| Assay ID | Title | Year | Journal | Article |
|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1304757 | Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID1304790 | Activation of pig heart PDC assessed as production of NADH at 10 mM in presence of ATP | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID1304794 | Inhibition of PDK1 in human MCF7 cells assessed as increase in oxygen consumption rate at 10 mM after 12 hrs | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID1514949 | Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Discovery of novel pyruvate dehydrogenase kinases inhibitors by screening of an in-house small molecule library for anti-lung cancer therapeutics. |
| AID1558190 | Induction of apoptosis in human MCF7 cells assessed as late apoptotic cells at 30 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 2.97 %) | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID511324 | Anticancer activity against human A549 cells after 72 hrs by MTT assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| Novel N-phenyl dichloroacetamide derivatives as anticancer reagents: design, synthesis and biological evaluation. |
| AID1304756 | Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID1558170 | Induction of ROS generation in human MCF7 cells assessed as ROS level at 30 uM after 24 hrs by DCFDA-fluorescence based flow cytometry (Rvb = 6.57 %) | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1304765 | Induction of apoptosis in human MCF7 assessed as late apoptotic cells at 10 mM after 10 hrs by FITC-annexin V/propidium iodide staining-based flow cytometric analysis (Rvb = 1.95%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID174038 | In vivo percent of control lactate in 24 hr fasted rats at 1 mM/kg oral dose | 2000 | Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
| Anilides of (R)-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase. |
| AID1558166 | Induction of mitochondrial dysfunction in human MCF7 cells assessed as cell population with mitochondrial membrane potential collapse at 30 uM after 24 hrs by JC1 staining-based FACScalibur flow cytometry analysis (Rvb = 2.74 %) | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1304809 | Reversal of hyperpolarized mitochondrial membrane potential in human MCF7 cells assessed as cells with vital and intact mitochondrial membranes at 20 uM after 12 hrs by JC1 staining-based flow cytometric analysis | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID1731459 | Antiproliferative activity against human PC3 cells assessed as growth inhibition after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer activity. |
| AID1558191 | Induction of apoptosis in human MCF7 cells assessed as necrotic cells at 30 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.10 %) | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1304764 | Induction of apoptosis in human MCF7 assessed as early apoptotic cells at 10 mM after 10 hrs by FITC-annexin V/propidium iodide staining-based flow cytometric analysis (Rvb = 2.38%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID1731461 | Inhibition of PDK (unknown origin) using RYHGHSMSDP as substrate after 30 mins by Kinase-Glo luminescent assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer activity. |
| AID1544832 | Anti-hypersensitive activity in MCT-induced pulmonary arterial hypertension Sprague-Dawley rat model assessed as mean pulmonary artery pressure at 15.5 mg/kg, po administered daily for 14 days starting from 14 days post-MCT challenge and measured post-las | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID1514944 | Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability at 20 mM after 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Discovery of novel pyruvate dehydrogenase kinases inhibitors by screening of an in-house small molecule library for anti-lung cancer therapeutics. |
| AID1558203 | Anticancer activity against mouse 4T1 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1558235 | Toxicity in BALB/c nude mouse xenografted with human MCF7 cells assessed as effect on body weight at 30 mg/kg, iv administered every 2 days for 2 weeks measured after 14 days | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1558183 | Inhibition of glycolysis in mouse 4T1 cells expressing PDK assessed as reduction in intracellular lactate level at 30 uM after 6 hrs by microplate reader assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1304781 | Binding affinity to recombinant N-terminal 6xHis-SUMO-tagged human PDK1 (29 to 436 residues) expressed in Escherichia coli BL-21 by isothermal titration calorimetric method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID1544819 | Inhibition of ROCK2 in rat PASMC assessed as inhibition of PGDF-BB-induced IL6 up regulation at 50 nM measured after 72 hrs by ELISA | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID1558189 | Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells at 30 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 3.53 %) | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1558157 | Inhibition of PDK1 (unknown origin) expressed in human MCF7 cells using PDK tide as substrate measured after 90 mins in presence of ATP by ADP-Glo luminescent kinase assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID162831 | Inhibitory activity against Pyruvate dehydrogenase kinase | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
