Adam Yasgar

发表

The NCGC Pharmaceutical Collection: A Comprehensive Resource of Clinically Approved Drugs Enabling Repurposing and Chemical Genomics

Ruili Huang, Noel Southall, Yuhong Wang, 2011, Science Translational Medicine.

Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries.

Adam Yasgar, A. Jadhav, C. Austin, 2006, Proceedings of the National Academy of Sciences of the United States of America.

Current approaches for the discovery of drugs that deter substance and drug abuse

Adam Yasgar, A. Simeonov, 2014, Expert opinion on drug discovery.

Electrical alternans and hemodynamics in the anesthetized guinea pig can discriminate the cardiac safety of antidepressants.

Adam Yasgar, K. Crimin, T. Wisialowski, 2007, Journal of pharmacological and toxicological methods.

Thiol-Containing Fluorescent Probe High-Throughput Identification of Promiscuous Inhibitors from Screening Libraries with the Use of a

Adam Yasgar, A. Jadhav, A. Simeonov, 2013 .

Quantitative High-Throughput Screening Using a Live-Cell cAMP Assay Identifies Small-Molecule Agonists of the TSH Receptor

Noel Southall, Adam Yasgar, P. Shinn, 2008, Journal of biomolecular screening.

Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space

Jared T. Shaw, Derek S. Tan, D. E. Olson, 2018, ACS central science.

Parallel Chemistry Approach to Identify Novel Nuclear Receptor Ligands Based on the GW0742 Scaffold.

Adam Yasgar, A. Jadhav, A. Simeonov, 2017, ACS combinatorial science.

High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell–like diffuse large B-cell lymphoma cells

Sam Michael, Christopher P Austin, Paul Shinn, 2014, Proceedings of the National Academy of Sciences.

A fluorescence-based high throughput assay for the determination of small molecule−human serum albumin protein binding

Adam Yasgar, A. Jadhav, A. Simeonov, 2014, Analytical and Bioanalytical Chemistry.

High-Throughput 1,536-Well Fluorescence Polarization Assays for α1-Acid Glycoprotein and Human Serum Albumin Binding

Adam Yasgar, A. Jadhav, A. Simeonov, 2012, PloS one.

Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors

A. Zakharov, Adam Yasgar, A. Jadhav, 2020, Proceedings of the National Academy of Sciences.

A strategy to discover inhibitors of Bacillus subtilis surfactin-type phosphopantetheinyl transferase.

Timothy L. Foley, Adam Yasgar, A. Jadhav, 2010, Molecular bioSystems.

Quantitative bioactivity signatures of dietary supplements and natural products

Deborah K. Ngan, A. Zakharov, Ruili Huang, 2022, bioRxiv.

Discovery of ML355, a Potent and Selective Inhibitor of Human 12-Lipoxygenase

Adam Yasgar, A. Jadhav, A. Simeonov, 2014 .

Corrigendum: A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate.

D. Sabatini, N. Gray, K. Westover, 2016, Nature chemical biology.

Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity

Adam Yasgar, A. Jadhav, V. Vasiliou, 2018, Journal of medicinal chemistry.

Preparation of FRET reporters to support chemical probe development.

Timothy L. Foley, Adam Yasgar, A. Jadhav, 2010, Organic & biomolecular chemistry.

4-(3-Chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-methoxypyridin-2-yl)piperazine-1-carbothioamide (ML267), a Potent Inhibitor of Bacterial Phosphopantetheinyl Transferase That Attenuates Secondary Metabolism and Thwarts Bacterial Growth

Timothy L. Foley, Adam Yasgar, A. Jadhav, 2014, Journal of medicinal chemistry.

Potent and Selective Inhibitors of Human Reticulocyte 12/15-Lipoxygenase as Anti-Stroke Therapies

Adam Yasgar, A. Jadhav, E. Lo, 2014, Journal of medicinal chemistry.

Testing for drug-human serum albumin binding using fluorescent probes and other methods

Adam Yasgar, A. Simeonov, Bolormaa Baljinnyam, 2018, Expert opinion on drug discovery.

