VEGFA   Click here for help

GtoPdb Ligand ID: 5085

Synonyms: vascular endothelial growth factor A | vascular permeability factor (VPF) | VEGF-A
Compound class: Endogenous peptide in human, mouse or rat
Comment: The active peptide is anti-parallel homodimer linked by disulphide bonds. VEGFA exists as four isoforms of 121, 165, 189 and 206 amino acids. The shortest variant contains the full VEGFR2 binding site but lacks domains that are involved in interactions with extracellular-matrix and co-receptors which are present in the longer isoforms [14-15].
A recombinant single-chain derivative of VEGFA121 (scVEGF) can be used experimentally as a fully functional peptide that binds and activates VEGFR2 in the same manner as endogenous VEGFA [1]. scVEGF can be labelled with a single fluorophore at its N-terminal, for use as a molecular probe [3].
Species: Human
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
Natural/Endogenous Targets
Target
fms related receptor tyrosine kinase 1
kinase insert domain receptor
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
kinase insert domain receptor Hs Agonist Agonist 8.0 – 9.6 pKd - 10
⤷ pKd 9.6 (Kd 2.3x10-10 M) [10]
Description: Dissociation constant for scVEGF-binding to dimeric VEGFR2.
pKd 8.0 (Kd 1x10-8 M) [10]
Description: Dissociation constant for scVEGF-binding to monomeric VEGFR2.
fms related receptor tyrosine kinase 1 Ligand is endogenous in the given species Hs None - - - -
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kinase insert domain receptor Ligand is endogenous in the given species Hs None - - - -
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Other ligands which bind to or alter the activity of this ligand
Key to terms and symbols Click column headers to sort
Ligand Sp. Type Action Value Parameter Concentration range (M) Reference
abicipar pegol Peptide Primary target of this compound Hs Inhibitor Inhibition 11.7 pKd - 6
⤷ pKd 11.7 (Kd 2x10-12 M) [6]
vanucizumab Peptide Primary target of this compound Hs Antibody Binding >10.0 pKd - 4
⤷ pKd >10.0 (Kd <1x10-10 M) [4]
ranibizumab Peptide Approved drug Primary target of this compound Hs Antibody Binding 9.8 pKd - 2
⤷ pKd 9.8 (Kd 1.5x10-10 M) [2]
brolucizumab Peptide Approved drug Primary target of this compound Hs Antibody Binding 8.8 pKd - 5
⤷ pKd 8.8 (Kd 1.59x10-9 M) [5]
faricimab Peptide Approved drug Primary target of this compound Hs Antibody Binding 8.5 pKd - 12
⤷ pKd 8.5 (Kd 3x10-9 M) [12]
Description: Binding affinity by ITC, to VEGFA121 and VEGFA165.
bevacizumab Peptide Approved drug Primary target of this compound Hs Antibody Binding 8.0 – 8.3 pIC50 - 2
⤷ pIC50 8.0 – 8.3 (IC50 1x10-8 – 5x10-9 M) [2]
aflibercept Peptide Approved drug Primary target of this compound Hs Fusion protein Inhibition - - - 7-8,13
⤷ [7-8,13]
pegaptanib Small molecule or natural product Approved drug Primary target of this compound Hs Antagonist Inhibition - - - 9,11
⤷ [9,11]
Ligand mentioned in the following text fields
Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family overview