| (R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionamides are orally active inhibitors of pyruvate dehydrogenase kinase. |
| AID1731460 | Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer activity. |
| AID1514948 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Discovery of novel pyruvate dehydrogenase kinases inhibitors by screening of an in-house small molecule library for anti-lung cancer therapeutics. |
| AID1544833 | Anti-hypersensitive activity in MCT-induced pulmonary arterial hypertension Sprague-Dawley rat model assessed as right ventricular systolic pressure at 15.5 mg/kg, po administered daily for 14 days starting from 14 days post-MCT challenge and measured pos | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID1558229 | Antitumor activity against human MCF7 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 30 mg/kg, iv administered every two days for two weeks measured after 14 days | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1544820 | Inhibition of ROCK2 in rat PAEC assessed as inhibition of PGDF-BB-induced TNFalpha up regulation at 50 nM measured after 72 hrs by ELISA | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID1544824 | Inhibition of ROCK2 in rat PAEC assessed as inhibition of hypoxia-induced TNFalpha up regulation at 50 nM measured after 72 hrs by ELISA | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID714358 | Cytotoxicity against human H460 cells after 68 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Design, synthesis and biological evaluation of N-arylphenyl-2,2-dichloroacetamide analogues as anti-cancer agents. |
| AID1558205 | Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1304767 | Induction of apoptosis in human MCF7 assessed as viable cells at 10 mM after 10 hrs by FITC-annexin V/propidium iodide staining-based flow cytometric analysis (Rvb = 93.8%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID1558160 | Downregulation of PDK expression in human MCF7 cells at 2.5 to 10 uM after 48 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1544822 | Inhibition of ROCK2 in rat PASMC assessed as inhibition of hypoxia-induced TNFalpha up regulation at 50 nM measured after 72 hrs by ELISA | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID1558164 | Anticancer activity against human HCT116 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1304759 | Cytotoxicity against human MCF10A cells assessed as growth inhibition at 20 uM after 72 hrs by MTT assay relative to control | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID1558204 | Cytotoxicity against human HBMEC cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID714357 | Cytotoxicity against human A549 cells after 68 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Design, synthesis and biological evaluation of N-arylphenyl-2,2-dichloroacetamide analogues as anti-cancer agents. |
| AID1558180 | Inhibition of glycolysis in human MCF7 cells assessed as reduction in intracellular lactate level at 30 uM after 6 hrs by microplate reader assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1304810 | Reversal of hyperpolarized mitochondrial membrane potential in human MCF7 cells assessed as cells with vital and intact mitochondrial membranes at 10 mM after 12 hrs by JC1 staining-based flow cytometric analysis | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID173642 | In vivo %control of lactate in normal Sprague-Dawley rats after 2 hr at a dose of 1 umol/Kg | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
| Secondary amides of (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase. |
| AID1731456 | Antiproliferative activity against human SHSY-5Y cells assessed as growth inhibition after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer activity. |
| AID1544895 | Anti-hypersensitive activity in MCT-induced pulmonary arterial hypertension Sprague-Dawley rat model assessed as reduction in cardiomyocyte hypertrophy by measuring cardiac fibrosis at 15.5 mg/kg, po administered daily for 14 days starting from 14 days po | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID1304798 | Inhibition of PDK1 in human MCF7 cells assessed as decrease in proton production rate at 10 mM after 12 hrs | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID1558264 | Induction of metabolic reversal from aerobic glycolysis to oxidative phosphorylation in human MCF7 cells assessed as increase in extracellular acidification rate at 30 uM pretreated for 4 hrs followed by glucose addition after 25 mins by seahorse XF24 ext | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1558266 | Induction of metabolic reversal from aerobic glycolysis to oxidative phosphorylation in human MCF7 cells assessed as decline in extracellular acidification rate at 30 uM pretreated for 4 hrs followed by glucose addition after 25 mins followed by subsequen | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID714359 | Cytotoxicity against human KB-3-1 cells after 68 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Design, synthesis and biological evaluation of N-arylphenyl-2,2-dichloroacetamide analogues as anti-cancer agents. |
