| Assay ID | Title | Year | Journal | Article |
|---|
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2014 | Oncotarget, Dec-30, Volume: 5, Issue:24
| VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. |
| AID1604074 | Inhibition of PDHK1 (unknown origin) by radiometric biochemical kinase assay | | | |
| AID1613791 | Inhibition of recombinant human His-tagged PDK2 expressed in Escherichia coli using PDH E1 as substrate measured after 30 mins by Kinase-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | High-throughput screening of novel pyruvate dehydrogenase kinases inhibitors and biological evaluation of their in vitro and in vivo antiproliferative activity. |
| AID1441269 | Displacement of fluorescein-labelled VER160364 from HSP90A (unknown origin) after 90 mins by fluorescence polarization assay | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
| Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase. |
| AID1441274 | Binding affinity to PDHK1 (unknown origin) by surface plasmon resonance method | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
| Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase. |
| AID1613785 | Inhibition of porcine PDK assessed as activation of pyruvate dehydrogenase complex measured after 3 mins | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | High-throughput screening of novel pyruvate dehydrogenase kinases inhibitors and biological evaluation of their in vitro and in vivo antiproliferative activity. |
| AID1441280 | Antiproliferative activity against human PC3 cells after 96 hrs by sulphorhodamine B assay | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
| Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase. |
| AID1604085 | Antiproliferative activity against p53 deficient human DU145 cells incubated for 72 hrs by CellTiter-Glo assay | | | |
| AID1613793 | Inhibition of recombinant human His-tagged PDK4 expressed in Escherichia coli using PDH E1 as substrate measured after 30 mins by Kinase-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | High-throughput screening of novel pyruvate dehydrogenase kinases inhibitors and biological evaluation of their in vitro and in vivo antiproliferative activity. |
| AID1571473 | Inhibition of PDK1 (unknown origin) using PDC E1 as substrate measured after 30 mins by kinase-glo assay | 2018 | MedChemComm, Nov-01, Volume: 9, Issue:11
| Discovery of potent pyruvate dehydrogenase kinase inhibitors and evaluation of their anti-lung cancer activity under hypoxia. |
| AID1441277 | Binding affinity to PDHK1 (unknown origin) by isothermal titration calorimetry | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
| Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase. |
| AID1604075 | Inhibition of PDHK3 (unknown origin) by radiometric biochemical kinase assay | | | |
| AID1441271 | Inhibition of fluorescein-labelled VER160364 binding to PDHK1 (unknown origin) after 90 mins by fluorescence polarization assay | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
| Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase. |
| AID1604083 | Inhibition of HSP90 (unknown origin) | | | |
| AID1441281 | Inhibition of PDHK2 (unknown origin) assessed as decrease in phosphorylation of E1alpha subunit at serine 293 residue after 1 hr by DELFIA | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
| Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase. |
| AID1604084 | Antiproliferative activity against p53 deficient human H1299 cells incubated for 72 hrs by CellTiter-Glo assay | | | |
| AID1441279 | Inhibition of HSP90 in human PC3 cells assessed as compound concentration required to evoke 4-fold increase of HSP70 level after 24 hrs by DELFIA | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
| Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase. |
| AID1613792 | 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 | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | High-throughput screening of novel pyruvate dehydrogenase kinases inhibitors and biological evaluation of their in vitro and in vivo antiproliferative activity. |
| AID1604073 | Inhibition of PDHK4 (unknown origin) by radiometric biochemical kinase assay | | | |
| AID1613790 | Inhibition of recombinant human His-tagged PDK1 expressed in Escherichia coli using PDH E1 as substrate measured after 30 mins by Kinase-Glo luminescence assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | High-throughput screening of novel pyruvate dehydrogenase kinases inhibitors and biological evaluation of their in vitro and in vivo antiproliferative activity. |
| AID1571480 | 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 | 2018 | MedChemComm, Nov-01, Volume: 9, Issue:11
| Discovery of potent pyruvate dehydrogenase kinase inhibitors and evaluation of their anti-lung cancer activity under hypoxia. |