A PHGDH inhibitor reveals coordination of serine synthesis and 1-carbon unit fate

D. Sabatini, N. Gray, K. Westover, 2016, Nature chemical biology.

Optimization of High-Throughput Methyltransferase Assays for the Discovery of Small Molecule Inhibitors.

A. Zakharov, Adam Yasgar, A. Jadhav, 2020, ACS Combinatorial Science.

Venglustat Inhibits Protein N-Terminal Methyltransferase 1 in a Substrate-Competitive Manner.

A. Zakharov, Adam Yasgar, A. Simeonov, 2022, Journal of medicinal chemistry.

Small Molecule Inhibitors of Activation-Induced Deaminase Decrease Class Switch Recombination in B Cells.

A. Zakharov, Adam Yasgar, A. Simeonov, 2021, ACS pharmacology & translational science.

Cross-Platform Bayesian Optimization System for Autonomous Biological Assay Development

Jayme L. Dahlin, A. Zakharov, Adam Yasgar, 2021, bioRxiv.

Fluorescent protein-based cellular assays analyzed by laser-scanning microplate cytometry in 1536-well plate format.

Christopher P Austin, Anton Simeonov, Wei Zheng, 2006, Methods in enzymology.

Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors

D. Sabatini, Adam Yasgar, M. Hall, 2018, bioRxiv.

A High-Content Assay Enables the Automated Screening and Identification of Small Molecules with Specific ALDH1A1-Inhibitory Activity

Adam Yasgar, A. Jadhav, V. Vasiliou, 2017, PloS one.

THE IMPACT OF P-GLYCOPROTEIN ON THE DISPOSITION OF DRUGS TARGETED FOR INDICATIONS OF THE CENTRAL NERVOUS SYSTEM: EVALUATION USING THE MDR1A/1B KNOCKOUT MOUSE MODEL

Xi Chen, Karthik Venkatakrishnan, Matthew Troutman, 2005, Drug Metabolism and Disposition.

A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.

A. Zakharov, Adam Yasgar, A. Jadhav, 2021, Cell reports.

Discovery and Structure-Activity Relationship Study of (Z)-5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors.

N. Gray, S. Ficarro, Tinghu Zhang, 2020, Journal of medicinal chemistry.

The Tox21 10K Compound Library: Collaborative Chemistry Advancing Toxicology

Antony J. Williams, Ryan R. Lougee, R. Judson, 2020, Chemical research in toxicology.

Fluorescence polarization assays in high-throughput screening and drug discovery: a review

Ajit Jadhav, Tyler Peryea, Adam Yasgar, 2016, Methods and applications in fluorescence.

Disrupting malaria parasite AMA1 – RON2 interaction with a small molecule prevents erythrocyte invasion

Anton Simeonov, Xin Hu, Ajit Jadhav, 2013, Nature Communications.

AlphaScreen-Based Assays: Ultra-High-Throughput Screening for Small-Molecule Inhibitors of Challenging Enzymes and Protein-Protein Interactions.

Anton Simeonov, Ajit Jadhav, Adam Yasgar, 2016, Methods in molecular biology.

Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1).

M. Ferrer, Adam Yasgar, A. Jadhav, 2015, Journal of medicinal chemistry.

Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase.

Adam Yasgar, A. Jadhav, A. Simeonov, 2014, Journal of medicinal chemistry.

Selective small molecule inhibitor of the Mycobacterium tuberculosis fumarate hydratase reveals an allosteric regulatory site

Adam Yasgar, Chris Abell, Gerhard Fischer, 2016, Proceedings of the National Academy of Sciences.

Applications of Differential Scanning Fluorometry and Related Technologies in Characterization of Protein-Ligand Interactions.

Adam Yasgar, A. Simeonov, Bolormaa Baljinnyam, 2020, Methods in molecular biology.

Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors.

N. Gray, S. Ficarro, Tinghu Zhang, 2020, ACS medicinal chemistry letters.

Compound Management for Quantitative High-Throughput Screening

Sam Michael, Christopher P Austin, Paul Shinn, 2008, JALA.

Discovery of ML351, a Potent and Selective Inhibitor of Human 15-Lipoxygenase-1

Adam Yasgar, A. Jadhav, A. Simeonov, 2014 .

A High-Throughput Screen Identifies 2,9-Diazaspiro[5.5]Undecanes as Inducers of the Endoplasmic Reticulum Stress Response with Cytotoxic Activity in 3D Glioma Cell Models

G. Riggins, Adam Yasgar, A. Jadhav, 2016, PloS one.

A high-throughput 1,536-well luminescence assay for glutathione S-transferase activity.

Adam Yasgar, A. Simeonov, James Inglese, 2010, Assay and drug development technologies.

Correction: A High-Content Assay Enables the Automated Screening and Identification of Small Molecules with Specific ALDH1A1-Inhibitory Activity

Adam Yasgar, A. Jadhav, V. Vasiliou, 2018, PloS one.

A platform of assays for the discovery of anti-Zika small-molecules with activity in a 3D-bioprinted outer-blood-retina model

Min Jae Song, M. Ferrer, A. Zakharov, 2022, PloS one.

SCAM Detective: Accurate Predictor of Small, Colloidally Aggregating Molecules

Alexey V Zakharov, Adam Yasgar, Alexander Tropsha, 2020, J. Chem. Inf. Model..

Peroxisome proliferation-activated receptor δ agonist GW0742 interacts weakly with multiple nuclear receptors, including the vitamin D receptor.

Adam Yasgar, A. Jadhav, A. Simeonov, 2013, Biochemistry.

Dual-fluorophore quantitative high-throughput screen for inhibitors of BRCT-phosphoprotein interaction.

Sam Michael, Christopher P Austin, Anton Simeonov, 2008, Analytical biochemistry.

High-Throughput Identification of Promiscuous Inhibitors from Screening Libraries with the Use of a Thiol-Containing Fluorescent Probe

C. Eyermann, Adam Yasgar, A. Jadhav, 2013, Journal of biomolecular screening.

Structure-activity relationship studies and biological characterization of human NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors.

Damien Y. Duveau, Adam Yasgar, A. Jadhav, 2014, Bioorganic & medicinal chemistry letters.

Discovery and Optimization of 2H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer.

Mindy I. Davis, D. Urban, Adam Yasgar, 2021, Journal of medicinal chemistry.

Quantitative high‐throughput screening identifies cytoprotective molecules that enhance SUMO conjugation via the inhibition of SUMO‐specific protease (SENP)2

Adam Yasgar, A. Jadhav, A. Simeonov, 2017, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

Novel Consensus Architecture To Improve Performance of Large-Scale Multitask Deep Learning QSAR Models

Noel Southall, Dac-Trung Nguyen, Alexey V Zakharov, 2019, J. Chem. Inf. Model..

Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.

Adam Yasgar, A. Jadhav, A. Simeonov, 2021, Bioorganic & medicinal chemistry.

Quantitative High-Throughput Screening Using a Live-Cell cAMP Assay Identifies Small-Molecule Agonists of the TSH Receptor

Noel Southall, Adam Yasgar, P. Shinn, 2008, Journal of biomolecular screening.

Evaluation of micro-parallel liquid chromatography as a method for HTS-coupled actives verification.

Adam Yasgar, C. Austin, A. Simeonov, 2007, Assay and drug development technologies.

Biochemical and Cellular Characterization and Inhibitor Discovery of Pseudomonas aeruginosa 15-Lipoxygenase.

Joshua D Deschamps, Adam Yasgar, A. Jadhav, 2016, Biochemistry.

Agonists of the TSH Receptor Quantitative High-Throughput Screening Using a Live-Cell cAMP Assay Identifies Small-Molecule

Noel Southall, Adam Yasgar, P. Shinn, 2008 .

Quantitative Bioactivity Signatures of Dietary Supplements and Natural Products.

Deborah K. Ngan, A. Zakharov, Ruili Huang, 2023, ACS pharmacology & translational science.

Discovering selective antiferroptotic inhibitors of the 15LOX/PEBP1 complex noninterfering with biosynthesis of lipid mediators

I. Bahar, H. Bayır, A. Zakharov, 2023, Proceedings of the National Academy of Sciences of the United States of America.