DGIdb - KDR Gene Record

KDR 3791 Druggable GenomeClinically Actionable

Alternate Names:

3791
KINASE INSERT DOMAIN RECEPTOR
KDR
CD309
FLK1
VEGFR
VEGFR2
191306
6307
ENSG00000128052
OTTHUMG00000128734
P35968
3153
VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2
VGFR2_HUMAN
PA30086
VEGFR2/3
VEGFR1/2/3
VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2 PRECURSOR (EC 2.7.1.112) (VEGFR-2) (KINASE INSERT DOMAIN RECEPTOR) (PROTEIN-TYROSINE KINASE RECEPTOR FLK-1). [SOURCE:UNIPROT/SWISSPROT;ACC:P35968]
PROTEIN-TYROSINE KINASE RECEPTOR FLK-1
VEGFR-2
FETAL LIVER KINASE 1
CD_antigen=CD309
FLK-1
T80975

Gene Info:

Target Class	Receptors
Target Subclass	EC:2.7.10.1
Human Readable Name	KINASE
Interpro Name	Serine-threonine/tyrosine-protein kinase catalytic domain
Interpro Type	Domain
Human Readable Name	DRUGGABLE GENOME
Interpro Short Name	Ser-Thr/Tyr_kinase_cat_dom
Uniprot Evidence	1: Evidence at protein level
Interpro Acc	IPR001245
Uniprot Status	Swiss-Prot
CancerCommons Reported Gene Name	VEGF, PDGF
Target Main Class	Receptors
Target Subclass	Kinase
Target Subclass	Other
Transmembrane Helix Count	1
Gene Biotype	PROTEIN_CODING

(25 More Sources)

Gene Categories: Category Details

KINASE
TYROSINE KINASE
EXTERNAL SIDE OF PLASMA MEMBRANE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE

Publications:

Matsui et al., 2008, E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition., Int. J. Cancer
Maitland ML et al., 2010, Vascular endothelial growth factor pathway., Pharmacogenet Genomics
Coxon et al., 2012, Anti-tumor activity of motesanib in a medullary thyroid cancer model., J. Endocrinol. Invest.
Gong L et al., 2017, PharmGKB summary: sorafenib pathways., Pharmacogenet Genomics
Escudier B et al., 2015, Genotype Correlations With Blood Pressure and Efficacy From a Randomized Phase III Trial of Second-Line Axitinib Versus Sorafenib in Metastatic Renal Cell Carcinoma., Clin Genitourin Cancer
Zheng YB et al., 2014, The relationship of kinase insert domain receptor gene polymorphisms and clinical outcome in advanced hepatocellular carcinoma patients treated with sorafenib., Med Oncol
Scartozzi M et al., 2014, VEGF and VEGFR genotyping in the prediction of clinical outcome for HCC patients receiving sorafenib: the ALICE-1 study., Int J Cancer
Jain L et al., 2010, Hypertension and hand-foot skin reactions related to VEGFR2 genotype and improved clinical outcome following bevacizumab and sorafenib., J Exp Clin Cancer Res
Antonescu et al., 2009, KDR activating mutations in human angiosarcomas are sensitive to specific kinase inhibitors., Cancer Res.
Schöffski et al., 2006, Emerging role of tyrosine kinase inhibitors in the treatment of advanced renal cell cancer: a review., Ann. Oncol.
Adnane et al., 2006, Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature., Meth. Enzymol.
Veronese et al., 2006, Mechanisms of hypertension associated with BAY 43-9006., J. Clin. Oncol.
Rini, 2006, Sorafenib., Expert Opin Pharmacother
Lacouture et al., 2006, Inflammation of actinic keratoses subsequent to therapy with sorafenib, a multitargeted tyrosine-kinase inhibitor., Clin. Exp. Dermatol.
Machado VA et al., 2015, Synthesis, antiangiogenesis evaluation and molecular docking studies of 1-aryl-3-[(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas: Discovery of a new substitution pattern for type II VEGFR-2 Tyr kinase inhibitors., Bioorg Med Chem
Li GB et al., 2015, LEADOPT: an automatic tool for structure-based lead optimization, and its application in structural optimizations of VEGFR2 and SYK inhibitors., Eur J Med Chem
Wedge et al., 2005, AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer., Cancer Res.
Sonpavde et al., 2007, Pazopanib: a novel multitargeted tyrosine kinase inhibitor., Curr Oncol Rep
Maitland ML et al., 2015, Identification of a variant in KDR associated with serum VEGFR2 and pharmacodynamics of Pazopanib., Clin Cancer Res
Xu F et al., 2013, Discovery of 4-amino-2-(thio)phenol derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: synthesis and biological evaluation. Part II., Eur J Med Chem
Grande E et al., 2015, Pazopanib in pretreated advanced neuroendocrine tumors: a phase II, open-label trial of the Spanish Task Force Group for Neuroendocrine Tumors (GETNE)., Ann Oncol
Ravi V et al., 2016, Antitumor Response of VEGFR2- and VEGFR3-Amplified Angiosarcoma to Pazopanib., J Natl Compr Canc Netw
Iwata H et al., 2011, Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2., Bioorg Med Chem
Perspicace E et al., 2013, Design, synthesis and biological evaluation of new classes of thieno[3,2-d]pyrimidinone and thieno[1,2,3]triazine as inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2)., Eur J Med Chem
Choi HE et al., 2011, BRN-103, a novel nicotinamide derivative, inhibits VEGF-induced angiogenesis and proliferation in human umbilical vein endothelial cells., Bioorg Med Chem Lett
Quek R et al., 2009, Gastrointestinal stromal tumor: a clinical overview., Hematol Oncol Clin North Am
Mendel et al., 2003, In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship., Clin. Cancer Res.
Wragg et al., 2017, Sunitinib Treatment Enhances Metastasis of Innately Drug-Resistant Breast Tumors., Cancer Res.
Wang et al., 2016, Recurrent Olfactory Neuroblastoma Treated With Cetuximab and Sunitinib: A Case Report., Medicine (Baltimore)
Gallagher et al., 2010, Phase II study of sunitinib in patients with metastatic urothelial cancer., J. Clin. Oncol.
Schueneman et al., 2003, SU11248 maintenance therapy prevents tumor regrowth after fractionated irradiation of murine tumor models., Cancer Res.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Barattè et al., 2004, Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction., J Chromatogr A
Amino et al., 2006, YM-359445, an orally bioavailable vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor, has highly potent antitumor activity against established tumors., Clin. Cancer Res.
Silva E et al., 2015, Refractory angiosarcoma of the breast with VEGFR2 upregulation successfully treated with sunitinib., Breast J
O'Hare et al., 2009, AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance., Cancer Cell
Yamamoto et al., 2007, Vascular endothelial growth factor receptor tyrosine kinase inhibitor PTK787/ZK 222584 inhibits both the induction and elicitation phases of contact hypersensitivity., J. Dermatol.
Goodkin et al., 1990, Arteriovenous malformation and glioma: coexistent or sequential? Case report., J. Neurosurg.
Spratlin et al., 2010, Phase I pharmacologic and biologic study of ramucirumab (IMC-1121B), a fully human immunoglobulin G1 monoclonal antibody targeting the vascular endothelial growth factor receptor-2., J. Clin. Oncol.
Nilsson et al., 2016, KDR Amplification Is Associated with VEGF-Induced Activation of the mTOR and Invasion Pathways but does not Predict Clinical Benefit to the VEGFR TKI Vandetanib., Clin. Cancer Res.
Millward MJ et al., 2006, The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study., Br J Cancer
Bamborough et al., 2008, Assessment of chemical coverage of kinome space and its implications for kinase drug discovery., J. Med. Chem.
Soria et al., 2014, Phase I/IIa study evaluating the safety, efficacy, pharmacokinetics, and pharmacodynamics of lucitanib in advanced solid tumors., Ann. Oncol.
Cohen et al., 2008, Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study., J. Clin. Oncol.
Mita MM et al., 2007, A phase II, pharmacokinetic, and biologic study of semaxanib and thalidomide in patients with metastatic melanoma., Cancer Chemother Pharmacol
Fury MG et al., 2007, A Phase II study of SU5416 in patients with advanced or recurrent head and neck cancers., Invest New Drugs
Hoff PM et al., 2006, A Phase I study of escalating doses of the tyrosine kinase inhibitor semaxanib (SU5416) in combination with irinotecan in patients with advanced colorectal carcinoma., Jpn J Clin Oncol
Villalta SA et al., 2013, Inhibition of VEGFR-2 reverses type 1 diabetes in NOD mice by abrogating insulitis and restoring islet function., Diabetes
Hilberg et al., 2008, BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy., Cancer Res.
Roth GJ et al., 2009, Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120)., J Med Chem
Wind S et al., 2019, Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib., Clin Pharmacokinet
Fujita et al., 2013, The novel VEGF receptor/MET-targeted kinase inhibitor TAS-115 has marked in vivo antitumor properties and a favorable tolerability profile., Mol. Cancer Ther.
Yakes et al., 2011, Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth., Mol. Cancer Ther.
Kurzrock et al., 2011, Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer., J. Clin. Oncol.
Loaiza-Bonilla et al., 2016, KDR Mutation as a Novel Predictive Biomarker of Exceptional Response to Regorafenib in Metastatic Colorectal Cancer., Cureus
Miyazawa et al., 2010, Phase I clinical trial using peptide vaccine for human vascular endothelial growth factor receptor 2 in combination with gemcitabine for patients with advanced pancreatic cancer., Cancer Sci.
Gingrich DE et al., 2003, A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clinical candidate CEP-7055., J Med Chem
Shi W et al., 2011, Itraconazole side chain analogues: structure-activity relationship studies for inhibition of endothelial cell proliferation, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and hedgehog signaling., J Med Chem
Graham Robinett R et al., 2007, The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors., Bioorg Med Chem Lett