| AID1613833 | Inhibition of porcine PDK assessed as activation of pyruvate dehydrogenase complex at 10 uM measured after 3 mins relative to control | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | High-throughput screening of novel pyruvate dehydrogenase kinases inhibitors and biological evaluation of their in vitro and in vivo antiproliferative activity. |
| AID1613794 | Inhibition of human HSP90 measured after 30 mins by fluorescence polarization assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | High-throughput screening of novel pyruvate dehydrogenase kinases inhibitors and biological evaluation of their in vitro and in vivo antiproliferative activity. |
| AID1441282 | Inhibition of PDHK3 (unknown origin) assessed as decrease in phosphorylation of E1alpha subunit at serine 293 residue after 1 hr by DELFIA | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
| Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase. |
| AID1441283 | Inhibition of PDHK4 (unknown origin) assessed as decrease in phosphorylation of E1alpha subunit at serine 293 residue after 1 hr by DELFIA | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
| Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase. |
| AID1604072 | Inhibition of PDHK2 (unknown origin) by radiometric biochemical kinase assay | | | |
| AID1441278 | Inhibition of PDHK1 in human PC3 cells assessed as decrease in phosphorylation of E1alpha subunit at serine 293 residue after 1 hr by ELISA | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
| Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase. |
| AID1441276 | Inhibition of PDHK1 (unknown origin) assessed as decrease in phosphorylation of E1alpha subunit at serine 293 residue after 1 hr by DELFIA | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
| Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase. |
| AID1571478 | Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell proliferation at 1 to 10 uM after 72 hrs under normoxic condition by MTT assay | 2018 | MedChemComm, Nov-01, Volume: 9, Issue:11
| Discovery of potent pyruvate dehydrogenase kinase inhibitors and evaluation of their anti-lung cancer activity under hypoxia. |
| AID1604096 | 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 | | | |
| AID1613788 | Inhibition of PDK in human NCI-H1975 cells assessed as reduction in PDH phosphorylation at Ser293 residue at 10 uM by ELISA | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | High-throughput screening of novel pyruvate dehydrogenase kinases inhibitors and biological evaluation of their in vitro and in vivo antiproliferative activity. |
| AID1571475 | Inhibition of PDK3 (unknown origin) using PDC E1 as substrate measured after 30 mins by kinase-glo assay | 2018 | MedChemComm, Nov-01, Volume: 9, Issue:11
| Discovery of potent pyruvate dehydrogenase kinase inhibitors and evaluation of their anti-lung cancer activity under hypoxia. |
| AID1571476 | Inhibition of PDK4 (unknown origin) using PDC E1 as substrate measured after 30 mins by kinase-glo assay | 2018 | MedChemComm, Nov-01, Volume: 9, Issue:11
| Discovery of potent pyruvate dehydrogenase kinase inhibitors and evaluation of their anti-lung cancer activity under hypoxia. |
| AID1833816 | Inhibition of human recombinant PDHK1 co-complexed with porcine PDH using sodium pyruvate, coenzymeA and NAD as substrates preincubated with enzyme complex for 45 mins followed by substrates addition and further incubated for 90 mins by spectrophotometric | 2021 | Bioorganic & medicinal chemistry, 12-15, Volume: 52 | Structure-based drug design of novel and highly potent pyruvate dehydrogenase kinase inhibitors. |
| AID1571474 | Inhibition of PDK2 (unknown origin) using PDC E1 as substrate measured after 30 mins by kinase-glo assay | 2018 | MedChemComm, Nov-01, Volume: 9, Issue:11
| Discovery of potent pyruvate dehydrogenase kinase inhibitors and evaluation of their anti-lung cancer activity under hypoxia. |
| AID1571479 | Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell proliferation after 72 hrs under hypoxic condition by MTT assay | 2018 | MedChemComm, Nov-01, Volume: 9, Issue:11
| Discovery of potent pyruvate dehydrogenase kinase inhibitors and evaluation of their anti-lung cancer activity under hypoxia. |
| AID1345758 | Human pyruvate dehydrogenase kinase 4 (PDHK family) | 2014 | Oncotarget, Dec-30, Volume: 5, Issue:24
| VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. |
| AID1345766 | Human pyruvate dehydrogenase kinase 2 (PDHK family) | 2014 | Oncotarget, Dec-30, Volume: 5, Issue:24
| VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. |
| AID1345762 | Human pyruvate dehydrogenase kinase 3 (PDHK family) | 2014 | Oncotarget, Dec-30, Volume: 5, Issue:24
| VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |