pegdinetanib Peptide Hs Inhibition ~9.0 pKd 27
pKd ~9.0 (Kd ~1x10-9 M) [27]
cediranib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.0 pKd 15
pKd 9.0 (Kd 1.1x10-9 M) [15]
SU-14813 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.6 pKd 15
pKd 8.6 (Kd 2.3x10-9 M) [15]
motesanib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.6 pKd 15
pKd 8.6 (Kd 2.6x10-9 M) [15]
BIBF-1202 Small molecule or natural product Hs Inhibition 8.5 pKd 15
pKd 8.5 (Kd 2.9x10-9 M) [15]
axitinib 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 8.2 pKd 15
pKd 8.2 (Kd 5.9x10-9 M) [15]
pazopanib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.8 pKd 15
pKd 7.8 (Kd 1.4x10-8 M) [15]
RG-1530 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pKd 70
pKd 7.8 (Kd 1.5x10-8 M) [70]
sorafenib 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 7.2 pKd 15
pKd 7.2 (Kd 5.9x10-8 M) [15]
vatalanib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.2 pKd 15
pKd 7.2 (Kd 6.2x10-8 M) [15]
toceranib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 pKi 42
pKi 8.2 (Ki 6x10-9 M) [42]
PLX-4720 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 pKi 48
pKi 8.1 (Ki 9x10-9 M) [48]
pamufetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.9 pKi 23
pKi 7.9 (Ki 1.2x10-8 M) [23]
VEGF receptor tyrosine kinase inhibitor II Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.8 pKi 16
pKi 7.8 (Ki 1.5x10-8 M) [16]
cabozantinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 10.5 pIC50 81
pIC50 10.5 (IC50 3.5x10-11 M) [81]
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 9.8 pIC50 49
pIC50 9.8 (IC50 1.6x10-10 M) [49]
axitinib 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 9.6 pIC50 41
pIC50 9.6 (IC50 2.5x10-10 M) [41]
cediranib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition >9.0 pIC50 75
pIC50 >9.0 (IC50 <1x10-9 M) [75]
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 19
pIC50 9.0 (IC50 1x10-9 M) [19]
rivoceranib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 9.0 pIC50 69
pIC50 9.0 (IC50 1x10-9 M) [69]
Description: Assay used apatinib mesylate (YN968D1)
tesevatinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.8 pIC50 26
pIC50 8.8 (IC50 1.5x10-9 M) [26]
compound 13a [PMID: 23639540] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.8 pIC50 18
pIC50 8.8 (IC50 1.68x10-9 M) [18]
MLKL compound 1 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pIC50 58
pIC50 8.7 (IC50 2x10-9 M) [58]
ilorasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.7 pIC50 28
pIC50 8.7 (IC50 2x10-9 M) [28]
Description: Measuring inhibition of kinase activity in a biochemical assay.
foretinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 – 9.1 pIC50 49
pIC50 8.2 – 9.1 (IC50 6.8x10-9 – 8x10-10 M) [49]
tinengotinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.6 pIC50 79
pIC50 8.6 (IC50 2.5x10-9 M) [79]
motesanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.5 pIC50 49
pIC50 8.5 (IC50 3x10-9 M) [49]
compound 8i [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 – 8.6 pIC50 37,82
pIC50 8.6 (IC50 2.6x10-9 M) [82]
pIC50 8.4 (IC50 4x10-9 M) [37]
dorsomorphin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.4 pIC50 44
pIC50 8.4 (IC50 4x10-9 M) [44]
Description: Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits
linifanib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 2
pIC50 8.4 (IC50 4x10-9 M) [2]
lenvatinib 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 8.4 pIC50 49
pIC50 8.4 (IC50 4x10-9 M) [49]
lucitanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.4 pIC50 84
pIC50 8.4 (IC50 4x10-9 M) [84]
CEP-11981 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 34
pIC50 8.4 (IC50 4x10-9 M) [34]
compound 8h [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 37
pIC50 8.4 (IC50 4.2x10-9 M) [37]
famitinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.3 pIC50 11
pIC50 8.3 (IC50 5x10-9 M) [11]
sitravatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.3 pIC50 53
pIC50 8.3 (IC50 5x10-9 M) [53]
Description: In a biochemical enzyme activity assay.
tafetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.3 pIC50 74
pIC50 8.3 (IC50 5x10-9 M) [74]
Description: In a radiometric biochemical protein kinase assay.
LY2874455 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pIC50 83
pIC50 8.1 (IC50 7x10-9 M) [83]
Description: In vitro biochemical assay result
ibcasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 85
pIC50 8.1 (IC50 7x10-9 M) [85]
Description: Inhibition in a biochemical assay.
OSI-930 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 25
pIC50 8.1 (IC50 9x10-9 M) [25]
altiratinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Guide to Malaria Pharmacology Ligand Hs Inhibition 8.0 pIC50 21
pIC50 8.0 (IC50 9.2x10-9 M) [21]
vandetanib 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 8.0 pIC50 31
pIC50 8.0 (IC50 9x10-9 M) [31]
glesatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 pIC50 12
pIC50 8.0 (IC50 1x10-8 M) [12]
CP-547632 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.0 pIC50 7
pIC50 8.0 (IC50 1.1x10-8 M) [7]
Ki-20227 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.9 pIC50 51
pIC50 7.9 (IC50 1.2x10-8 M) [51]
PP121 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.9 pIC50 4
pIC50 7.9 (IC50 1.2x10-8 M) [4]
regorafenib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.9 pIC50 77
pIC50 7.9 (IC50 1.3x10-8 M) [77]
golvatinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 50
pIC50 7.8 (IC50 1.6x10-8 M) [50]
Description: Measured as inhibition of VEGFR-2 autophosphorylation in HUVEC cells.
VEGF receptor 2 kinase inhibitor IV Small molecule or natural product Primary target of this compound Hs Inhibition 7.7 pIC50 22
pIC50 7.7 (IC50 1.9x10-8 M) [22]
SU5402 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.7 pIC50 65
pIC50 7.7 (IC50 2x10-8 M) [65]
vatalanib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.7 pIC50 39
pIC50 7.7 (IC50 2.1x10-8 M) [39]
nintedanib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.7 pIC50 33
pIC50 7.7 (IC50 2.1x10-8 M) [33]
surufatinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.7 pIC50 60
pIC50 7.7 (IC50 2.1x10-8 M) [60]
Description: In a biochemical assay using recombinant KDR kinase catalytic domain.
sunitinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.7 pIC50 36
pIC50 7.7 (IC50 2.26x10-8 M) [36]
AZD4547 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.6 pIC50 5
pIC50 7.6 (IC50 2.4x10-8 M) [5]
brivanib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.6 pIC50 8
pIC50 7.6 (IC50 2.5x10-8 M) [8]
SU11652 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.6 pIC50 63
pIC50 7.6 (IC50 2.7x10-8 M) [63]
henatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 11
pIC50 7.6 (IC50 2.7x10-8 M) [11]
fruquintinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.5 – 7.6 pIC50 67
pIC50 7.6 (IC50 2.5x10-8 M) [67]
Description: Evaluated in a Z-lyte assay.
pIC50 7.5 (IC50 3.5x10-8 M) [67]
Description: Evaluated in a [32]p-ATP incorporation assay
pazopanib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.5 pIC50 30
pIC50 7.5 (IC50 3x10-8 M) [30]
pralsetinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.5 pIC50 61
pIC50 7.5 (IC50 3.5x10-8 M) [61]
Description: In a biochemical assay.
ENMD-2076 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.4 pIC50 55
pIC50 7.4 (IC50 3.6x10-8 M) [55]
erdafitinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.4 pIC50 59
pIC50 7.4 (IC50 3.63x10-8 M) [59]
ningetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pIC50 80
pIC50 7.4 (IC50 3.7x10-8 M) [80]
MK-2461 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pIC50 52
pIC50 7.4 (IC50 4.4x10-8 M) [52]
catequentinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.3 pIC50 10
pIC50 7.3 (IC50 4.5x10-8 M) [10]
Description: In vitro activity
SU-14813 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.3 pIC50 54
pIC50 7.3 (IC50 5x10-8 M) [54]
BMS-690514 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.3 pIC50 45
pIC50 7.3 (IC50 5x10-8 M) [45]
VEGF receptor 2 kinase inhibitor I Small molecule or natural product Primary target of this compound Mm Inhibition 7.2 pIC50 66
pIC50 7.2 (IC50 7x10-8 M) [66]
VEGF receptor 2 kinase inhibitor II Small molecule or natural product Primary target of this compound Hs Inhibition 7.2 pIC50 64
pIC50 7.2 (IC50 7x10-8 M) [64]
AEE788 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 pIC50 71
pIC50 7.1 (IC50 7.7x10-8 M) [71]
sorafenib 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 7.1 pIC50 76,82
pIC50 7.1 (IC50 9x10-8 M) [82]
pIC50 7.1 (IC50 9x10-8 M) [76]
cenisertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 14
pIC50 7.0 (IC50 9.5x10-8 M) [14]
Description: In a biochemical homogeneous time-resolved fluorescence (HTRF) kinase assay with an ATP concentration of 1 mM.
ZM-306416 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 32
pIC50 7.0 (IC50 1x10-7 M) [32]
telatinib Small molecule or natural product Hs Inhibition >7.0 pIC50 17
pIC50 >7.0 (IC50 <1x10-7 M) [17]
mivavotinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.9 pIC50 40
pIC50 6.9 (IC50 1.35x10-7 M) [40]
Description: Measured in a caliper-based electrophoretic mobility shift assay.
AST-487 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 1
pIC50 6.8 (IC50 1.7x10-7 M) [1]
Description: In vitro inhibition of KDR.
infigratinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.7 pIC50 29
pIC50 6.7 (IC50 1.8x10-7 M) [29]
semaxanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.7 pIC50 9
pIC50 6.7 (IC50 2x10-7 M) [9]
BX-912 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pIC50 20
pIC50 6.4 (IC50 4.1x10-7 M) [20]
pexidartinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.4 pIC50 68
pIC50 6.4 (IC50 4.4x10-7 M) [68]
orantinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.2 pIC50 35
pIC50 6.2 (IC50 6.8x10-7 M) [35]
DMBI Small molecule or natural product Primary target of this compound Mm Inhibition 6.1 pIC50 73
pIC50 6.1 (IC50 7.94x10-7 M) [73]
compound 19a [PMID: 30503936] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.1 pIC50 56
pIC50 6.1 (IC50 8.5x10-7 M) [56]
lazertinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition <6.0 pIC50 62
pIC50 <6.0 (IC50 >1x10-6 M) [62]
Description: In a biochemical enzyme activity assay.
BX-795 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.0 pIC50 20
pIC50 6.0 (IC50 1.1x10-6 M) [20]
GSK2646264 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 4.5 pIC50 6
pIC50 4.5 (IC50 3.162x10-5 M) [6]
dovitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition - pIC50 57,72
pIC50 (IC50 6.5x10-8 – 1.3x10-8 M) [57,72]
compound T.14 Small molecule or natural product Immunopharmacology Ligand Hs Inhibition - - 13
[13]
View species-specific inhibitor tables
Inhibitor Comments
Note that pazopanib is a multi-target kinase inhibitor. See [30] for additional data.
Vandetanib also inhibits EGFR and RET tyrosine kinases, as well as VEGFR2.
Although LY2874455 has equipotent IC50s for FGFRs and VEGFR2 in biochemical assays, in vivo efficacy appears to be 6-9-fold less for VEGFR2 phosphorylation in mouse heart muscle compared to inhibition of FGFR phosphorylation [83].
Agonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
VEGFA {Sp: Human} Peptide Click here for species-specific activity table Hs Agonist 8.0 – 9.6 pKd 38
pKd 9.6 (Kd 2.3x10-10 M) [38]
Description: Dissociation constant for scVEGF-binding to dimeric VEGFR2.
pKd 8.0 (Kd 1x10-8 M) [38]
Description: Dissociation constant for scVEGF-binding to monomeric VEGFR2.
Agonist Comments
Note that a VEGFA mimetic probe peptide (scVEGF) was used to determine the dissociation constants in the table above.
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
ramucirumab Peptide Approved drug Primary target of this compound Hs Antagonist 10.3 pKd 43
pKd 10.3 (Kd 5x10-11 M) [43]
ramucirumab Peptide Approved drug Primary target of this compound Hs Antagonist 9.0 pIC50 43
pIC50 9.0 (IC50 1x10-9 M) [43]
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: 15,78

Key to terms and symbols Click column headers to sort
Target used in screen: VEGFR2
Ligand Sp. Type Action Value Parameter
cediranib Small molecule or natural product Hs Inhibitor Inhibition 9.0 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.8 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 8.6 pKd
brivanib 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
foretinib 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
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 7.7 pKd
motesanib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 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: 3,24

Key to terms and symbols Click column headers to sort
Target used in screen: KDR/KDR(VEGFR2)
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 1.9 109.0 104.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 4.5 38.0 18.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 4.5 1.5 0.5
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 0.0 0.0
TWS119 Small molecule or natural product Hs Inhibitor Inhibition 6.7 5.0 2.0
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 12.6
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 13.8 2.0 1.0
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 16.9
VEGF receptor tyrosine kinase inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 19.7
K-252a Small molecule or natural product Hs Inhibitor Inhibition 20.0 3.0 0.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Immune system development
Immuno Process:  Immune regulation
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Hemangioma, capillary infantile
Synonyms: Familial capillary hemangioma [Orphanet: ORPHA91415]
OMIM: 602089
Orphanet: ORPHA91415
General Comments
This protein contains an immunoglobulin (Ig)-like domain that resembles the antibody variable domain, that has been coined the 'V-set domain'. The genes for all human V-set domain containing proteins are listed in HGNC gene group 590.

References

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1. Akeno-Stuart N, Croyle M, Knauf JA, Malaguarnera R, Vitagliano D, Santoro M, Stephan C, Grosios K, Wartmann M, Cozens R et al.. (2007) The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells. Cancer Res, 67 (14): 6956-64. [PMID:17638907]

2. Albert DH, Tapang P, Magoc TJ, Pease LJ, Reuter DR, Wei RQ, Li J, Guo J, Bousquet PF, Ghoreishi-Haack NS et al.. (2006) Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol Cancer Ther, 5 (4): 995-1006. [PMID:16648571]

3. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]

4. Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA. (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol, 4 (11): 691-9. [PMID:18849971]

5. AstraZeneca. AZD4547. Accessed on 11/09/2014. Modified on 11/09/2014. astrazeneca.com, http://openinnovation.astrazeneca.com/what-we-offer/compound/azd4547/

6. Barker MD, Liddle J, Atkinson FL, Wilson DM, Dickson MC, Ramirez-Molina C, Lewis H, Davis RP, Somers DO, Neu M et al.. (2018) Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease. Bioorg Med Chem Lett, 28 (21): 3458-3462. [PMID:30249354]

7. Beebe JS, Jani JP, Knauth E, Goodwin P, Higdon C, Rossi AM, Emerson E, Finkelstein M, Floyd E, Harriman S et al.. (2003) Pharmacological characterization of CP-547,632, a novel vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for cancer therapy. Cancer Res, 63 (21): 7301-9. [PMID:14612527]

8. Bhide RS, Cai ZW, Zhang YZ, Qian L, Wei D, Barbosa S, Lombardo LJ, Borzilleri RM, Zheng X, Wu LI et al.. (2006) Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor. J Med Chem, 49 (7): 2143-6. [PMID:16570908]

9. Bold G, Altmann KH, Frei J, Lang M, Manley PW, Traxler P, Wietfeld B, Brüggen J, Buchdunger E, Cozens R et al.. (2000) New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. J Med Chem, 43 (12): 2310-23. [PMID:10882357]

10. Chen GP. (2008) Spiro substituted compounds as angiogenesis inhibitors. Patent number: WO2008112407 A1. Assignee: Advenchen Laboratories, Llc. Priority date: 14/03/2007. Publication date: 18/09/2008.

11. Cho TP, Dong SY, Jun F, Hong FJ, Liang YJ, Lu X, Hua PJ, Li LY, Lei Z, Bing H et al.. (2010) Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives. J Med Chem, 53 (22): 8140-9. [PMID:21028894]

12. Claridge S, Raeppel F, Granger MC, Bernstein N, Saavedra O, Zhan L, Llewellyn D, Wahhab A, Deziel R, Rahil J et al.. (2008) Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. Bioorg Med Chem Lett, 18 (9): 2793-8. [PMID:18434145]

13. Conesa-Milián L, Falomir E, Murga J, Carda M, Marco JA. (2019) Novel multitarget inhibitors with antiangiogenic and immunomodulator properties. Eur J Med Chem, 170: 87-98. [PMID:30878834]

14. Curtin ML, Heyman HR, Frey RR, Marcotte PA, Glaser KB, Jankowski JR, Magoc TJ, Albert DH, Olson AM, Reuter DR et al.. (2012) Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases. Bioorg Med Chem Lett, 22 (14): 4750-5. [PMID:22695126]

15. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

16. Dominguez C, Smith L, Huang Q, Yuan C, Ouyang X, Cai L, Chen P, Kim J, Harvey T, Syed R et al.. (2007) Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr. Bioorg Med Chem Lett, 17 (21): 6003-8. [PMID:17869515] <