PF-00337210 KDR

Interaction Score: 1.47

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
23835340

Sources:
ChemblInteractions TTD
PEGDINETANIB KDR

Interaction Score: 1.47

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name CT-322

Novel drug target Established target

PMIDs:
None found

Sources:
TALC TdgClinicalTrial TTD
RIVOCERANIB KDR

Interaction Score: 1.47

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions TTD
TAS-115 KDR

Interaction Score: 0.74

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type pancreatic cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
24140932

Sources:
JAX-CKB ChemblInteractions
RAMUCIRUMAB KDR

Interaction Score: 0.65

Interaction Types & Directionality:

antibody (inhibitory)

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name IMC-1121B

Novel drug target Established target

Notes

PMIDs:
2182794 20048182

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions TTD
ZD-4190 KDR

Interaction Score: 0.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CEP-5214 KDR

Interaction Score: 0.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
14640546

Sources:
DTC ChemblInteractions
DELPHINIDIN KDR

Interaction Score: 0.49

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ALACIZUMAB PEGOL KDR

Interaction Score: 0.49

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor 2 antagonist

PMIDs:
None found

Sources:
ChemblInteractions
RIVOCERANIB MESYLATE KDR

Interaction Score: 0.49

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ELPAMOTIDE KDR

Interaction Score: 0.49

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
TIVOZANIB KDR

Interaction Score: 0.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name AV-951

Novel drug target Established target

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

PMIDs:
None found

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions TTD
RAF-265 KDR

Interaction Score: 0.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name CHIR-265

Novel drug target Established target

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

PMIDs:
None found

Sources:
MyCancerGenome TdgClinicalTrial ChemblInteractions TTD
MOTESANIB KDR

Interaction Score: 0.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Trial Name motesanib diphosphate, AMG 706

PMIDs:
20124951 21422803

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions PharmGKB
FRUQUINTINIB KDR

Interaction Score: 0.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Trial Name fruquintinib

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TTD
HENATINIB KDR

Interaction Score: 0.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AXITINIB KDR

Interaction Score: 0.41

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Reported Cancer Type Prostate

