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 |
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 |
KINASE |
TYROSINE KINASE |
DRUGGABLE GENOME |
CLINICALLY ACTIONABLE |
inhibitor (inhibitory) |
Notes | |
Trial Name | CT-322 |
Novel drug target | Established target |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
Direct Interaction | yes |
antibody (inhibitory) |
antagonist (inhibitory) |
inhibitor (inhibitory) |
Trial Name | IMC-1121B |
Novel drug target | Established target |
Notes |
inhibitor (inhibitory) |
Indication/Tumor Type | pancreatic cancer |
Response Type | sensitive |
Approval Status | Preclinical |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
Trial Name | fruquintinib |
inhibitor (inhibitory) |
Trial Name | CHIR-265 |
Novel drug target | Established target |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
inhibitor (inhibitory) |
Trial Name | AV-951 |
Novel drug target | Established target |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
Trial Name | motesanib diphosphate, AMG 706 |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
antagonist (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 antagonist |
inhibitor (inhibitory) |
Notes | |
Trial Name | telatinib |
Novel drug target | Established target |
inhibitor (inhibitory) |
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 |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
Direct Interaction | yes |
Direct Interaction? | False |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | True |
inhibitor (inhibitory) |
Notes | |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
inhibitor (inhibitory) |
Notes | |
Direct Interaction? | True |
Endogenous Drug? | False |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
Direct Interaction | yes |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Indication/Tumor Type | Advanced Solid Tumor |
Response Type | sensitive |
Approval Status | Preclinical |
inhibitor (inhibitory) |
Direct Interaction? | True |
Endogenous Drug? | False |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
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 |
inhibitor (inhibitory) |
Novel drug target | Established target |
Trial Name | OSI-930 |
Direct Interaction | yes |
antagonist (inhibitory) |
inhibitor (inhibitory) |
Notes | |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Notes | |
Trial Name | XL647 |
Novel drug target | Established target |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
inhibitor (inhibitory) |
Direct Interaction? | False |
Endogenous Drug? | False |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Notes | |
Direct Interaction? | False |
Endogenous Drug? | False |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | True |
agonist (activating) |
Mechanism of Interaction | Vascular endothelial growth factor receptor 1 and 2 (Flt-1 and KDR) agonist |
Direct Interaction | yes |
inhibitor (inhibitory) |
Trial Name | E7080 |
Novel drug target | Established target |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Novel drug target | Established target |
Trial Name | BIBF-1120,Vargatef |
Notes |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | False |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
Direct Interaction | yes |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
Evidence Type | Actionable |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Direct Interaction? | False |
Endogenous Drug? | False |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Direct Interaction? | True |
Endogenous Drug? | False |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | False |
inhibitor (inhibitory) |
Trial Name | regorafenib, BAY 73-4506 |
Novel drug target | Established target |
Endogenous Drug? | False |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
n/a |
Trial Name | MP0112 |
Novel drug target | Established target |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Trial Name | Pazopanib |
Novel drug target | Established target |
Notes |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
Direct Interaction? | True |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Direct Interaction? | False |
Endogenous Drug? | False |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Direct Interaction? | True |
Endogenous Drug? | False |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Notes | |
Direct Interaction | yes |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
inhibitor (inhibitory) |
Details of the Assay for Interaction | In a radiometric biochemical protein kinase assay. |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
