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Inhibition of PDK in human A-375 cells assessed as reduction in PDH phosphorylation at ser293 residue at 5 to 20 uM after 24 to 48 hrs
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
PDK Inhibition Assay from Article 10.1074/jbc.M113.533885: "Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket."
Assay data:6 Active, 3 Activity ≤ 1 µM, 8 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Inhibition of human PDHK3 co-complexed with porcine PDH using sodium pyruvate, coenzymeA and NAD as substrate preincubated with enzyme complex for 45 mins followed by ATP addition and then later incubated with substrate for 90 mins by absorption spectrophotometric assay
Binding affinity to PDK3 (unknown origin) by isothermal titration calorimetry
Inhibition of recombinant human His-tagged PDK3 expressed in Escherichia coli using PDH E1 as substrate measured after 30 mins by Kinase-Glo luminescence assay
Assay data:4 Active, 1 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of PDHK3 (unknown origin) at 1 uM relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of PDHK in human DU145 cells assessed as reduction in PDHE1a phosphorylation at Ser293 residue incubated for 2 hrs by Western blot analysis
Inhibition of PDHK in human H1299 cells assessed as reduction in PDHE1a phosphorylation at Ser293 residue at 20 uM incubated for 2 hrs by Western blot analysis
Assay data:2 Active, 2 Tested
Inhibition of PDHK in human H1299 cells assessed as reduction in PDHE1a phosphorylation at Ser293 residue incubated for 2 hrs by Western blot analysis
Assay data:2 Tested
Inhibition of PDHK3 (unknown origin) by radiometric biochemical kinase assay
Assay data:16 Active, 16 Activity ≤ 1 µM, 24 Tested
Inhibition of PDK3 (unknown origin) using PDCE1 as substrate incubated for 30 mins by kinase-Glo reagent based luminescence assay
Inhibition of PDK in human NCI-H1975 cells assessed as reduction in PDC phosphorylation at 10 uM measured after 12 hrs under hypoxic condition by Western blot analysis
Inhibition of PDK in human NCI-H1975 cells assessed as reduction in PDC phosphorylation at 2 uM measured after 12 hrs under hypoxic condition by Western blot analysis
Assay data:3 Active, 3 Tested
Inhibition of PDK3 (unknown origin) using PDC E1 as substrate measured after 30 mins by kinase-glo assay
Inhibition of human PDK3 at 100 nM using MBP as substrate by [gamma-33P]-ATP assay
Inhibition of PDK in human NCI-H1975 cells assessed as switch of pyruvate metabolism from lactate production to oxidative phosphorylation by measuring decrease in lactate production at 1 to 10 uM measured after 4 hrs
Inhibition of PDK in human NCI-H1975 cells assessed as switch of pyruvate metabolism from lactate production to oxidative phosphorylation by measuring increase in oxygen consumption rate measured after 2 hrs
Inhibition of PDK in human NCI-H1975 cells assessed as switch of pyruvate metabolism from lactate production to oxidative phosphorylation by measuring increase in ROS production at 1 to 10 uM measured after 4 hrs by DCFH-DA dye based assay
Inhibition of PDK in human NCI-H1975 cells assessed as reduction in phosphorylated S293 PDC E1 level by Western blot analysis
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