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
1813
P35968
kinase insert domain receptor (a type III receptor tyrosine kinase)
NM_002253
NP_002244
3153
VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2
VGFR2_HUMAN
PA30086
BE0000369
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]
TTDS00008
PROTEIN-TYROSINE KINASE RECEPTOR FLK-1
VEGFR-2
FETAL LIVER KINASE 1
KINASE NYK
CD_antigen=CD309
FLK-1
T80975

Gene Info:

GuideToPharmacology Gene Category Name	Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family
GuideToPharmacology Gene Category ID	324
GuideToPharmacology Gene Type	catalytic_receptor
Target Class	Receptors
Target Subclass	EC:2.7.10.1
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
Human Readable Name	KINASE
Interpro Acc	IPR001245
Uniprot Status	Swiss-Prot
Source Reported Gene Name	KDR
Has Variant Annotation	false
Is VIP	false
CancerCommons Reported Gene Name	VEGF, PDGF
Target Main Class	Receptors
Target Subclass	Kinase
Target Subclass	Other
Transmembrane Helix Count	1
Human Readable Name	TYROSINE KINASE
Gene Biotype	PROTEIN_CODING

(27 More Sources)

Gene Categories: Category Details

KINASE
TYROSINE KINASE
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
Toledo RA et al., 2018, Exome Sequencing of Plasma DNA Portrays the Mutation Landscape of Colorectal Cancer and Discovers Mutated VEGFR2 Receptors as Modulators of Antiangiogenic Therapies., Clin Cancer Res
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
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.
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.
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.
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
Lee SJ et al., 2017, Phase I trial and pharmacokinetic study of tanibirumab, a fully human monoclonal antibody to vascular endothelial growth factor receptor 2, in patients with refractory solid tumors., Invest New Drugs
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
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
McCoach CE et al., 2018, Resistance Mechanisms to Targeted Therapies in <i>ROS1</i><sup>+</sup> and <i>ALK</i><sup>+</sup> Non-small Cell Lung Cancer., Clin Cancer Res
Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect

LENVATINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name E7080

Novel drug target Established target

Specific Action of the Ligand Inhibition

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

Toledo RA et al., 2018, Exome Sequencing of Plasma DNA Portrays the Mutation Landscape of Colorectal Cancer and Discovers Mutated VEGFR2 Receptors as Modulators of Antiangiogenic Therapies., Clin Cancer Res

MOTESANIB KDR

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

Publications:

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.

CEDIRANIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Direct Interaction? True

Endogenous Drug? False

Publications:

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.

PAZOPANIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Pazopanib

Novel drug target Established target

Notes

Publications:

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

SUNITINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

Publications:

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

VATALANIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Direct Interaction? True

Endogenous Drug? False

Publications:

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.

RAMUCIRUMAB KDR

Interaction Types & Directionality:

antibody (inhibitory)

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name IMC-1121B

Novel drug target Established target

Notes

Publications:

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.

VANDETANIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

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.

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

LUCITANIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Evidence Type Actionable

Publications:

Soria et al., 2014, Phase I/IIa study evaluating the safety, efficacy, pharmacokinetics, and pharmacodynamics of lucitanib in advanced solid tumors., Ann. Oncol.

AXITINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:

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

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.

SEMAXANIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

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

BRIVANIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

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

NINTEDANIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name BIBF-1120,Vargatef

Notes

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

Wind S et al., 2019, Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib., Clin Pharmacokinet

TAS-115 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

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.

CABOZANTINIB KDR

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:

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.

Toledo RA et al., 2018, Exome Sequencing of Plasma DNA Portrays the Mutation Landscape of Colorectal Cancer and Discovers Mutated VEGFR2 Receptors as Modulators of Antiangiogenic Therapies., Clin Cancer Res

REGORAFENIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name regorafenib, BAY 73-4506

Novel drug target Established target

Endogenous Drug? False

Publications:

Loaiza-Bonilla et al., 2016, KDR Mutation as a Novel Predictive Biomarker of Exceptional Response to Regorafenib in Metastatic Colorectal Cancer., Cureus

Toledo RA et al., 2018, Exome Sequencing of Plasma DNA Portrays the Mutation Landscape of Colorectal Cancer and Discovers Mutated VEGFR2 Receptors as Modulators of Antiangiogenic Therapies., Clin Cancer Res

ENMD-2076 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Publications:
BX-795 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

CENISERTIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a biochemical homogeneous time-resolved fluorescence (HTRF) kinase assay with an ATP concentration of 1 mM.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:

RIVOCERANIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Direct Interaction? False

Publications:
HENATINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Publications:
FRUQUINTINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Trial Name fruquintinib

Publications:
FAMITINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Publications:
TELBERMIN KDR

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

Publications:
FORETINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:
GLESATINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Direct Interaction? False

Endogenous Drug? False

Publications:
TAK-593 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Publications:
OSI-632 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:
LENVATINIB MESYLATE KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Publications:
CEP-7055 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Publications:
RAF-265 KDR

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

Publications:
JI-101 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Publications:
PLX-4720 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:
BMS-690514 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:
PRALSETINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
GOLVATINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Measured as inhibition of VEGFR-2 autophosphorylation in HUVEC cells.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:
TIVOZANIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name AV-951

Novel drug target Established target

Specific Action of the Ligand Inhibition

Publications:
AG-13958 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Publications:
XL-999 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Publications:
TELATINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name telatinib

Novel drug target Established target

Publications:
CABOZANTINIB S-MALATE KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Publications:
PEGDINETANIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name CT-322

Novel drug target Established target

Publications:
ALTIRATINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
ANLOTINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Details of the Assay for Interaction In vitro activity

Publications:
ORANTINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
TG100-801 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Publications:
LINIFANIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
SUNITINIB MALATE KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Publications:
XL-820 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Publications:
MGCD-265 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Publications:
OSI-930 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name OSI-930

Direct Interaction yes

Publications:
DOVITINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
CEP-11981 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
TESEVATINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Trial Name XL647

Novel drug target Established target

Publications:

ILORASERTIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Details of the Assay for Interaction Measuring inhibition of kinase activity in a biochemical assay.

Publications:

INFIGRATINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
chembl:CHEMBL1908396 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
PEXIDARTINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
PAZOPANIB HYDROCHLORIDE KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Publications:
BMS-817378 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Publications:
PUQUITINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Publications:
MK-2461 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
ALACIZUMAB PEGOL KDR

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor 2 antagonist

Publications:
RG-1530 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Publications:
CM-082 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Publications:
NINTEDANIB ESYLATE KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Publications:
4SC-203 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Publications:
ENMD-981693 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Publications:
CYC-116 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Publications:
AST-487 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In vitro inhibition of KDR.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:
SU-014813 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Direct Interaction? True

Publications:
SORAFENIB TOSYLATE KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Publications:
CP-459632 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Publications:
CHIAURANIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Publications:
L-21649 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Publications:
BRIVANIB ALANINATE KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Publications:
BMS-794833 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Publications:
SITRAVATINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a biochemical enzyme activity assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:
ZD-4190 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Publications:
AEE-788 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:
SURUFATINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a biochemical assay using recombinant KDR kinase catalytic domain.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:
DORSOMORPHIN KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:
KRN-633 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Publications:
X-82 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Publications:
LY-2874455 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In vitro biochemical assay result

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:
TAFETINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a radiometric biochemical protein kinase assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Publications:
ERDAFITINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

substrate

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

SORAFENIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Notes

Evidence Type Actionable

Approval Status Preclinical

Publications:

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

PONATINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

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
MIDOSTAURIN KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Publications:

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
HESPERADIN KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Bamborough et al., 2008, Assessment of chemical coverage of kinome space and its implications for kinase drug discovery., J. Med. Chem.
PF-00337210 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

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

CEP-5214 KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Publications:

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

FOSTAMATINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect
RABEPRAZOLE SODIUM KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:
RIPRETINIB KDR

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

ELPAMOTIDE KDR

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Elpamotide + Gemcitabine

Indication/Tumor Type pancreatic cancer

Response Type sensitive

Publications:

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.

OLINVACIMAB KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase I

Response Type predicted - sensitive

Publications:

Lee SJ et al., 2017, Phase I trial and pharmacokinetic study of tanibirumab, a fully human monoclonal antibody to vascular endothelial growth factor receptor 2, in patients with refractory solid tumors., Invest New Drugs

GEMCITABINE KDR

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy VEGFR2-169 + Gemcitabine

Indication/Tumor Type pancreatic cancer

Response Type sensitive

Publications:

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.

