Gene and Protein Information
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

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
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
	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
	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
EC Number: 2.7.10.1

Natural/Endogenous Ligands
VEGFA {Sp: Human}
VEGFC {Sp: Human}
VEGFE {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 pegdinetanib Hs Inhibition ~9.0 pKd 28 ⤷ pKd ~9.0 (Kd ~1x10-9 M) [28] cediranib Hs Inhibition 9.0 pKd 16 ⤷ pKd 9.0 (Kd 1.1x10-9 M) [16] SU-14813 Hs Inhibition 8.6 pKd 16 ⤷ pKd 8.6 (Kd 2.3x10-9 M) [16] motesanib Hs Inhibition 8.6 pKd 16 ⤷ pKd 8.6 (Kd 2.6x10-9 M) [16] BIBF-1202 Hs Inhibition 8.5 pKd 16 ⤷ pKd 8.5 (Kd 2.9x10-9 M) [16] axitinib Hs Inhibition 8.2 pKd 16 ⤷ pKd 8.2 (Kd 5.9x10-9 M) [16] pazopanib Hs Inhibition 7.8 pKd 16 ⤷ pKd 7.8 (Kd 1.4x10-8 M) [16] RG-1530 Hs Inhibition 7.8 pKd 74 ⤷ pKd 7.8 (Kd 1.5x10-8 M) [74] sorafenib Hs Inhibition 7.2 pKd 16 ⤷ pKd 7.2 (Kd 5.9x10-8 M) [16] vatalanib Hs Inhibition 7.2 pKd 16 ⤷ pKd 7.2 (Kd 6.2x10-8 M) [16] toceranib Hs Inhibition 8.2 pKi 44 ⤷ pKi 8.2 (Ki 6x10-9 M) [44] PLX-4720 Hs Inhibition 8.1 pKi 50 ⤷ pKi 8.1 (Ki 9x10-9 M) [50] pamufetinib Hs Inhibition 7.9 pKi 24 ⤷ pKi 7.9 (Ki 1.2x10-8 M) [24] VEGF receptor tyrosine kinase inhibitor II Hs Inhibition 7.8 pKi 17 ⤷ pKi 7.8 (Ki 1.5x10-8 M) [17] cabozantinib Hs Inhibition 10.5 pIC50 85 ⤷ pIC50 10.5 (IC50 3.5x10-11 M) [85] tivozanib Hs Inhibition 9.8 pIC50 51 ⤷ pIC50 9.8 (IC50 1.6x10-10 M) [51] axitinib Hs Inhibition 9.6 pIC50 42 ⤷ pIC50 9.6 (IC50 2.5x10-10 M) [42] canlitinib Hs Inhibition 9.4 pIC50 71 ⤷ pIC50 9.4 (IC50 3.8x10-10 M) [71] cediranib Hs Inhibition >9.0 pIC50 79 ⤷ pIC50 >9.0 (IC50 <1x10-9 M) [79] VEGF receptor tyrosine kinase inhibitor III Hs Inhibition 9.0 pIC50 20 ⤷ pIC50 9.0 (IC50 1x10-9 M) [20] rivoceranib Hs Inhibition 9.0 pIC50 73 ⤷ pIC50 9.0 (IC50 1x10-9 M) [73] Description: Assay used apatinib mesylate (YN968D1) tesevatinib Hs Inhibition 8.8 pIC50 27 ⤷ pIC50 8.8 (IC50 1.5x10-9 M) [27] compound 13a [PMID: 23639540] Hs Inhibition 8.8 pIC50 19 ⤷ pIC50 8.8 (IC50 1.68x10-9 M) [19] MLKL compound 1 Hs Inhibition 8.7 pIC50 60 ⤷ pIC50 8.7 (IC50 2x10-9 M) [60] ilorasertib 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 Hs Inhibition 8.2 – 9.1 pIC50 51 ⤷ pIC50 8.2 – 9.1 (IC50 6.8x10-9 – 8x10-10 M) [51] tinengotinib Hs Inhibition 8.6 pIC50 83 ⤷ pIC50 8.6 (IC50 2.5x10-9 M) [83] motesanib Hs Inhibition 8.5 pIC50 51 ⤷ pIC50 8.5 (IC50 3x10-9 M) [51] compound 8i [PMID: 22765894] 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 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 Hs Inhibition 8.4 pIC50 3 ⤷ pIC50 8.4 (IC50 4x10-9 M) [3] lenvatinib Hs Inhibition 8.4 pIC50 51 ⤷ pIC50 8.4 (IC50 4x10-9 M) [51] lucitanib Hs Inhibition 8.4 pIC50 88 ⤷ pIC50 8.4 (IC50 4x10-9 M) [88] CEP-11981 Hs Inhibition 8.4 pIC50 35 ⤷ pIC50 8.4 (IC50 4x10-9 M) [35] compound 8h [PMID: 22765894] Hs