PMIDs:
20124951 18541897

Sources:
TALC MyCancerGenome TdgClinicalTrial ChemblInteractions CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD
TELATINIB KDR

Interaction Score: 0.41

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name telatinib

Novel drug target Established target

PMIDs:
None found

Sources:
TALC MyCancerGenome TdgClinicalTrial ChemblInteractions TTD
LUCITANIB KDR

Interaction Score: 0.33

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Evidence Type Actionable

PMIDs:
25193991

Sources:
JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial
GOLVATINIB KDR

Interaction Score: 0.33

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
SUNITINIB KDR

Interaction Score: 0.33

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
21885287 23583911 21963305 20124951 19248971 12538485 28011623 27149458 20142593 19723655 16418310 12873999 11752352 14753710 16533791 25639617

Sources:
TALC DTC MyCancerGenome TdgClinicalTrial JAX-CKB TEND CIViC MyCancerGenomeClinicalTrial PharmGKB TTD
OSI-930 KDR

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name OSI-930

Direct Interaction yes

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TTD
BMS-690514 KDR

Interaction Score: 0.28

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
TALC MyCancerGenome ChemblInteractions TTD
BRIVANIB KDR

Interaction Score: 0.27

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
20124951

Sources:
TALC MyCancerGenome ChemblInteractions PharmGKB TTD
VATALANIB KDR

Interaction Score: 0.26

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name Vatalanib

Novel drug target Established target

PMIDs:
17584317

Sources:
TALC DTC MyCancerGenome TdgClinicalTrial ChemblInteractions TTD
BMS-794833 KDR

Interaction Score: 0.25

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CABOZANTINIB KDR

Interaction Score: 0.25

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name XL184

Novel drug target Established target

PMIDs:
21926191 21606412

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial TTD
BMS-817378 KDR

Interaction Score: 0.25

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CABOZANTINIB S-MALATE KDR

Interaction Score: 0.25

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
TELBERMIN KDR

Interaction Score: 0.25

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 1 and 2 (Flt-1 and KDR) agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TESEVATINIB KDR

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name XL647

Novel drug target Established target

PMIDs:
None found

Sources:
TALC MyCancerGenome TdgClinicalTrial
FORETINIB KDR

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name XL880

Novel drug target Established target

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

PMIDs:
None found

Sources:
TALC MyCancerGenome TdgClinicalTrial ChemblInteractions TTD
LENVATINIB KDR

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name E7080

Novel drug target Established target

Notes

PMIDs:
17943726

Sources:
TALC MyCancerGenome TdgClinicalTrial TTD
X-82 KDR

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
GW559768X KDR

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17884497

Sources:
DTC
SURUFATINIB KDR

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
TAK-593 KDR

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
NINTEDANIB KDR

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name BIBF-1120,Vargatef

Notes

PMIDs:
18559524 19522465 31016670

Sources:
TALC DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial
GLESATINIB KDR

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name MGCD265

Novel drug target Established target

PMIDs:
None found

Sources:
TALC MyCancerGenome TdgClinicalTrial
EUPATORIN KDR

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
KRN-633 KDR

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AEE-788 KDR

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
L-21649 KDR

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
ABICIPAR PEGOL KDR

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name MP0112

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
ORANTINIB KDR

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Notes

PMIDs:
None found

Sources:
TALC MyCancerGenome ChemblInteractions
AG-13958 KDR

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
JI-101 KDR

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CEP-7055 KDR

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LENVATINIB MESYLATE KDR

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SORAFENIB KDR

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

Evidence Type Actionable

Approval Status Preclinical

PMIDs:
28362716 25816720 25182707 24510746 20630084 20124951 19723655 16418310 16757355 16446323 16503817 16824050 26344591 25743214

Sources:
TALC DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB TEND CIViC MyCancerGenomeClinicalTrial PharmGKB TTD
PAZOPANIB KDR

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Pazopanib

Novel drug target Established target

Notes

PMIDs:
17288876 25411163 24036042 26063633 27160228

Sources:
TALC DTC MyCancerGenome TdgClinicalTrial CIViC MyCancerGenomeClinicalTrial PharmGKB
REGORAFENIB KDR