inhibitor (inhibitory) |
Details of the Assay for Interaction | <i>In vitro</i> biochemical assay result |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
n/a |
Trial Name | Vadimezan |
Novel drug target | Established target |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
inhibitor (inhibitory) |
Notes | |
Direct Interaction? | True |
Endogenous Drug? | False |
inhibitor (inhibitory) |
inhibitor (inhibitory) |
Direct Interaction? | False |
Endogenous Drug? | False |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
n/a |
Novel drug target | Established target |
Trial Name | E-10030 |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | False |
inhibitor (inhibitory) |
substrate |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | False |
antagonist (inhibitory) |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Direct Interaction? | False |
Endogenous Drug? | False |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
inhibitor (inhibitory) |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
Direct Interaction | yes |
n/a |
Trial Name | Muparfostat |
Novel drug target | Established target |
inhibitor (inhibitory) |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | True |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | False |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | True |
inhibitor (inhibitory) |
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 |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
inhibitor (inhibitory) |
Details of the Assay for Interaction | In a biochemical enzyme activity assay. |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
inhibitor (inhibitory) |
Direct Interaction? | False |
Endogenous Drug? | False |
Specific Action of the Ligand | Inhibition |
n/a |
Trial Name | ARRY-614 |
Novel drug target | Established target |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | False |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
inhibitor (inhibitory) |
Details of the Assay for Interaction | <i>In vitro</i> inhibition of KDR. |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
inhibitor (inhibitory) |
Direct Interaction? | False |
Endogenous Drug? | False |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor inhibitor |
Direct Interaction | yes |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
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. |
inhibitor (inhibitory) |
Mechanism of Interaction | Vascular endothelial growth factor receptor 2 inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
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 |
KDR | Ensembl Gene Name |
Gene Biotype | PROTEIN_CODING |
ENSG00000128052 | Ensembl Gene Id |
KDR | Gene Symbol |
VGFR2_HUMAN | Uniprot Id |
Target Main Class | Receptors |
Target Subclass | Kinase |
Target Subclass | Other |
3791 | Entrez Gene ID |
CancerCommons Reported Gene Name | VEGF, PDGF |
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 |
Human Readable Name | DRUGGABLE GENOME |
DRUGGABLE GENOME |
KDR | Gene Symbol |
Target Class | Receptors |
Target Subclass | EC:2.7.10.1 |
VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2 | Uniprot Protein Name |
3791 | Entrez Gene Id |
P35968 | Uniprot Accession |
Interpro Name | Serine-threonine/tyrosine-protein kinase catalytic domain |
Interpro Type | Domain |
Human Readable Name | DRUGGABLE GENOME |
KINASE, DRUGGABLE GENOME |
6307 | HUGO Gene ID |
6307 | HUGO Gene Symbol |
kinase insert domain receptor | HUGO Gene Name |
GuideToPharmacology Gene Category Name | Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family |
GuideToPharmacology Gene Category ID | 324 |
3791 | CKB Entrez Id |
KDR | CKB Gene Synonym |
CD309 | CKB Gene Synonym |
PA30086 | PharmGKB ID |
3791 | Entrez Gene ID |
3153 | CIViC Gene ID |
KDR | DrugBank Gene Name |
P35968 | UniProt Accession |
3791 | Entrez Gene Id |
KDR | TTD Gene Abbreviation |
T80975 | TTD Target ID |
VEGFR2 | Gene Symbol |
3791 | Entrez Gene Id |
KDR | MyCancerGenome Gene Symbol |
VEGFR2 | MyCancerGenome Reported Gene Name |
VEGFR-2 | Gene Symbol |
VEGFR | Gene Symbol |
ENSG00000128052 | Gene Symbol |
KDR | Ensembl Id |
DRUGGABLE GENOME |
VEGFR2 | GENE_SYMBOL |
KDR | GENE_SYMBOL |
Vascular endothelial growth factor receptor 2 | UNIPROT |
Vascular endothelial growth factor receptor 2 | Gene Name |
P35968 | UniProt ID |
KINASE |
FLK1 | GO Gene Synonym |
VEGFR2 | GO Gene Synonym |
TYROSINE KINASE |
KDR | Gene Symbol |
CLINICALLY ACTIONABLE |
3791 | Gene ID |
CD309 | dGene Synonym |
FLK1 | dGene Synonym |
KINASE, TYROSINE KINASE |
CLINICALLY ACTIONABLE |
CLINICALLY ACTIONABLE |
CLINICALLY ACTIONABLE |
CLINICALLY ACTIONABLE |