Inhibition 8.4 pIC50 38 ⤷ pIC50 8.4 (IC50 4.2x10-9 M) [38] famitinib Hs Inhibition 8.3 pIC50 12 ⤷ pIC50 8.3 (IC50 5x10-9 M) [12] sitravatinib Hs Inhibition 8.3 pIC50 55 ⤷ pIC50 8.3 (IC50 5x10-9 M) [55] Description: In a biochemical enzyme activity assay. tafetinib Hs Inhibition 8.3 pIC50 78 ⤷ pIC50 8.3 (IC50 5x10-9 M) [78] Description: In a radiometric biochemical protein kinase assay. LY2874455 Hs Inhibition 8.1 pIC50 87 ⤷ pIC50 8.1 (IC50 7x10-9 M) [87] Description: In vitro biochemical assay result ibcasertib Hs Inhibition 8.1 pIC50 89 ⤷ pIC50 8.1 (IC50 7x10-9 M) [89] Description: Inhibition in a biochemical assay. OSI-930 Hs Inhibition 8.1 pIC50 26 ⤷ pIC50 8.1 (IC50 9x10-9 M) [26] altiratinib Hs Inhibition 8.0 pIC50 22 ⤷ pIC50 8.0 (IC50 9.2x10-9 M) [22] vandetanib Hs Inhibition 8.0 pIC50 32 ⤷ pIC50 8.0 (IC50 9x10-9 M) [32] glesatinib Hs Inhibition 8.0 pIC50 13 ⤷ pIC50 8.0 (IC50 1x10-8 M) [13] CP-547632 Hs Inhibition 8.0 pIC50 8 ⤷ pIC50 8.0 (IC50 1.1x10-8 M) [8] Ki-20227 Hs Inhibition 7.9 pIC50 53 ⤷ pIC50 7.9 (IC50 1.2x10-8 M) [53] PP121 Hs Inhibition 7.9 pIC50 5 ⤷ pIC50 7.9 (IC50 1.2x10-8 M) [5] regorafenib Hs Inhibition 7.9 pIC50 81 ⤷ pIC50 7.9 (IC50 1.3x10-8 M) [81] golvatinib 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 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 Hs Inhibition 7.7 pIC50 23 ⤷ pIC50 7.7 (IC50 1.9x10-8 M) [23] SU5402 Hs Inhibition 7.7 pIC50 68 ⤷ pIC50 7.7 (IC50 2x10-8 M) [68] vatalanib Hs Inhibition 7.7 pIC50 40 ⤷ pIC50 7.7 (IC50 2.1x10-8 M) [40] nintedanib Hs Inhibition 7.7 pIC50 34 ⤷ pIC50 7.7 (IC50 2.1x10-8 M) [34] surufatinib 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 Hs Inhibition 7.7 pIC50 63 ⤷ pIC50 7.7 (IC50 2.17x10-8 M) [63] sunitinib Hs Inhibition 7.7 pIC50 37 ⤷ pIC50 7.7 (IC50 2.26x10-8 M) [37] fexagratinib Hs Inhibition 7.6 pIC50 6 ⤷ pIC50 7.6 (IC50 2.4x10-8 M) [6] brivanib Hs Inhibition 7.6 pIC50 9 ⤷ pIC50 7.6 (IC50 2.5x10-8 M) [9] SU11652 Hs Inhibition 7.6 pIC50 66 ⤷ pIC50 7.6 (IC50 2.7x10-8 M) [66] henatinib Hs Inhibition 7.6 pIC50 12 ⤷ pIC50 7.6 (IC50 2.7x10-8 M) [12] fruquintinib 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 Hs Inhibition 7.5 pIC50 31 ⤷ pIC50 7.5 (IC50 3x10-8 M) [31] pralsetinib Hs Inhibition 7.5 pIC50 64 ⤷ pIC50 7.5 (IC50 3.5x10-8 M) [64] Description: In a biochemical assay. ENMD-2076 Hs Inhibition 7.4 pIC50 57 ⤷ pIC50 7.4 (IC50 3.6x10-8 M) [57] erdafitinib Hs Inhibition 7.4 pIC50 61 ⤷ pIC50 7.4 (IC50 3.63x10-8 M) [61] ningetinib Hs Inhibition 7.4 pIC50 84 ⤷ pIC50 7.4 (IC50 3.7x10-8 M) [84] MK-2461 Hs Inhibition 7.4 pIC50 54 ⤷ pIC50 7.4 (IC50 4.4x10-8 M) [54] catequentinib Hs Inhibition 7.3 pIC50 11 ⤷ pIC50 7.3 (IC50 4.5x10-8 M) [11] Description: In vitro activity SU-14813 Hs Inhibition 7.3 pIC50 56 ⤷ pIC50 7.3 (IC50 5x10-8 M) [56] BMS-690514 Hs Inhibition 7.3 pIC50 47 ⤷ pIC50 7.3 (IC50 5x10-8 M) [47] VEGF receptor 2 kinase inhibitor I Mm Inhibition 7.2 pIC50 69 ⤷ pIC50 7.2 (IC50 7x10-8 M) [69] VEGF receptor 2 kinase