| AID1558154 | Anticancer activity against human MCF7 cells overexpressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1558270 | Induction of metabolic reversal from aerobic glycolysis to oxidative phosphorylation in human MCF7 cells assessed as decrease in oxygen consumption rate at 30 uM pretreated for 6 hrs followed by oligomycin A addition after 25 mins followed by subsequent a | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1558181 | Inhibition of glycolysis in human MCF7 cells assessed as reduction in extracellular lactate level at 30 uM after 6 hrs by microplate reader assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1731457 | Antiproliferative activity against human HCT-116 cells assessed as growth inhibition after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer activity. |
| AID1558165 | Induction of mitochondrial dysfunction in human MCF7 cells assessed as cell population with intact mitochondrial membrane potential at 30 uM after 24 hrs by JC1 staining-based FACScalibur flow cytometry analysis (Rvb = 97%) | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1558232 | Toxicity in BALB/c nude mouse xenografted with human MCF7 cells assessed as mouse death at 30 mg/kg, iv administered every 2 days for 2 weeks measured after 14 days | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1558265 | Induction of metabolic reversal from aerobic glycolysis to oxidative phosphorylation in human MCF7 cells assessed as increase in extracellular acidification rate at 30 uM pretreated for 4 hrs followed by glucose addition after 25 mins followed by subseque | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1304806 | Inhibition of PDK1 in human MCF7 cells assessed as decrease in lactate production at 10 mM after 12 hrs | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID1304800 | Inhibition of PDK1 in human MCF7 cells assessed as increase in ratio of oxygen consumption rate to extracellular acidification rate at 10 mM after 12 hrs | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID1304761 | Cytotoxicity against human MCF10A cells assessed as growth inhibition at 10 mM after 72 hrs by MTT assay relative to control | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID1544894 | Anti-hypersensitive activity in MCT-induced pulmonary arterial hypertension Sprague-Dawley rat model assessed as reduction in cardiomyocyte hypertrophy by measuring cross-sectional area of cardiomyocyte at 15.5 mg/kg, po administered daily for 14 days sta | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID1558182 | Inhibition of glycolysis in mouse 4T1 cells expressing PDK assessed as reduction in extracellular lactate level at 30 uM after 6 hrs by microplate reader assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID162830 | In vivo inhibion of pyruvate dehydrogenase kinase, increased oxidation of lactate | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
| (R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionamides are orally active inhibitors of pyruvate dehydrogenase kinase. |
| AID1558202 | Anticancer activity against human A375 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1650770 | Cytotoxicity against human HCT116 cells assessed as inhibition of cell growth | 2020 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 30, Issue:3
| Novel hybrid molecules of 3,5-bis(benzylidene)-4-piperidones and dichloroacetic acid which demonstrate potent tumour-selective cytotoxicity. |
| AID1544842 | Anti-hypersensitive activity in MCT-induced pulmonary arterial hypertension Sprague-Dawley rat model assessed as pulmonary artery medial thickness at 15.5 mg/kg, po administered daily for 14 days starting from 14 days post-MCT challenge and measured post- | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID1544821 | Inhibition of ROCK2 in rat PAEC assessed as inhibition of PGDF-BB-induced IL6 up regulation at 50 nM measured after 72 hrs by ELISA | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID1514934 | Inhibition of PDK1 (unknown origin) at 10 mM using PDH E1 as substrate measured after 30 mins by kinase-glo assay relative to control | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Discovery of novel pyruvate dehydrogenase kinases inhibitors by screening of an in-house small molecule library for anti-lung cancer therapeutics. |
| AID1304766 | Induction of apoptosis in human MCF7 assessed as necrotic cells at 10 mM after 10 hrs by FITC-annexin V/propidium iodide staining-based flow cytometric analysis (Rvb = 1.86%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID1731455 | Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer activity. |
| AID1323835 | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Identification of small molecules that bind to the mitochondrial protein mitoNEET. |
| AID162971 | Inhibition of porcine pyruvate dehydrogenase kinase (PDHK)in a primary enzymatic assay | 2000 | Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
| Anilides of (R)-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase. |
| AID1514935 | Inhibition of PDK1 (unknown origin) using PDH E1 as substrate measured after 30 mins by kinase-glo assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Discovery of novel pyruvate dehydrogenase kinases inhibitors by screening of an in-house small molecule library for anti-lung cancer therapeutics. |
| AID1304796 | Inhibition of PDK1 in human MCF7 cells assessed as decrease in extracellular acidification rate at 10 mM after 12 hrs | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation. |
| AID162959 | In vivo inhibition of pyruvate dehydrogenase kinase, reduced lactate level in normal 24 hr r fasted rats at 1 mmol/kg oral dose | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
| (R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionamides are orally active inhibitors of pyruvate dehydrogenase kinase. |
| AID1544825 | Inhibition of ROCK2 in rat PAEC assessed as inhibition of hypoxia-induced IL6 up regulation at 50 nM measured after 72 hrs by ELISA | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID1514937 | Binding affinity to SUMO-fused/His-tagged PDK1 (unknown origin) expressed in Escherichia coli by isothermal calorimetric titration analysis | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Discovery of novel pyruvate dehydrogenase kinases inhibitors by screening of an in-house small molecule library for anti-lung cancer therapeutics. |
| AID511323 | Anticancer activity against human KB cells after 72 hrs by MTT assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| Novel N-phenyl dichloroacetamide derivatives as anticancer reagents: design, synthesis and biological evaluation. |
| AID155206 | Inhibitory activity tested against Pyruvate Dehydrogenase Kinase (PDHK) receptor from rats. | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
| Secondary amides of (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase. |
| AID1650769 | Cytotoxicity against human CRL1790 cells assessed as inhibition of cell growth | 2020 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 30, Issue:3
| Novel hybrid molecules of 3,5-bis(benzylidene)-4-piperidones and dichloroacetic acid which demonstrate potent tumour-selective cytotoxicity. |
| AID89059 | Effective concentration required to increase the oxidation of lactate in cellular assay using Human Skin Fibroblasts | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
| Secondary amides of (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase. |
| AID1558201 | Cytotoxicity against human MCF7 cells assessed as cell death at 30 uM pretreated with Z-VAD-fmk followed by compound addition by MTT assay | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID1544823 | Inhibition of ROCK2 in rat PASMC assessed as inhibition of hypoxia-induced IL6 up regulation at 50 nM measured after 72 hrs by ELISA | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID1544889 | Hemodynamic activity in Sprague-Dawley rat assessed as effect on mean systemic arterial pressure at 15.5 mg/kg, po administered daily for 2 weeks by pressure transducer-coupled polygraphy | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID1323834 | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Identification of small molecules that bind to the mitochondrial protein mitoNEET. |
| AID511325 | Anticancer activity against human Bel7402 cells after 72 hrs by MTT assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| Novel N-phenyl dichloroacetamide derivatives as anticancer reagents: design, synthesis and biological evaluation. |
| AID1731458 | Antiproliferative activity against human A375 cells assessed as growth inhibition after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer activity. |
| AID1544818 | Inhibition of ROCK2 in rat PASMC assessed as inhibition of PGDF-BB-induced TNFalpha up regulation at 50 nM measured after 72 hrs by ELISA | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID1558188 | Induction of apoptosis in human MCF7 cells assessed as viable cells at 30 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 93.39 %) | 2019 | Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
| Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy. |
| AID511322 | Anticancer activity against human BGC823 cells after 72 hrs by MTT assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| Novel N-phenyl dichloroacetamide derivatives as anticancer reagents: design, synthesis and biological evaluation. |
| AID1544843 | Anti-hypersensitive activity in MCT-induced pulmonary arterial hypertension Sprague-Dawley rat model assessed as lung fibrosis at 15.5 mg/kg, po administered daily for 14 days starting from 14 days post-MCT challenge and measured post-last dose by Masson' | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID1650768 | Selectivity index, ratio of IC50 for human CRL1790 cells assessed as inhibition of cell growth to IC50 for human HCT116 cells assessed as inhibition of cell growth | 2020 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 30, Issue:3
| Novel hybrid molecules of 3,5-bis(benzylidene)-4-piperidones and dichloroacetic acid which demonstrate potent tumour-selective cytotoxicity. |
| AID1544834 | Anti-hypersensitive activity in MCT-induced pulmonary arterial hypertension Sprague-Dawley rat model assessed as right ventricular hypertrophy index at 15.5 mg/kg, po administered daily for 14 days starting from 14 days post-MCT challenge and measured pos | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats. |
| AID91138 | Effective concentration in human fibroblasts for increased oxidation of lactate | 2000 | Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
| Anilides of (R)-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase. |
| AID1731454 | Antiproliferative activity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer activity. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |