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KDR Gene Record

  • Summary
  • Interactions
  • Claims
  • KDR 3791 Druggable GenomeClinically Actionable

    Alternate Names:

    3791
    KINASE INSERT DOMAIN RECEPTOR
    KDR
    CD309
    FLK1
    VEGFR
    VEGFR2
    191306
    6307
    ENSG00000128052
    OTTHUMG00000128734
    1813
    P35968
    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]
    PROTEIN-TYROSINE KINASE RECEPTOR FLK-1
    VEGFR-2
    FETAL LIVER KINASE 1
    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
    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
    (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
    Coxon et al., 2012, Anti-tumor activity of motesanib in a medullary thyroid cancer model., J. Endocrinol. Invest.
    Maitland ML et al., 2010, Vascular endothelial growth factor pathway., Pharmacogenet Genomics
    Lacouture et al., 2006, Inflammation of actinic keratoses subsequent to therapy with sorafenib, a multitargeted tyrosine-kinase inhibitor., Clin. Exp. Dermatol.
    Schöffski et al., 2006, Emerging role of tyrosine kinase inhibitors in the treatment of advanced renal cell cancer: a review., Ann. Oncol.
    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
    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
    Rini, 2006, Sorafenib., Expert Opin Pharmacother
    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.
    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
    Gong L et al., 2017, PharmGKB summary: sorafenib pathways., Pharmacogenet Genomics
    Veronese et al., 2006, Mechanisms of hypertension associated with BAY 43-9006., J. Clin. Oncol.
    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
    Antonescu et al., 2009, KDR activating mutations in human angiosarcomas are sensitive to specific kinase inhibitors., 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
    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
    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.
    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
    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
    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.
    Silva E et al., 2015, Refractory angiosarcoma of the breast with VEGFR2 upregulation successfully treated with sunitinib., Breast J
    Quek R et al., 2009, Gastrointestinal stromal tumor: a clinical overview., Hematol Oncol Clin North Am
    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
    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.
    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
    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
    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.
    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
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Wragg et al., 2017, Sunitinib Treatment Enhances Metastasis of Innately Drug-Resistant Breast Tumors., Cancer Res.
    Schueneman et al., 2003, SU11248 maintenance therapy prevents tumor regrowth after fractionated irradiation of murine tumor models., 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.
    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.
    Goodkin et al., 1990, Arteriovenous malformation and glioma: coexistent or sequential? Case report., J. Neurosurg.
    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.
    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
    Fury MG et al., 2007, A Phase II study of SU5416 in patients with advanced or recurrent head and neck cancers., Invest New Drugs
    Mita MM et al., 2007, A phase II, pharmacokinetic, and biologic study of semaxanib and thalidomide in patients with metastatic melanoma., Cancer Chemother Pharmacol
    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.
    Wind S et al., 2019, Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib., Clin Pharmacokinet
    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
    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.
    Kurzrock et al., 2011, Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer., J. Clin. Oncol.
    Yakes et al., 2011, Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth., Mol. Cancer Ther.
    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
    Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
  • PEGDINETANIB   KDR

    Interaction Score: 1.89

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD DrugBank TALC GuideToPharmacology

  • PF-00337210   KDR

    Interaction Score: 1.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    23835340


    Sources:
    TTD ChemblInteractions

  • CHEMBL194176   KDR

    Interaction Score: 0.76

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • CHEMBL504805   KDR

    Interaction Score: 0.76

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • CHEMBL272198   KDR

    Interaction Score: 0.76

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • CHEMBL493986   KDR

    Interaction Score: 0.76

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • CHEMBL385178   KDR

    Interaction Score: 0.76

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • CHEMBL491429   KDR

    Interaction Score: 0.76

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • CHEMBL487431   KDR

    Interaction Score: 0.76

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • CHEMBL394826   KDR

    Interaction Score: 0.76

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • RAMUCIRUMAB   KDR

    Interaction Score: 0.63

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

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

    PMIDs:
    20048182 2182794


    Sources:
    JAX-CKB TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • TAS-115   KDR

    Interaction Score: 0.57

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    24140932


    Sources:
    JAX-CKB ChemblInteractions

  • FRUQUINTINIB   KDR

    Interaction Score: 0.5

    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 TTD GuideToPharmacology ChemblInteractions

  • RAF-265   KDR

    Interaction Score: 0.47

    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:
    TdgClinicalTrial TTD DrugBank MyCancerGenome ChemblInteractions

  • TIVOZANIB   KDR

    Interaction Score: 0.44

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ClearityFoundationClinicalTrial TdgClinicalTrial TTD TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • MOTESANIB   KDR

    Interaction Score: 0.43

    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:
    21422803 20124951


    Sources:
    PharmGKB JAX-CKB TdgClinicalTrial TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • GW612286X   KDR