CETUXIMAB KDR

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Cetuximab + Sunitinib

Indication/Tumor Type olfactory neuroblastoma

Response Type sensitive

Publications:

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

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Case Reports/Case Series

Response Type predicted - resistant

Publications:

McCoach CE et al., 2018, Resistance Mechanisms to Targeted Therapies in ROS1+ and ALK+ Non-small Cell Lung Cancer., Clin Cancer Res
PEGPLERANIB SODIUM KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name E-10030

Publications:
PEXMETINIB KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name ARRY-614

Novel drug target Established target

Publications:
ABICIPAR PEGOL KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name MP0112

Novel drug target Established target

Publications:
VADIMEZAN KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Vadimezan

Novel drug target Established target

Publications:
MUPARFOSTAT KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Muparfostat

Novel drug target Established target

Publications:

ITRACONAZOLE KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

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

GW559768X KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Graham Robinett R et al., 2007, The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors., Bioorg Med Chem Lett
DORAMAPIMOD KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL1681932 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
DASATINIB KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ERLOTINIB KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL379975 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
JNJ-7706621 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TAE-684 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
PF-00562271 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL230686 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TAK-715 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
GW441756X KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
SNS-314 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
R-406 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
MLN-8054 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ALISERTIB KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
RIVOCERANIB MESYLATE KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
SP-600125 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL536151 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
GO-6976 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL380316 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL370586 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ENTRECTINIB KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL460989 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
SU-11652 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL193342 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL261592 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
DELPHINIDIN KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
GW843682X KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
PD-0166285 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
NERATINIB KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
IMC-1C11 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL401930 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL606964 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL202721 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TOZASERTIB KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
ROMIPLOSTIM KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
AZD-1152-HQPA KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
SB-220025 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
L000021649 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL150315 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
BARASERTIB KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL406845 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
KENPAULLONE KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL153843 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
SOTRASTAURIN KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL546797 KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
EUPATORIN KDR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ensembl: ENSG00000128052
- Version: 101_38
Alternate Names:

KDR Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:

GuideToPharmacologyGenes: 1813

Version: 4-March-2015

Alternate Names:

3791 Entrez Gene ID

kinase insert domain receptor (a type III receptor tyrosine kinase) HUGO Gene Name

6307 HUGO Gene ID

Gene Info:

GuideToPharmacology Gene Category Name Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family

GuideToPharmacology Gene Category ID 324

GuideToPharmacology Gene Type catalytic_receptor

Gene Categories:

KINASE, TYROSINE KINASE

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:

PharmGKB: KDR

Version: 18-August-2020

Alternate Names:

PA30086 PharmGKB ID

Gene Info:

Publications:

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

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

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

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

JAX-CKB: KDR

Version: 15-September-2020

Alternate Names:

3791 CKB Entrez Id

KDR CKB Gene Synonym

CD309 CKB Gene Synonym

Gene Info:

Publications:

Chinnasamy et al., 2010, Gene therapy using genetically modified lymphocytes targeting VEGFR-2 inhibits the growth of vascularized syngenic tumors in mice., J. Clin. Invest.

Chinnasamy et al., 2013, Simultaneous targeting of tumor antigens and the tumor vasculature using T lymphocyte transfer synergize to induce regression of established tumors in mice., Cancer Res.

Coxon et al., 2012, Anti-tumor activity of motesanib in a medullary thyroid cancer model., J. Endocrinol. Invest.

DrugBank: BE0000369

Version: 5.1.7

Alternate Names:

KDR DrugBank Gene Name

P35968 UniProt Accession

3791 Entrez Gene Id

Gene Info:

Publications:

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.

