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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

Contents:

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 P35968 (Hs), P35918 (Mm), O08775 (Rn)
BRENDA 2.7.10.1
CATH/Gene3D 2.60.40.10
ChEMBL Target CHEMBL279 (Hs), CHEMBL3337 (Mm)
DrugBank Target P35968 (Hs)
Ensembl Gene ENSG00000128052 (Hs), ENSMUSG00000062960 (Mm), ENSRNOG00000046829 (Rn)
Entrez Gene 3791 (Hs), 16542 (Mm), 25589 (Rn)
Human Protein Atlas ENSG00000128052 (Hs)
KEGG Enzyme 2.7.10.1
KEGG Gene hsa:3791 (Hs), mmu:16542 (Mm), rno:25589 (Rn)
OMIM 191306 (Hs)
Orphanet ORPHA229801 (Hs)
Pharos P35968 (Hs)
RefSeq Nucleotide NM_002253 (Hs), NM_010612 (Mm), NM_013062 (Rn)
RefSeq Protein NP_002244 (Hs), NP_034742 (Mm), NP_037194 (Rn)
SynPHARM 78759 (in complex with axitinib)
81169 (in complex with axitinib)
79689 (in complex with lenvatinib)
79677 (in complex with nintedanib)
81175 (in complex with sorafenib)
81305 (in complex with sorafenib)
81287 (in complex with sunitinib)
79680 (in complex with tivozanib)
UniProtKB P35968 (Hs), P35918 (Mm), O08775 (Rn)
Wikipedia KDR (Hs)
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:  49
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:  48
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 28
⤷ pKd ~9.0 (Kd ~1x10-9 M) [28]
cediranib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.0 pKd 16
⤷ pKd 9.0 (Kd 1.1x10-9 M) [16]
SU-14813 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.6 pKd 16
⤷ pKd 8.6 (Kd 2.3x10-9 M) [16]
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 16
⤷ pKd 8.6 (Kd 2.6x10-9 M) [16]
BIBF-1202 Small molecule or natural product Hs Inhibition 8.5 pKd 16
⤷ pKd 8.5 (Kd 2.9x10-9 M) [16]
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 16
⤷ pKd 8.2 (Kd 5.9x10-9 M) [16]
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 16
⤷ pKd 7.8 (Kd 1.4x10-8 M) [16]
RG-1530 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pKd 74
⤷ pKd 7.8 (Kd 1.5x10-8 M) [74]
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 16
⤷ pKd 7.2 (Kd 5.9x10-8 M) [16]
vatalanib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.2 pKd 16
⤷ pKd 7.2 (Kd 6.2x10-8 M) [16]
toceranib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 pKi 44
⤷ pKi 8.2 (Ki 6x10-9 M) [44]
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 50
⤷ pKi 8.1 (Ki 9x10-9 M) [50]
pamufetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.9 pKi 24
⤷ pKi 7.9 (Ki 1.2x10-8 M) [24]
VEGF receptor tyrosine kinase inhibitor II Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.8 pKi 17
⤷ pKi 7.8 (Ki 1.5x10-8 M) [17]
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 85
⤷ pIC50 10.5 (IC50 3.5x10-11 M) [85]
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 51
⤷ pIC50 9.8 (IC50 1.6x10-10 M) [51]
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 42
⤷ pIC50 9.6 (IC50 2.5x10-10 M) [42]
canlitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.4 pIC50 71
⤷ pIC50 9.4 (IC50 3.8x10-10 M) [71]
cediranib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition >9.0 pIC50 79
⤷ pIC50 >9.0 (IC50 <1x10-9 M) [79]
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 20
⤷ pIC50 9.0 (IC50 1x10-9 M) [20]
rivoceranib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 9.0 pIC50 73
⤷ pIC50 9.0 (IC50 1x10-9 M) [73]
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 27
⤷ pIC50 8.8 (IC50 1.5x10-9 M) [27]
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 19
⤷ pIC50 8.8 (IC50 1.68x10-9 M) [19]
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 60
⤷ pIC50 8.7 (IC50 2x10-9 M) [60]
ilorasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.7 pIC50 29
⤷ pIC50 8.7 (IC50 2x10-9 M) [29]
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 51
⤷ pIC50 8.2 – 9.1 (IC50 6.8x10-9 – 8x10-10 M) [51]
tinengotinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.6 pIC50 83
⤷ pIC50 8.6 (IC50 2.5x10-9 M) [83]
motesanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.5 pIC50 51
⤷ pIC50 8.5 (IC50 3x10-9 M) [51]
compound 8i [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 – 8.6 pIC50 38,86
⤷ pIC50 8.6 (IC50 2.6x10-9 M) [86]
pIC50 8.4 (IC50 4x10-9 M) [38]
dorsomorphin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.4 pIC50 46
⤷ pIC50 8.4 (IC50 4x10-9 M) [46]
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 3
⤷ pIC50 8.4 (IC50 4x10-9 M) [3]
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 51
⤷ pIC50 8.4 (IC50 4x10-9 M) [51]
lucitanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.4 pIC50 88
⤷ pIC50 8.4 (IC50 4x10-9 M) [88]
CEP-11981 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 35
⤷ pIC50 8.4 (IC50 4x10-9 M) [35]
compound 8h [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 38
⤷ pIC50 8.4 (IC50 4.2x10-9 M) [38]
famitinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.3 pIC50 12
⤷ pIC50 8.3 (IC50 5x10-9 M) [12]
sitravatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.3 pIC50 55
⤷ pIC50 8.3 (IC50 5x10-9 M) [55]
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 78
⤷ pIC50 8.3 (IC50 5x10-9 M) [78]
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 87
⤷ pIC50 8.1 (IC50 7x10-9 M) [87]
Description: In vitro biochemical assay result
ibcasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 89
⤷ pIC50 8.1 (IC50 7x10-9 M) [89]
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 26
⤷ pIC50 8.1 (IC50 9x10-9 M) [26]
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 22
⤷ pIC50 8.0 (IC50 9.2x10-9 M) [22]
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 32
⤷ pIC50 8.0 (IC50 9x10-9 M) [32]
glesatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 pIC50 13
⤷ pIC50 8.0 (IC50 1x10-8 M) [13]
CP-547632 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.0 pIC50 8
⤷ pIC50 8.0 (IC50 1.1x10-8 M) [8]
Ki-20227 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.9 pIC50 53
⤷ pIC50 7.9 (IC50 1.2x10-8 M) [53]
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 5
⤷ pIC50 7.9 (IC50 1.2x10-8 M) [5]
regorafenib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.9 pIC50 81
⤷ pIC50 7.9 (IC50 1.3x10-8 M) [81]
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 52
⤷ pIC50 7.8 (IC50 1.6x10-8 M) [52]
Description: Measured as inhibition of VEGFR-2 autophosphorylation in HUVEC cells.
acrizanib Small molecule or natural product Hs Inhibition 7.8 pIC50 1
⤷ pIC50 7.8 (IC50 1.74x10-8 M) [1]
Description: Determined in a Ba/F3 VEGFR2 cellular proliferation assay
VEGF receptor 2 kinase inhibitor IV Small molecule or natural product Primary target of this compound Hs Inhibition 7.7 pIC50 23
⤷ pIC50 7.7 (IC50 1.9x10-8 M) [23]
SU5402 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.7 pIC50 68
⤷ pIC50 7.7 (IC50 2x10-8 M) [68]
vatalanib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.7 pIC50 40
⤷ pIC50 7.7 (IC50 2.1x10-8 M) [40]
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 34
⤷ pIC50 7.7 (IC50 2.1x10-8 M) [34]
surufatinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.7 pIC50 62
⤷ pIC50 7.7 (IC50 2.1x10-8 M) [62]
Description: In a biochemical assay using recombinant KDR kinase catalytic domain.
resencatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pIC50 63
⤷ pIC50 7.7 (IC50 2.17x10-8 M) [63]
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 37
⤷ pIC50 7.7 (IC50 2.26x10-8 M) [37]
fexagratinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.6 pIC50 6
⤷ pIC50 7.6 (IC50 2.4x10-8 M) [6]
brivanib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.6 pIC50 9
⤷ pIC50 7.6 (IC50 2.5x10-8 M) [9]
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 66
⤷ pIC50 7.6 (IC50 2.7x10-8 M) [66]
henatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 12
⤷ pIC50 7.6 (IC50 2.7x10-8 M) [12]
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 70
⤷ pIC50 7.6 (IC50 2.5x10-8 M) [70]
Description: Evaluated in a Z-lyte assay.
pIC50 7.5 (IC50 3.5x10-8 M) [70]
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 31
⤷ pIC50 7.5 (IC50 3x10-8 M) [31]
pralsetinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.5 pIC50 64
⤷ pIC50 7.5 (IC50 3.5x10-8 M) [64]
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 57
⤷ pIC50 7.4 (IC50 3.6x10-8 M) [57]
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 61
⤷ pIC50 7.4 (IC50 3.63x10-8 M) [61]
ningetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pIC50 84
⤷ pIC50 7.4 (IC50 3.7x10-8 M) [84]
MK-2461 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pIC50 54
⤷ pIC50 7.4 (IC50 4.4x10-8 M) [54]
catequentinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.3 pIC50 11
⤷ pIC50 7.3 (IC50 4.5x10-8 M) [11]
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 56
⤷ pIC50 7.3 (IC50 5x10-8 M) [56]
BMS-690514 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.3 pIC50 47
⤷ pIC50 7.3 (IC50 5x10-8 M) [47]
VEGF receptor 2 kinase inhibitor I Small molecule or natural product Primary target of this compound Mm Inhibition 7.2 pIC50 69
⤷ pIC50 7.2 (IC50 7x10-8 M) [69]
VEGF receptor 2 kinase inhibitor II Small molecule or natural product Primary target of this compound Hs Inhibition 7.2 pIC50 67
⤷ pIC50 7.2 (IC50 7x10-8 M) [67]
AEE788 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 pIC50 75
⤷ pIC50 7.1 (IC50 7.7x10-8 M) [75]
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 80,86
⤷ pIC50 7.1 (IC50 9x10-8 M) [80]
pIC50 7.1 (IC50 9x10-8 M) [86]
cenisertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 15
⤷ pIC50 7.0 (IC50 9.5x10-8 M) [15]
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 33
⤷ pIC50 7.0 (IC50 1x10-7 M) [33]
telatinib Small molecule or natural product Hs Inhibition >7.0 pIC50 18
⤷ pIC50 >7.0 (IC50 <1x10-7 M) [18]
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 41
⤷ pIC50 6.9 (IC50 1.35x10-7 M) [41]
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 2
⤷ pIC50 6.8 (IC50 1.7x10-7 M) [2]
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 30
⤷ pIC50 6.7 (IC50 1.8x10-7 M) [30]
dual VEGFR/PARP inhibitor 14b Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pIC50 43
⤷ pIC50 6.7 (IC50 1.906x10-7 M) [43]
semaxanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.7 pIC50 10
⤷ pIC50 6.7 (IC50 2x10-7 M) [10]
BX-912 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pIC50 21
⤷ pIC50 6.4 (IC50 4.1x10-7 M) [21]
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 72
⤷ pIC50 6.4 (IC50 4.4x10-7 M) [72]
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 36
⤷ pIC50 6.2 (IC50 6.8x10-7 M) [36]
DMBI Small molecule or natural product Primary target of this compound Mm Inhibition 6.1 pIC50 77
⤷ pIC50 6.1 (IC50 7.94x10-7 M) [77]
compound 19a [PMID: 30503936] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.1 pIC50 58
⤷ pIC50 6.1 (IC50 8.5x10-7 M) [58]
lazertinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition <6.0 pIC50 65
⤷ pIC50 <6.0 (IC50 >1x10-6 M) [65]
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 21
⤷ pIC50 6.0 (IC50 1.1x10-6 M) [21]
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 7
⤷ pIC50 4.5 (IC50 3.162x10-5 M) [7]
dovitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition - pIC50 59,76
⤷ pIC50 (IC50 6.5x10-8 – 1.3x10-8 M) [59,76]
compound T.14 Small molecule or natural product Immunopharmacology Ligand Hs Inhibition - - 14
⤷ [14]
View species-specific inhibitor tables
Inhibitor Comments
Note that pazopanib is a multi-target kinase inhibitor. See [31] 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 [87].
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 39
⤷ pKd 9.6 (Kd 2.3x10-10 M) [39]
Description: Dissociation constant for scVEGF-binding to dimeric VEGFR2.
pKd 8.0 (Kd 1x10-8 M) [39]
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 45
⤷ pKd 10.3 (Kd 5x10-11 M) [45]
ramucirumab Peptide Approved drug Primary target of this compound Hs Antagonist 9.0 pIC50 45
⤷ pIC50 9.0 (IC50 1x10-9 M) [45]
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: 16,82
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: 4,25
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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Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family: kinase insert domain receptor. Last modified on 28/08/2023. Accessed on 24/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1813.