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Compound class: Synthetic organic
Comment: VER-246608 is a potent, selective and ATP-competitive, pan-isoform inhibitor of pyruvate dehydrogenase kinases (PDKs). Analysis of VER-246608 activity suggests that PDK inhibitors may be most effective within the nutrient-depleted tumour microenvironment, and may potentiate the activity of other chemotherapeutic agents.
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.✖
1. Moore JD, Staniszewska A, Shaw T, D'Alessandro J, Davis B, Surgenor A, Baker L, Matassova N, Murray J, Macias A et al.. (2014)
VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells.
Oncotarget, 5 (24): 12862-76. [PMID:25404640]