inhibitor II Hs Inhibition 7.2 pIC50 67 ⤷ pIC50 7.2 (IC50 7x10-8 M) [67] AEE788 Hs Inhibition 7.1 pIC50 75 ⤷ pIC50 7.1 (IC50 7.7x10-8 M) [75] sorafenib Hs Inhibition 7.1 pIC50 80,86 ⤷ pIC50 7.1 (IC50 9x10-8 M) [86] pIC50 7.1 (IC50 9x10-8 M) [80] cenisertib 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 Hs Inhibition 7.0 pIC50 33 ⤷ pIC50 7.0 (IC50 1x10-7 M) [33] telatinib Hs Inhibition >7.0 pIC50 18 ⤷ pIC50 >7.0 (IC50 <1x10-7 M) [18] mivavotinib 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 Hs Inhibition 6.8 pIC50 2 ⤷ pIC50 6.8 (IC50 1.7x10-7 M) [2] Description: In vitro inhibition of KDR. infigratinib Hs Inhibition 6.7 pIC50 30 ⤷ pIC50 6.7 (IC50 1.8x10-7 M) [30] dual VEGFR/PARP inhibitor 14b Hs Inhibition 6.7 pIC50 43 ⤷ pIC50 6.7 (IC50 1.906x10-7 M) [43] semaxanib Hs Inhibition 6.7 pIC50 10 ⤷ pIC50 6.7 (IC50 2x10-7 M) [10] BX-912 Hs Inhibition 6.4 pIC50 21 ⤷ pIC50 6.4 (IC50 4.1x10-7 M) [21] pexidartinib Hs Inhibition 6.4 pIC50 72 ⤷ pIC50 6.4 (IC50 4.4x10-7 M) [72] orantinib Hs Inhibition 6.2 pIC50 36 ⤷ pIC50 6.2 (IC50 6.8x10-7 M) [36] DMBI Mm Inhibition 6.1 pIC50 77 ⤷ pIC50 6.1 (IC50 7.94x10-7 M) [77] compound 19a [PMID: 30503936] Hs Inhibition 6.1 pIC50 58 ⤷ pIC50 6.1 (IC50 8.5x10-7 M) [58] lazertinib Hs Inhibition <6.0 pIC50 65 ⤷ pIC50 <6.0 (IC50 >1x10-6 M) [65] Description: In a biochemical enzyme activity assay. BX-795 Hs Inhibition 6.0 pIC50 21 ⤷ pIC50 6.0 (IC50 1.1x10-6 M) [21] GSK2646264 Hs Inhibition 4.5 pIC50 7 ⤷ pIC50 4.5 (IC50 3.162x10-5 M) [7] dovitinib Hs Inhibition - pIC50 59,76 ⤷ pIC50 (IC50 6.5x10-8 – 1.3x10-8 M) [59,76] compound T.14 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} 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 Hs Antagonist 10.3 pKd 45 ⤷ pKd 10.3 (Kd 5x10-11 M) [45] ramucirumab Hs Antagonist 9.0 pIC50 45 ⤷ pIC50 9.0 (IC50 1x10-9 M) [45]

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: 16,82
Key to terms and symbols		Click column headers to sort
Target used in screen: VEGFR2
Ligand Sp. Type Action Value Parameter cediranib Hs Inhibitor Inhibition 9.0 pKd sunitinib Hs Inhibitor Inhibition 8.8 pKd SU-14813 Hs Inhibitor Inhibition 8.6 pKd brivanib Hs Inhibitor Inhibition 8.3 pKd axitinib Hs Inhibitor Inhibition 8.2 pKd linifanib Hs Inhibitor Inhibition 8.1 pKd foretinib Hs Inhibitor Inhibition 7.9 pKd pazopanib Hs Inhibitor Inhibition 7.8 pKd Ki-20227 Hs Inhibitor Inhibition 7.7 pKd motesanib 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
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 Hs Inhibitor Inhibition 1.9 109.0 104.0 SB 218078 Hs Inhibitor Inhibition 4.5 38.0 18.0 staurosporine Hs Inhibitor Inhibition 4.5 1.5 0.5 Cdk1/2 inhibitor III Hs Inhibitor Inhibition 6.5 0.0 0.0 TWS119 Hs Inhibitor Inhibition 6.7 5.0 2.0 vandetanib Hs Inhibitor Inhibition 12.6 SU11652 Hs Inhibitor Inhibition 13.8 2.0 1.0 pazopanib Hs Inhibitor Inhibition 16.9 VEGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 19.7 K-252a Hs Inhibitor Inhibition 20.0 3.0 0.0