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name regorafenib, BAY 73-4506

Novel drug target Established target

Indication/Tumor Type colorectal cancer

PMIDs:
27004155

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial TTD
SEMAXANIB KDR

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
16736151 16983506 16449240

Sources:
ChemblInteractions
FAMITINIB KDR

Interaction Score: 0.14

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
CHIAURANIB KDR

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
4SC-203 KDR

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CM-082 KDR

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL536151 KDR

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ALTIRATINIB KDR

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
VANDETANIB KDR

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type no benefit

Approval Status Phase III

PMIDs:
26578684 20124951

Sources:
TALC DTC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial PharmGKB TTD
ITRACONAZOLE KDR

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21936514

Sources:
DTC
VADIMEZAN KDR

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Vadimezan

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
ANLOTINIB KDR

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
CEP-11981 KDR

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
MGCD-265 KDR

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
XL-820 KDR

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
PEGPLERANIB SODIUM KDR

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name E-10030

PMIDs:
None found

Sources:
TdgClinicalTrial
ENMD-2076 KDR

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

PMIDs:
None found

Sources:
TALC MyCancerGenome TdgClinicalTrial ChemblInteractions
CEDIRANIB KDR

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Novel drug target Established target

Trial Name cediranib, AZD2171,Recentin

PMIDs:
15899831

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions TTD
BRIVANIB ALANINATE KDR

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SU-014813 KDR

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PEXMETINIB KDR

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name ARRY-614

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
ROMIPLOSTIM KDR

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CP-459632 KDR

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
MIDOSTAURIN KDR

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

PMIDs:
16969355

Sources:
MyCancerGenome ChemblInteractions
RABEPRAZOLE SODIUM KDR

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome TTD
BARASERTIB KDR

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
NINTEDANIB ESYLATE KDR

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SUNITINIB MALATE KDR

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MUPARFOSTAT KDR

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Muparfostat

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
NERATINIB KDR

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PUQUITINIB KDR

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
PAZOPANIB HYDROCHLORIDE KDR

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
XL-999 KDR

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
PONATINIB KDR

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
19878872

Sources:
MyCancerGenome
MK-2461 KDR

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
TTD
LINIFANIB KDR

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name ABT-869, Linifanib

Novel drug target Established target

Notes

PMIDs:
None found

Sources:
TALC DTC MyCancerGenome TdgClinicalTrial ChemblInteractions
OSI-632 KDR

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions TTD
SORAFENIB TOSYLATE KDR

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
TG100-801 KDR

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL202721 KDR

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB KDR

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Notes

PMIDs:
None found

Sources:
TALC DTC TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions
DORAMAPIMOD KDR

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CETUXIMAB KDR

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Sunitinib

Indication/Tumor Type olfactory neuroblastoma

Response Type sensitive

PMIDs:
27149458

Sources:
JAX-CKB
AZD-1152-HQPA KDR

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAK-715 KDR

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ENMD-981693 KDR

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MLN-8054 KDR

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL406845 KDR

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SB-220025 KDR

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL546797 KDR

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
AST-487 KDR

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DTC
GW843682X KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
HESPERADIN KDR

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
19035792

Sources:
DTC
GEMCITABINE KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy VEGFR2-169 + Gemcitabine

Indication/Tumor Type pancreatic cancer

Response Type sensitive

PMIDs:
19930156

Sources:
JAX-CKB
ALISERTIB KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SNS-314 KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RG-1530 KDR

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions
GO-6976 KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL379975 KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
KENPAULLONE KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ERLOTINIB KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CYC-116 KDR

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions
JNJ-7706621 KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PD-0166285 KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ILORASERTIB KDR

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions
SOTRASTAURIN KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ENTRECTINIB KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GW441756X KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TOZASERTIB KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
R-406 KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SP-600125 KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAE-684 KDR

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PF-00562271 KDR

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CENISERTIB KDR

Interaction Score: 0.0

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DTC

Ensembl: ENSG00000128052
- Version: 101_38
Alternate Names:

KDR Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: P35968
- Version: 01-August-2011
Alternate Names:

ENSG00000128052 Ensembl Gene Id

KDR Gene Symbol

VGFR2_HUMAN Uniprot Id

Gene Info:

Target Main Class Receptors

Target Subclass Kinase

Target Subclass Other

Publications:
CancerCommons: KDR
- Version: 25-July-2013
Alternate Names:

3791 Entrez Gene ID

Gene Info:

CancerCommons Reported Gene Name VEGF, PDGF

Publications:

RussLampel: ENSG00000128052

Version: 26-July-2011

Alternate Names:

VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2 PRECURSOR (EC 2.7.1.112) (VEGFR-2) (KINASE INSERT DOMAIN RECEPTOR) (PROTEIN-TYROSINE KINASE RECEPTOR FLK-1). [SOURCE:UNIPROT/SWISSPROT;ACC:P35968] Description

ENSG00000128052 Ensembl Gene Id

KDR Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

TdgClinicalTrial: P35968
- Version: January-2014
Alternate Names:

KDR Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass EC:2.7.10.1

Publications:
HopkinsGroom: P35968
- Version: 11-September-2012
Alternate Names:

VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2 Uniprot Protein Name

3791 Entrez Gene Id

P35968 Uniprot Accession

Gene Info:

Interpro Name Serine-threonine/tyrosine-protein kinase catalytic domain

Interpro Type Domain

Human Readable Name DRUGGABLE GENOME

Gene Categories:

KINASE, DRUGGABLE GENOME

Publications:

JAX-CKB: KDR

Version: 27-September-2017

Alternate Names:

3791 CKB Entrez Id

KDR CKB Gene Synonym

CD309 CKB Gene Synonym

Gene Info:

Publications:

Antonescu et al., 2009, KDR activating mutations in human angiosarcomas are sensitive to specific kinase inhibitors., Cancer Res.

Fujita et al., 2013, The novel VEGF receptor/MET-targeted kinase inhibitor TAS-115 has marked in vivo antitumor properties and a favorable tolerability profile., Mol. Cancer Ther.

Wang et al., 2016, Recurrent Olfactory Neuroblastoma Treated With Cetuximab and Sunitinib: A Case Report., Medicine (Baltimore)

PharmGKB: KDR

Version: 18-August-2020

Alternate Names:

PA30086 PharmGKB ID

Gene Info:

Publications:

Zheng YB et al., 2014, The relationship of kinase insert domain receptor gene polymorphisms and clinical outcome in advanced hepatocellular carcinoma patients treated with sorafenib., Med Oncol

Maitland ML et al., 2010, Vascular endothelial growth factor pathway., Pharmacogenet Genomics

Gong L et al., 2017, PharmGKB summary: sorafenib pathways., Pharmacogenet Genomics

CIViC: KDR

Version: 14-September-2020

Alternate Names:

3791 Entrez Gene ID

3153 CIViC Gene ID

Gene Info:

Publications:

Silva E et al., 2015, Refractory angiosarcoma of the breast with VEGFR2 upregulation successfully treated with sunitinib., Breast J

Antonescu et al., 2009, KDR activating mutations in human angiosarcomas are sensitive to specific kinase inhibitors., Cancer Res.

Grande E et al., 2015, Pazopanib in pretreated advanced neuroendocrine tumors: a phase II, open-label trial of the Spanish Task Force Group for Neuroendocrine Tumors (GETNE)., Ann Oncol

TTD: Vascular endothelial growth factor receptor 2
- Version: 2020.06.01
Alternate Names:

KDR TTD Gene Abbreviation

T80975 TTD Target ID

Gene Info:

Publications:

Villalta SA et al., 2013, Inhibition of VEGFR-2 reverses type 1 diabetes in NOD mice by abrogating insulitis and restoring islet function., Diabetes

DTC: KDR

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Hilberg et al., 2008, BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy., Cancer Res.

Roth GJ et al., 2009, Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120)., J Med Chem

Machado VA et al., 2015, Synthesis, antiangiogenesis evaluation and molecular docking studies of 1-aryl-3-[(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas: Discovery of a new substitution pattern for type II VEGFR-2 Tyr kinase inhibitors., Bioorg Med Chem

TALC: VEGFR2
- Version: 12-May-2016
Alternate Names:

VEGFR2 Gene Symbol

Gene Info:

Publications:
MyCancerGenome: KDR
- Version: 20-Jun-2017
Alternate Names:

3791 Entrez Gene Id

KDR MyCancerGenome Gene Symbol

VEGFR2 MyCancerGenome Reported Gene Name

Gene Info:

Publications:
TALC: VEGFR-2
- Version: 12-May-2016
Alternate Names:

VEGFR-2 Gene Symbol

Gene Info:

Publications:
TALC: VEGFR
- Version: 12-May-2016
Alternate Names:

VEGFR Gene Symbol

Gene Info:

Publications:
HingoraniCasas: ENSG00000128052
- Version: 31-May-2017
Alternate Names:

ENSG00000128052 Gene Symbol

KDR Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: FLK1
- Version: chembl_23
Alternate Names:

VEGFR2 GENE_SYMBOL

KDR GENE_SYMBOL

Vascular endothelial growth factor receptor 2 UNIPROT

Gene Info:

Publications:
GO: KDR
- Version: 01-February-2022
Alternate Names:

FLK1 GO Gene Synonym

VEGFR2 GO Gene Synonym

Gene Info:

Gene Categories:

TYROSINE KINASE, EXTERNAL SIDE OF PLASMA MEMBRANE

Publications:
Tempus: KDR
- Version: 11-November-2018
Alternate Names:

KDR Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
dGene: KDR
- Version: 27-Jun-2013
Alternate Names:

3791 Gene ID

CD309 dGene Synonym

FLK1 dGene Synonym

Gene Info:

Gene Categories:

KINASE, TYROSINE KINASE

Publications:
Pharos: KDR
- Version: 01-February-2022
Alternate Names:

Vascular endothelial growth factor receptor 2 Gene Name

P35968 UniProt ID

Gene Info:

Gene Categories:

KINASE

Publications:
MyCancerGenomeClinicalTrial: VEGFR2
- Version: 30-February-2014
Alternate Names:

Gene Info:

Publications:
MyCancerGenomeClinicalTrial: KDR
- Version: 30-February-2014
Alternate Names:

Gene Info:

Publications:
MskImpact: KDR
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
ClearityFoundationClinicalTrial: FLK1
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:
ClearityFoundationClinicalTrial: KDR
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:
FoundationOneGenes: KDR
- Version: 03-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
CarisMolecularIntelligence: KDR
- Version: 04-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
Oncomine: KDR
- Version: v3
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:

Mechanism of Interaction	Vascular endothelial growth factor receptor 2 inhibitor
Direct Interaction	yes

Indication/Tumor Type	pancreatic cancer
Response Type	sensitive
Approval Status	Preclinical

Trial Name	AV-951
Novel drug target	Established target
Mechanism of Interaction	Vascular endothelial growth factor receptor inhibitor

Trial Name	CHIR-265
Novel drug target	Established target
Mechanism of Interaction	Vascular endothelial growth factor receptor 2 inhibitor

Indication/Tumor Type	Advanced Solid Tumor
Response Type	sensitive
Approval Status	Preclinical

Notes
Mechanism of Interaction	Vascular endothelial growth factor receptor inhibitor
Direct Interaction	yes

Trial Name	XL880
Novel drug target	Established target
Mechanism of Interaction	Vascular endothelial growth factor receptor inhibitor

Trial Name	regorafenib, BAY 73-4506
Novel drug target	Established target
Indication/Tumor Type	colorectal cancer

Indication/Tumor Type	non-small cell lung carcinoma
Response Type	no benefit
Approval Status	Phase III

Trial Name	ABT-869, Linifanib
Novel drug target	Established target
Notes

antibody (inhibitory)
antagonist (inhibitory)
inhibitor (inhibitory)

combination therapy	Cetuximab + Sunitinib
Indication/Tumor Type	olfactory neuroblastoma
Response Type	sensitive

combination therapy	VEGFR2-169 + Gemcitabine
Indication/Tumor Type	pancreatic cancer
Response Type	sensitive

ENSG00000128052	Ensembl Gene Id
KDR	Gene Symbol
VGFR2_HUMAN	Uniprot Id

VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2 PRECURSOR (EC 2.7.1.112) (VEGFR-2) (KINASE INSERT DOMAIN RECEPTOR) (PROTEIN-TYROSINE KINASE RECEPTOR FLK-1). [SOURCE:UNIPROT/SWISSPROT;ACC:P35968]	Description
ENSG00000128052	Ensembl Gene Id
KDR	Display Id

VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2	Uniprot Protein Name
3791	Entrez Gene Id
P35968	Uniprot Accession

3791	Entrez Gene Id
KDR	MyCancerGenome Gene Symbol
VEGFR2	MyCancerGenome Reported Gene Name

VEGFR2	GENE_SYMBOL
KDR	GENE_SYMBOL
Vascular endothelial growth factor receptor 2	UNIPROT

Vascular endothelial growth factor receptor 2	Gene Name
P35968	UniProt ID

KDR Gene Record

KDR 3791 Druggable GenomeClinically Actionable

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor Direct Interaction yes

PMIDs: 23835340

Sources: ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Trial Name CT-322 Novel drug target Established target

PMIDs: None found

Sources: TALC TdgClinicalTrial TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor Direct Interaction yes

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type pancreatic cancer Response Type sensitive Approval Status Preclinical

PMIDs: 24140932

Sources: JAX-CKB ChemblInteractions

Interaction Types & Directionality: antibody (inhibitory) antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Trial Name IMC-1121B Novel drug target Established target Notes

PMIDs: 2182794 20048182

Sources: TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor Direct Interaction yes

PMIDs: 14640546

Sources: DTC ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Vascular endothelial growth factor receptor 2 antagonist

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name AV-951 Novel drug target Established target Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

PMIDs: None found

Sources: TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name CHIR-265 Novel drug target Established target Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

PMIDs: None found

Sources: MyCancerGenome TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor Direct Interaction yes Trial Name motesanib diphosphate, AMG 706

PMIDs: 20124951 21422803

Sources: TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor Direct Interaction yes Trial Name fruquintinib

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor Reported Cancer Type Prostate

PMIDs: 20124951 18541897

Sources: TALC MyCancerGenome TdgClinicalTrial ChemblInteractions CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Trial Name telatinib Novel drug target Established target

PMIDs: None found

Sources: TALC MyCancerGenome TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor Direct Interaction yes Evidence Type Actionable

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
23835340

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name CT-322

Novel drug target Established target

PMIDs:
None found

Sources:
TALC TdgClinicalTrial TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type pancreatic cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
24140932

Sources:
JAX-CKB ChemblInteractions

Interaction Types & Directionality:

antibody (inhibitory)

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name IMC-1121B

Novel drug target Established target

Notes

PMIDs:
2182794 20048182

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
14640546

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor 2 antagonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name AV-951

Novel drug target Established target

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

PMIDs:
None found

Sources:
TALC MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name CHIR-265

Novel drug target Established target

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

PMIDs:
None found

Sources:
MyCancerGenome TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Trial Name motesanib diphosphate, AMG 706

PMIDs:
20124951 21422803

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Trial Name fruquintinib

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Reported Cancer Type Prostate

PMIDs:
20124951 18541897

Sources:
TALC MyCancerGenome TdgClinicalTrial ChemblInteractions CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name telatinib

Novel drug target Established target

PMIDs:
None found

Sources:
TALC MyCancerGenome TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Evidence Type Actionable

PMIDs:
25193991

Sources:
JAX-CKB ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
21885287 23583911 21963305 20124951 19248971 12538485 28011623 27149458 20142593 19723655 16418310 12873999 11752352 14753710 16533791 25639617