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

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

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

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:
GuideToPharmacologyInteractions: ENSG00000128052
- Version: 20-July-2020
Alternate Names:

kinase insert domain receptor GuideToPharmacology Name

P35968 UniProtKB ID

Gene Info:

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

Vascular endothelial growth factor receptor 2 Gene Name

P35968 UniProt ID

Gene Info:

Gene Categories:

KINASE

Publications:
GO: KDR
- Version: 05-September-2020
Alternate Names:

FLK1 GO Gene Synonym

VEGFR2 GO Gene Synonym

Gene Info:

Gene Categories:

TYROSINE KINASE

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

KDR Gene Symbol

Gene Info:

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:
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:

Trial Name	E7080
Novel drug target	Established target
Specific Action of the Ligand	Inhibition

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

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

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Inhibition

Notes
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Trial Name	regorafenib, BAY 73-4506
Novel drug target	Established target
Endogenous Drug?	False

Details of the Assay for Interaction	In a biochemical homogeneous time-resolved fluorescence (HTRF) kinase assay with an ATP concentration of 1 mM.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

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

Details of the Assay for Interaction	Measured as inhibition of VEGFR-2 autophosphorylation in HUVEC cells.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Trial Name	AV-951
Novel drug target	Established target
Specific Action of the Ligand	Inhibition

Details of the Assay for Interaction	<i>In vitro</i> inhibition of KDR.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	In a biochemical enzyme activity assay.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	In a biochemical assay using recombinant KDR kinase catalytic domain.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	<i>In vitro</i> biochemical assay result
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	In a radiometric biochemical protein kinase assay.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

combination therapy	Elpamotide + Gemcitabine
Indication/Tumor Type	pancreatic cancer
Response Type	sensitive

Evidence Type	Actionable
Approval Status	Phase I
Response Type	predicted - sensitive

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

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

KDR Gene Record

KDR 3791 Druggable GenomeClinically Actionable

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name E7080 Novel drug target Established target Specific Action of the Ligand Inhibition

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

Publications: 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.

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Direct Interaction? True Endogenous Drug? False

Publications: 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.

Interaction Types & Directionality: inhibitor (inhibitory)

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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type Advanced Solid Tumor Response Type sensitive Approval Status Preclinical

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Direct Interaction? True Endogenous Drug? False

Publications: 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.

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

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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications: Soria et al., 2014, Phase I/IIa study evaluating the safety, efficacy, pharmacokinetics, and pharmacodynamics of lucitanib in advanced solid tumors., Ann. Oncol.

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Inhibition

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inhibition

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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name BIBF-1120,Vargatef Notes

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

Publications: 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.

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

Interaction Info: Notes Specific Action of the Ligand Inhibition Endogenous Drug? False

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name regorafenib, BAY 73-4506 Novel drug target Established target Endogenous Drug? False

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction In a biochemical homogeneous time-resolved fluorescence (HTRF) kinase assay with an ATP concentration of 1 mM. Specific Action of the Ligand Inhibition Endogenous Drug? False

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor Direct Interaction yes Specific Action of the Ligand Inhibition

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor Direct Interaction yes Specific Action of the Ligand Inhibition

Publications:

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Direct Interaction? False Endogenous Drug? False

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name E7080

Novel drug target Established target

Specific Action of the Ligand Inhibition

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

Publications:

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.

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Direct Interaction? True

Endogenous Drug? False

Publications:

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.

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Pazopanib

Novel drug target Established target

Notes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Direct Interaction? True

Endogenous Drug? False

Publications:

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.

Interaction Types & Directionality:

antibody (inhibitory)

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name IMC-1121B

Novel drug target Established target

Notes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Evidence Type Actionable

Publications:

Soria et al., 2014, Phase I/IIa study evaluating the safety, efficacy, pharmacokinetics, and pharmacodynamics of lucitanib in advanced solid tumors., Ann. Oncol.

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Publications:

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

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.

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name BIBF-1120,Vargatef

Notes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Publications:

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.

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name regorafenib, BAY 73-4506

Novel drug target Established target

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Direct Interaction yes

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a biochemical homogeneous time-resolved fluorescence (HTRF) kinase assay with an ATP concentration of 1 mM.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Direct Interaction? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Trial Name fruquintinib

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Direct Interaction? False

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor inhibitor

Direct Interaction yes

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Vascular endothelial growth factor receptor 2 inhibitor

Direct Interaction yes

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Measured as inhibition of VEGFR-2 autophosphorylation in HUVEC cells.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

3791	Entrez Gene ID
kinase insert domain receptor (a type III receptor tyrosine kinase)	HUGO Gene Name
6307	HUGO Gene ID

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

KDR	DrugBank Gene Name
P35968	UniProt Accession
3791	Entrez Gene Id

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

kinase insert domain receptor	GuideToPharmacology Name
P35968	UniProtKB ID

Vascular endothelial growth factor receptor 2	Gene Name
P35968	UniProt ID