    Interaction Score: 0.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10592235


    Sources:
    DrugBank

  • CHEMBL194911   KDR

    Interaction Score: 0.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • ZD-4190   KDR

    Interaction Score: 0.38

    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: 0.38

    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: 0.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • ALACIZUMAB PEGOL   KDR

    Interaction Score: 0.38

    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: 0.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • ELPAMOTIDE   KDR

    Interaction Score: 0.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • TELATINIB   KDR

    Interaction Score: 0.38

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • GOLVATINIB   KDR

    Interaction Score: 0.38

    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

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology ChemblInteractions

  • RIVOCERANIB   KDR

    Interaction Score: 0.38

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    TTD MyCancerGenome GuideToPharmacology ChemblInteractions

  • AXITINIB   KDR

    Interaction Score: 0.32

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    20124951 18541897


    Sources:
    CancerCommons MyCancerGenomeClinicalTrial PharmGKB TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • BMS-690514   KDR

    Interaction Score: 0.27

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    TTD TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • VATALANIB   KDR

    Interaction Score: 0.26

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    17584317


    Sources:
    DTC TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • HENATINIB   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
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology ChemblInteractions

  • SUNITINIB   KDR

    Interaction Score: 0.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

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


    Sources:
    MyCancerGenomeClinicalTrial TEND DTC PharmGKB JAX-CKB TdgClinicalTrial CIViC TTD DrugBank TALC MyCancerGenome GuideToPharmacology

  • BRIVANIB   KDR

    Interaction Score: 0.24

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    20124951


    Sources:
    PharmGKB TTD TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • SURUFATINIB   KDR

    Interaction Score: 0.23

    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

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology ChemblInteractions

  • OSI-930   KDR

    Interaction Score: 0.22

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name OSI-930
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions

  • CABOZANTINIB   KDR

    Interaction Score: 0.21

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

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

    PMIDs:
    21606412 21926191


    Sources:
    ClearityFoundationClinicalTrial TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology

  • BMS-794833   KDR

    Interaction Score: 0.19

    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

  • BMS-817378   KDR

    Interaction Score: 0.19

    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

  • TESEVATINIB   KDR

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes
    Trial Name XL647
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TALC MyCancerGenome GuideToPharmacology

  • CABOZANTINIB S-MALATE   KDR

    Interaction Score: 0.19

    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

  • PRALSETINIB   KDR

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • GLESATINIB   KDR

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TALC MyCancerGenome GuideToPharmacology

  • FORETINIB   KDR

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • TELBERMIN   KDR

    Interaction Score: 0.19

    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

  • LENVATINIB   KDR

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    17943726


    Sources:
    TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology

  • NINTEDANIB   KDR

    Interaction Score: 0.17

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    18559524 31016670 19522465


    Sources:
    ClearityFoundationClinicalTrial DTC TdgClinicalTrial DrugBank TALC MyCancerGenome GuideToPharmacology

  • AEE-788   KDR

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    MyCancerGenome GuideToPharmacology ChemblInteractions

  • FAMITINIB   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
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology ChemblInteractions

  • LUCITANIB   KDR

    Interaction Score: 0.16

    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:
    MyCancerGenomeClinicalTrial JAX-CKB GuideToPharmacology ChemblInteractions

  • X-82   KDR

    Interaction Score: 0.15

    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: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17884497


    Sources:
    DTC

  • SEMAXANIB   KDR

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    16449240 16983506 16736151


    Sources:
    DrugBank GuideToPharmacology ChemblInteractions

  • ORANTINIB   KDR

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • TAK-593   KDR

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    TTD ChemblInteractions

  • ALTIRATINIB   KDR

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology ChemblInteractions

  • REGORAFENIB   KDR

    Interaction Score: 0.14

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    27004155


    Sources:
    MyCancerGenomeClinicalTrial JAX-CKB TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • EUPATORIN   KDR

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • KRN-633   KDR

    Interaction Score: 0.13

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • IMC-1C11   KDR

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • L-21649   KDR

    Interaction Score: 0.13

    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: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name MP0112
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • AG-13958   KDR

    Interaction Score: 0.13

    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: 0.13

    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: 0.13

    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: 0.13

    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: 0.12

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

    Interaction Info:
    Notes
    Evidence Type Actionable
    Approval Status Preclinical

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


    Sources:
    ClearityFoundationClinicalTrial MyCancerGenomeClinicalTrial TEND DTC PharmGKB JAX-CKB TdgClinicalTrial CIViC TTD DrugBank TALC MyCancerGenome GuideToPharmacology

  • PAZOPANIB   KDR

    Interaction Score: 0.12

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    26063633 27160228 17288876 25411163 24036042


    Sources:
    MyCancerGenomeClinicalTrial DTC PharmGKB TdgClinicalTrial CIViC DrugBank TALC MyCancerGenome GuideToPharmacology

  • CHIAURANIB   KDR

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • SU-014813   KDR

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology ChemblInteractions

  • 4SC-203   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

  • CM-082   KDR

    Interaction Score: 0.09

    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: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL1908396   KDR

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • VANDETANIB   KDR

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    26578684 20124951


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

  • 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:
    TdgClinicalTrial TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • TAFETINIB   KDR

    Interaction Score: 0.08

    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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • LY-2874455   KDR

    Interaction Score: 0.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • VADIMEZAN   KDR

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name Vadimezan
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • ANLOTINIB   KDR

    Interaction Score: 0.08

    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

  • CEDIRANIB   KDR

    Interaction Score: 0.07

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    15899831


    Sources:
    ClearityFoundationClinicalTrial TdgClinicalTrial TTD DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • ITRACONAZOLE   KDR

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21936514


    Sources:
    DTC

  • RIPRETINIB   KDR

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • CEP-11981   KDR

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology ChemblInteractions

  • MGCD-265   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

  • XL-820   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

  • PEGPLERANIB SODIUM   KDR

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Novel drug target Established target
    Trial Name E-10030

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • BX-795   KDR

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • ERDAFITINIB   KDR

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)
    substrate

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

    PMIDs:
    None found


    Sources:
    DrugBank GuideToPharmacology

  • 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:
    DrugBank MyCancerGenome ChemblInteractions

  • BRIVANIB ALANINATE   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

  • MK-2461   KDR

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology

  • ROMIPLOSTIM   KDR

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • CP-459632   KDR

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RABEPRAZOLE SODIUM   KDR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD MyCancerGenome

  • BARASERTIB   KDR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • NINTEDANIB ESYLATE   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

  • SUNITINIB MALATE   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

  • TG100-801   KDR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    DrugBank ChemblInteractions

  • MUPARFOSTAT   KDR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name Muparfostat
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • PONATINIB   KDR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    19878872


    Sources:
    DrugBank MyCancerGenome

  • PLX-4720   KDR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • LINIFANIB   KDR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    DTC TdgClinicalTrial DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • OSI-632   KDR

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    DTC TTD GuideToPharmacology ChemblInteractions

  • DORSOMORPHIN   KDR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Assayed using AMPK heterotrimeric complex containing &alpha;2, &beta;1, &gamma;1 subunits
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • NERATINIB   KDR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • PUQUITINIB   KDR

    Interaction Score: 0.03

    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: 0.03

    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: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • SITRAVATINIB   KDR

    Interaction Score: 0.03

    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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • PEXIDARTINIB   KDR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • PEXMETINIB   KDR

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name ARRY-614
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • DOVITINIB   KDR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ClearityFoundationClinicalTrial DTC TdgClinicalTrial TALC GuideToPharmacology ChemblInteractions

  • SORAFENIB TOSYLATE   KDR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CHEMBL202721   KDR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • AST-487   KDR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    DTC GuideToPharmacology

  • AZD-1152-HQPA   KDR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DORAMAPIMOD   KDR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • INFIGRATINIB   KDR

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • TAK-715   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

  • ENMD-981693   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:
    ChemblInteractions

  • MLN-8054   KDR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL406845   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
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    DTC GuideToPharmacology ChemblInteractions

  • SB-220025   KDR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL546797   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
    Details of the Assay for Interaction Measuring inhibition of kinase activity in a biochemical assay.

    PMIDs:
    None found


    Sources:
    DTC GuideToPharmacology ChemblInteractions

  • 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

  • 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

  • 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

  • PD-0166285   KDR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • JNJ-7706621   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

  • SOTRASTAURIN   KDR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CENISERTIB   KDR

    Interaction Score: 0.01

    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

    PMIDs:
    None found


    Sources:
    DTC GuideToPharmacology

  • 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: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • R-406   KDR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SP-600125   KDR

    Interaction Score: 0.0

    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

  • FOSTAMATINIB   KDR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    26516587


    Sources:
    DrugBank

  • 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:

  • GuideToPharmacology: 3791

    • Version: 29-September-2020

    Alternate Names:
    6307 HUGO Gene ID
    6307 HUGO Gene Symbol
    kinase insert domain receptor HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family
    GuideToPharmacology Gene Category ID 324

    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

  • DrugBank: BE0000369

    • Version: 5.1.7

    Alternate Names:
    KDR DrugBank Gene Name
    P35968 UniProt Accession
    3791 Entrez Gene Id

    Gene Info:

    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.
    Goodkin et al., 1990, Arteriovenous malformation and glioma: coexistent or sequential? Case report., J. Neurosurg.
    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

  • 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:

  • 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:

    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:

  • 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:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21