James Inglese

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O. J. Trask, G. Sittampalam, N. Coussens, 2004 .

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.

Subcloning, characterization, and affinity labeling of Escherichia coli glycinamide ribonucleotide transformylase.

S. Benkovic, James Inglese, D. Johnson, 1990, Biochemistry.

Identification of phosphotyrosine mimetic inhibitors of human tyrosyl-DNA phosphodiesterase I by a novel AlphaScreen high-throughput assay

Y. Pommier, A. Jadhav, C. Austin, 2009, Molecular Cancer Therapeutics.

Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase.

Maria Paola Costi, Michael E. Nelson, J. Irwin, 2008, Journal of medicinal chemistry.

Illuminating insights into firefly luciferase and other bioluminescent reporters used in chemical biology.

D. Auld, James Inglese, Natasha Thorne, 2010, Chemistry & biology.

Profile of the GSK Published Protein Kinase Inhibitor Set Across ATP-Dependent and-Independent Luciferases: Implications for Reporter-Gene Assays

R. Guha, D. Drewry, W. Zuercher, 2013, PloS one.

Fluorescence spectroscopic profiling of compound libraries.

Ruili Huang, Noel Southall, P. Shinn, 2008, Journal of medicinal chemistry.

A multiplex calcium assay for identification of GPCR agonists and antagonists.

Noel Southall, P. Shinn, C. Austin, 2010, Assay and drug development technologies.

High-throughput screening assays for the identification of chemical probes.

Christopher P Austin, Anton Simeonov, Menghang Xia, 2007, Nature chemical biology.

A high-throughput screen for aggregation-based inhibition in a large compound library.

Christopher P Austin, Anton Simeonov, James Inglese, 2007, Journal of medicinal chemistry.

Organic Synthesis Toward Small-Molecule Probes and Drugs Special Feature: Discovery of new antimalarial chemotypes through chemical methodology and library development

Aaron B. Beeler, X. Su, S. Schaus, 2011 .

Reporting data from high-throughput screening of small-molecule libraries.

James Inglese, Caroline E Shamu, R Kiplin Guy, 2007, Nature chemical biology.

Characterization of chemical libraries for luciferase inhibitory activity.

Christopher P Austin, Anton Simeonov, James Inglese, 2008, Journal of medicinal chemistry.

A specific mechanism for nonspecific activation in reporter-gene assays.

James Inglese, Dac-Trung Nguyen, Natasha Thorne, 2008, ACS chemical biology.

A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution.

Christopher P Austin, James Inglese, Ganesha Rai, 2009, Journal of medicinal chemistry.

Apparent activity in high-throughput screening: origins of compound-dependent assay interference.

James Inglese, Natasha Thorne, D. Auld, 2010, Current opinion in chemical biology.

Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124

Anton Simeonov, James Inglese, Robert P Hanzlik, 2010, Proceedings of the National Academy of Sciences.

Firefly luciferase in chemical biology: a compendium of inhibitors, mechanistic evaluation of chemotypes, and suggested use as a reporter.

Anton Simeonov, James Inglese, Natasha Thorne, 2012, Chemistry & biology.

Miniaturization of Whole Live Cell-Based GPCR Assays Using Microdispensing and Detection Systems

James Inglese, Oleg Kornienko, Berta Strulovici, 2004, Journal of biomolecular screening.

Miniaturization of a hepatitis C virus RNA polymerase assay using a -102 degrees C cooled CCD camera-based imaging system.

B. Strulovici, James Inglese, L. Howells, 2001, Analytical biochemistry.

High Throughput Screening (HTS) Techniques: Applications in Chemical Biology

James Inglese, Douglas S. Auld, D. Auld, 2008 .

Identification of metabotropic glutamate receptor antagonists using an automated high-throughput screening system.

B. Strulovici, C. Bayly, James Inglese, 2003, Analytical biochemistry.

A quantitative high-throughput screen identifies potential epigenetic modulators of gene expression.

Christopher P Austin, Wenwei Huang, James Inglese, 2008, Analytical biochemistry.

Understanding Enzymes as Reporters or Targets in Assays Using Quantitative High-throughput Screening (qHTS)

Noel Southall, D. Auld, James Inglese, 2010 .

N4-phenyl modifications of N2-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease.

D. Urban, C. Austin, Wei Zheng, 2007, Bioorganic & medicinal chemistry letters.

Active-site mapping and site-specific mutagenesis of glycinamide ribonucleotide transformylase from Escherichia coli.

S. Benkovic, James Inglese, J. Smith, 1990, Biochemistry.

A multisubstrate adduct inhibitor of a purine biosynthetic enzyme with a picomolar dissociation constant.

S. Benkovic, James Inglese, R. Blatchly, 1989, Journal of medicinal chemistry.

Designing innovative therapies for neuropathic pain: pros and cons of target‐based drug discovery

James Inglese, 2014, Journal of the peripheral nervous system : JPNS.

Chemical genomics for studying parasite gene function and interaction.

X. Su, James Inglese, Jian Li, 2013, Trends in parasitology.

Multisubstrate adduct inhibitors of glycinamide ribonucleotide transformylase : synthetic and enzyme-assembled

S. Benkovic, James Inglese, 1991 .

Chemical Genomic Profiling for Antimalarial Therapies, Response Signatures, and Molecular Targets

X. Su, Ruili Huang, C. Austin, 2011, Science.

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.

The Synthesis and Evaluation of Dihydroquinazolin-4-ones and Quinazolin-4-ones as Thyroid Stimulating Hormone Receptor Agonists.

Noel Southall, C. Austin, Wei Zheng, 2011, MedChemComm.

Functionally active targeting domain of the beta-adrenergic receptor kinase: an inhibitor of G beta gamma-mediated stimulation of type II adenylyl cyclase.

R. Lefkowitz, James Inglese, W. Koch, 1994, Proceedings of the National Academy of Sciences of the United States of America.

A macrocyclic peptide library with a structurally constrained cyclopropane-containing building block leads to thiol-independent inhibitors of phosphoglycerate mutase.

S. Shuto, James Inglese, H. Suga, 2020, Chemistry, an Asian journal.

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.

Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors

Joshua D. Amason, J. Rubin, James Inglese, 2019, PloS one.

A homogeneous SIRPα-CD47 cell-based, ligand-binding assay: Utility for small molecule drug development in immuno-oncology

Damien Y. Duveau, Joshua D. Amason, J. Rubin, 2019, bioRxiv.

Isoprenylation of a protein kinase. Requirement of farnesylation/alpha-carboxyl methylation for full enzymatic activity of rhodopsin kinase.

M. Caron, R. Lefkowitz, James Inglese, 1992, The Journal of biological chemistry.

qHTSWaterfall: 3-dimensional visualization software for quantitative high-throughput screening (qHTS) data

James Inglese, J. Braisted, P. Dranchak, 2022, bioRxiv.

High-content quantitative high-throughput screening identifies a cell cycle-associated signaling cascade that regulates a multienzyme metabolic assembly for glucose metabolism

James Inglese, T. Voss, P. Dranchak, 2022, bioRxiv.

ICE1 promotes the link between splicing and nonsense-mediated mRNA decay

Scott E. Martin, Eugen C. Buehler, James Inglese, 2018, eLife.

ICE 1 promotes the link between splicing and nonsense-mediated mRNA decay

Scott E. Martin, Eugen C. Buehler, James Inglese, 2018 .

Chemokine receptor-ligand interactions measured using time-resolved fluorescence.

James Inglese, S. Patel, J. Burbaum, 1998, Biochemistry.

Quantitative High‐Throughput Screening Using a Coincidence Reporter Biocircuit

James Inglese, R. Macarthur, Brittany W Schuck, 2017, Current protocols in neuroscience.

Reply to Peltz et al: Post-translational stabilization of the firefly luciferase reporter by PTC124 (Ataluren)

D. Auld, James Inglese, Natasha Thorne, 2009, Proceedings of the National Academy of Sciences.

Adrenergic receptors: recent insights into their mechanism of activation and desensitization.

M. Caron, R. Lefkowitz, James Inglese, 1993, Advances in second messenger and phosphoprotein research.

Binding of G protein beta gamma-subunits to pleckstrin homology domains.

R. Lefkowitz, James Inglese, G. Shaw, 1994, The Journal of biological chemistry.

Structure and mechanism of the G protein-coupled receptor kinases.

R. Lefkowitz, James Inglese, W. Koch, 1993, The Journal of biological chemistry.

Prenylation-dependent targeting of G-protein-coupled receptor kinases.

James Inglese, 1995, Methods in enzymology.

G-protein-coupled receptors: regulatory role of receptor kinases and arrestin proteins.

M. Caron, R. Lefkowitz, James Inglese, 1992, Cold Spring Harbor symposia on quantitative biology.

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

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

The Binding Site for the @ r Subunits of Heterotrimeric G Proteins on the @-Adrenergic Receptor Kinase *

Robert, W., James Inglese, 2001 .

Cardiac muscarinic potassium channel activity is attenuated by inhibitors of G beta gamma.

R. Stoffel, R. Lefkowitz, James Inglese, 1995, Circulation research.

Palmitoylation increases the kinase activity of the G protein-coupled receptor kinase, GRK6.

R. Stoffel, James Inglese, A. Macrae, 1998, Biochemistry.

The receptor kinase family: primary structure of rhodopsin kinase reveals similarities to the beta-adrenergic receptor kinase.

M. Caron, K. Palczewski, R. Lefkowitz, 1991, Proceedings of the National Academy of Sciences of the United States of America.

Olfactory desensitization requires membrane targeting of receptor kinase mediated by beta gamma-subunits of heterotrimeric G proteins.

R. Lefkowitz, James Inglese, W. Koch, 1994, The Journal of biological chemistry.

Heterotrimeric G Proteins Interact with the Small GTPase ARF

James Inglese, C. D’Souza-Schorey, M. Colombo, 1995, The Journal of Biological Chemistry.

Phosducin, Potential Role in Modulation of Olfactory Signaling*

R. Lefkowitz, James Inglese, M. Lohse, 1997, The Journal of Biological Chemistry.

Determination of the G beta gamma-binding domain of phosducin. A regulatable modulator of G beta gamma signaling.

R. Lefkowitz, James Inglese, B. Hawes, 1994, The Journal of biological chemistry.

Identification of Small Molecule Modulators of Gene Transcription with Anticancer Activity

Ruili Huang, C. Austin, James Inglese, 2014, ACS chemical biology.

Inhibition of natriuretic peptide receptor 1 reduces itch in mice

James Inglese, M. Hoon, J. Braisted, 2019, Science Translational Medicine.

A fluorescence-based thiol quantification assay for ultra-high-throughput screening for inhibitors of coenzyme A production.

Erica M. Stec, M. Ferrer, B. Strulovici, 2008, Assay and drug development technologies.

Bioluminescence-based reporters for characterizing inhibitors and activators of human Sonic Hedgehog protein autoprocessing in live cells at high throughput

James Inglese, P. Dranchak, G. Rai, 2022, bioRxiv.

A 1,536-well-based kinetic HTS assay for inhibitors of Schistosoma mansoni thioredoxin glutathione reductase.

A. Jadhav, C. Austin, A. Simeonov, 2008, Assay and drug development technologies.

Identification of oxadiazoles as new drug leads for the control of schistosomiasis

Anton Simeonov, Christopher P. Austin, James Inglese, 2008, Nature Medicine.

A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases().

A. Jadhav, R. Guha, A. Simeonov, 2012, MedChemComm.

In vivo quantitative high-throughput screening for drug discovery and comparative toxicology

Ruili Huang, M. Xia, James Inglese, 2022, bioRxiv.

Rhodopsin Kinase Autophosphorylation

K. Palczewski, James Inglese, R. Premont, 1995, The Journal of Biological Chemistry.

Cardiomyocyte Impedance Assays -- Assay Guidance Manual

N. Coussens, H. Nelson, M. Arkin, 2004 .

Radiolabeling of receptor ligands by chemical incorporation of phosphorylation sites.

James Inglese, J. Glickman, 1999, Analytical biochemistry.

Functionally active targeting domainofthef-adrenergic receptor kinase: Aninhibitor ofGp'.mediated stimulation oftypeII adenylyl cyclase

R. Lefkowitz, James Inglese, W. Koch, 1994 .

Miniaturizable homogenous time-resolved fluorescence assay for carboxypeptidase B activity.

M. Ferrer, B. Strulovici, James Inglese, 2003, Analytical biochemistry.

Role of beta gamma subunits of G proteins in targeting the beta-adrenergic receptor kinase to membrane-bound receptors.

J. B. Higgins, M. Caron, P. Casey, 1992, Science.

- βARK: β-Adrenergic receptor kinases (vertebrates)

R. Lefkowitz, James Inglese, W. Koch, 1995 .

Protein kinases that phosphorylate activated G protein‐coupled receptors

James Inglese, R. Lefkowitz, R. T. Premont, 1995, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

The binding site for the beta gamma subunits of heterotrimeric G proteins on the beta-adrenergic receptor kinase.

R. Lefkowitz, James Inglese, W. Koch, 1993, The Journal of biological chemistry.

A cell-based bioluminescence reporter assay of human Sonic Hedgehog protein autoprocessing to identify inhibitors and activators

James Inglese, P. Dranchak, G. Rai, 2022, The Journal of biological chemistry.

Compound Cytotoxicity Profiling Using Quantitative High-Throughput Screening

Ruili Huang, Menghang Xia, Noel Southall, 2007, Environmental health perspectives.

High-throughput matrix screening identifies synergistic and antagonistic antimalarial drug combinations

Sam Michael, Paul Shinn, James Inglese, 2015, Scientific Reports.

Rhodopsin kinase: expression in baculovirus-infected insect cells, and characterization of post-translational modifications.

H. Khorana, James Inglese, C. Bruel, 1997, Proceedings of the National Academy of Sciences of the United States of America.

Assay Development for Protein Kinase Enzymes -- Assay Guidance Manual

C. Austin, N. Coussens, M. Arkin, 2004 .

Characterization of diversity in toxicity mechanism using in vitro cytotoxicity assays in quantitative high throughput screening.

Ruili Huang, Christopher P Austin, Menghang Xia, 2008, Chemical research in toxicology.

Use of a Machine Learning-Based High Content Analysis Approach to Identify Photoreceptor Neurite Promoting Molecules.

D. Zack, James Inglese, C. Berlinicke, 2016, Advances in experimental medicine and biology.

Optimization and validation of two miniaturized glucocerebrosidase enzyme assays for high throughput screening.

D. Urban, A. Jadhav, C. Austin, 2008, Combinatorial chemistry & high throughput screening.

Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis.

A. Jadhav, C. Austin, A. Simeonov, 2009, Journal of medicinal chemistry.

Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1α inhibitors.

Ruili Huang, C. Austin, M. Xia, 2011, Bioorganic & medicinal chemistry letters.

Identification of a potent new chemotype for the selective inhibition of PDE4.

M. Nirenberg, Ruili Huang, Noel Southall, 2008, Bioorganic & medicinal chemistry letters.

Cell Viability Assays -- Assay Guidance Manual

Christopher P. Austin, James Inglese, Sittampalam Gs, 2004 .

A robotic platform for quantitative high-throughput screening.

Sam Michael, Christopher P Austin, Anton Simeonov, 2008, Assay and drug development technologies.

Macrocycle peptides delineate locked-open inhibition mechanism for microorganism phosphoglycerate mutases

James Inglese, D. Ross, Hao Yu, 2017, Nature Communications.

Ipomoeassin F Binds Sec61α to Inhibit Protein Translocation

James Inglese, S. High, C. Demangel, 2019, Journal of the American Chemical Society.

Serum-Stable and Selective Backbone-N-Methylated Cyclic Peptides That Inhibit Prokaryotic Glycolytic Mutases.

T. Katoh, James Inglese, K. Battaile, 2022, ACS chemical biology.

Identification of Potent and Selective Diphenylpropanamide RORγ Inhibitors.

Ruili Huang, C. Austin, Jun R Huh, 2013, ACS medicinal chemistry letters.

A PDZ domain-based detection system for enzymatic assays.

M. Ferrer, James Inglese, A. C. Hamilton, 2002, Analytical biochemistry.

The increasing urgency for standards in basic biologic research.

James Inglese, James Inglese, L. Freedman, 2014, Cancer research.

Crystal structure of glycinamide ribonucleotide transformylase from Escherichia coli at 3.0 A resolution. A target enzyme for chemotherapy.

I. Wilson, S. Benkovic, James Inglese, 1992, Journal of molecular biology.

Preliminary crystallographic investigations of glycinamide ribonucleotide transformylase.

I. Wilson, S. Benkovic, James Inglese, 1989, The Journal of biological chemistry.

Mechanism of PTC124 activity in cell-based luciferase assays of nonsense codon suppression

D. Auld, James Inglese, Natasha Thorne, 2009, Proceedings of the National Academy of Sciences.

Activation of the cloned muscarinic potassium channel by G protein βγ subunits

Y. Jan, L. Jan, H. Bourne, 1994, Nature.

Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.

Ruili Huang, C. Austin, M. Xia, 2009, Bioorganic & medicinal chemistry letters.

Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum

X. Su, Ruili Huang, C. Austin, 2009, Nature chemical biology.

Comprehensive Characterization of Cytochrome P450 Isozyme Selectivity across Chemical Libraries

Ruili Huang, Noel Southall, Christopher P. Austin, 2009, Nature Biotechnology.

Genome-Edited Cell Lines for High-Throughput Screening.

James Inglese, J. Svaren, John J. Moran, 2018, Methods in molecular biology.

Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis

Christian M. Metallo, William J. Israelsen, Abhishek K. Jha, 2012, Nature chemical biology.

Functional genomic screening identifies dual leucine zipper kinase as a key mediator of retinal ganglion cell death

D. Zack, W. Hauswirth, S. Boye, 2013, Proceedings of the National Academy of Sciences.

Cellular expression of the carboxyl terminus of a G protein-coupled receptor kinase attenuates G beta gamma-mediated signaling.

R. Lefkowitz, James Inglese, W. Koch, 1994, The Journal of biological chemistry.

Identification of chemical compounds that induce HIF-1alpha activity.

Ruili Huang, Christopher P Austin, Raymond R Tice, 2009, Toxicological sciences : an official journal of the Society of Toxicology.

Palmitoylation of G protein-coupled receptor kinase, GRK6. Lipid modification diversity in the GRK family.

R. Stoffel, R. Lefkowitz, James Inglese, 1994, The Journal of biological chemistry.

Innovation in academic chemical screening: filling the gaps in chemical biology.

James Inglese, James Inglese, Samuel A. Hasson, 2013, Current opinion in chemical biology.

Selective and cell-active inhibitors of the USP1/ UAF1 deubiquitinase complex reverse cisplatin resistance in non-small cell lung cancer cells.

A. Jadhav, A. Simeonov, James Inglese, 2011, Chemistry & biology.

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.

Authentication of Human Cell Lines by STR DNA Profiling Analysis -- Assay Guidance Manual

James Inglese, Sittampalam Gs, Michelle R. Arkin, 2013 .

A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.

James Inglese, C. S. Hoffman, S. Mbugua, 2019, Cellular signalling.

A dual-fluorescence high-throughput cell line system for probing multidrug resistance.

Christopher P Austin, James Inglese, Michael M Gottesman, 2009, Assay and drug development technologies.

Mitigating risk in academic preclinical drug discovery

James Inglese, Jayme L. Dahlin, Michael A. Walters, 2015, Nature Reviews Drug Discovery.

Quantitative High-Throughput Screen Identifies Inhibitors of the Schistosoma mansoni Redox Cascade

Anton Simeonov, Christopher P. Austin, James Inglese, 2008, PLoS neglected tropical diseases.

Genome Editing-Enabled HTS Assays Expand Drug Target Pathways for Charcot–Marie–Tooth Disease

R. Guha, James Inglese, Yolanda Santiago, 2014, ACS chemical biology.

High throughput screening to identify inhibitors of the type I interferon – major histocompatibility complex class I pathway in skeletal muscle

James Inglese, P. Dranchak, Travis B. Kinder, 2020, bioRxiv.

Gβγ interactions with PH domains and Ras-MAPK signaling pathways

R. Lefkowitz, James Inglese, W. Koch, 1995 .

Identification of pregnane X receptor ligands using time-resolved fluorescence resonance energy transfer and quantitative high-throughput screening.

Christopher P Austin, Anton Simeonov, James Inglese, 2009, Assay and drug development technologies.

Phenotype-driven chemical screening in zebrafish for compounds that inhibit collective cell migration identifies multiple pathways potentially involved in metastatic invasion

N. Crawford, P. Shinn, James Inglese, 2015, Disease Models & Mechanisms.

Isoprenylation in regulation of signal transduction by G-protein-coupled receptor kinases

James Inglese, Marc G. Caron, Robert J. Lefkowitz, 1992, Nature.

Chemogenomic profiling of endogenous PARK2 expression using a genome-edited coincidence reporter.

R. Guha, James Inglese, R. Youle, 2015, ACS chemical biology.

Early Drug Discovery and Development Guidelines: For Academic Researchers, Collaborators, and Start-up Companies

Jeffrey Strovel, Sitta Sittampalam, James Inglese, 2016 .

Ligand-receptor binding measured by laser-scanning imaging.

James Inglese, J. Burbaum, P. Zuck, 1999, Proceedings of the National Academy of Sciences of the United States of America.

Detecting Secretory Proteins by Acoustic Droplet Ejection in Multiplexed High-Throughput Applications.

James Inglese, I. Singeç, Dingyin Tao, 2019, ACS chemical biology.

Development of an intact cell reporter gene beta-lactamase assay for G protein-coupled receptors for high-throughput screening.

James Inglese, Peter Hodder, Berta Strulovici, 2003, Analytical biochemistry.

G beta gamma interactions with PH domains and Ras-MAPK signaling pathways.

R. Lefkowitz, James Inglese, W. Koch, 1995, Trends in biochemical sciences.

A PDZ domain‐based assay for measuring HIV protease activity: Assay design considerations

M. Ferrer, James Inglese, A. C. Hamilton, 2003, Protein science : a publication of the Protein Society.

Assay design considerations A PDZ domain-based assay for measuring HIV protease activity :

M. Ferrer, James Inglese, A. C. Hamilton, 2003 .

Identification, purification, and characterization of GRK5, a member of the family of G protein-coupled receptor kinases.

R. Lefkowitz, James Inglese, W. Koch, 1994, The Journal of biological chemistry.

Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.

Christopher P Austin, Anton Simeonov, James Inglese, 2010, Journal of medicinal chemistry.

Genome-Edited Coincidence and PMP22-HiBiT Fusion Reporter Cell Lines Enable an Artifact-Suppressive Quantitative High-Throughput Screening Strategy for PMP22 Gene-Dosage Disorder Drug Discovery.

A. Dutra, James Inglese, J. Svaren, 2021, ACS pharmacology & translational science.

Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease.

Christopher P Austin, Anton Simeonov, James Inglese, 2010, Journal of medicinal chemistry.

Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice

B. Raaka, Noel Southall, C. Austin, 2009, Proceedings of the National Academy of Sciences.

Assay Development Guidelines for Image-Based High Content Screening, High Content Analysis and High Content Imaging -- Assay Guidance Manual

James Inglese, Sittampalam Gs, Nathan P. Coussens, 2014 .

G Protein–Coupled Receptor Kinase Mediates Desensitization of Norepinephrine-Induced Ca2+ Channel Inhibition

R. Stoffel, R. Lefkowitz, James Inglese, 1996, Neuron.

A Cell-Based β-Lactamase Reporter Gene Assay for the CREB Signaling Pathway

M. Nirenberg, Ruili Huang, C. Austin, 2009, Current chemical genomics.

Weighted feature significance: a simple, interpretable model of compound toxicity based on the statistical enrichment of structural features.

Ruili Huang, Christopher P Austin, Raymond R Tice, 2009, Toxicological sciences : an official journal of the Society of Toxicology.

Comparison on Functional Assays for Gq-Coupled GPCRs by Measuring Inositol Monophospate-1 and Intracellular Calcium in 1536-Well Plate Format

Noel Southall, C. Austin, Wei Zheng, 2008, Current chemical genomics.

Characterization of the G Protein-coupled Receptor Kinase GRK4

M. MacDonald, R. Stoffel, R. Lefkowitz, 1996, The Journal of Biological Chemistry.

Structure–activity relationship of ipglycermide binding to phosphoglycerate mutases

James Inglese, J. M. Rogers, L. Lamy, 2021, The Journal of biological chemistry.

A Quantitative High-Throughput Screen Identifies Novel Inhibitors of the Interaction of Thyroid Receptor β with a Peptide of Steroid Receptor Coactivator 2

Ruili Huang, C. Austin, James Inglese, 2011, Journal of biomolecular screening.

The pilot phase of the NIH Chemical Genomics Center.

Ruili Huang, Sam Michael, Christopher P Austin, 2009, Current topics in medicinal chemistry.

A quantitative high-throughput screen for modulators of IL-6 signaling: a model for interrogating biological networks using chemical libraries.

Ruili Huang, Menghang Xia, Noel Southall, 2009, Molecular bioSystems.

Identification of compounds that potentiate CREB signaling as possible enhancers of long-term memory

Ruili Huang, Christopher P Austin, Menghang Xia, 2009, Proceedings of the National Academy of Sciences.

A bioluminescent cytotoxicity assay for assessment of membrane integrity using a proteolytic biomarker.

Ruili Huang, Christopher P Austin, Menghang Xia, 2008, Toxicology in vitro : an international journal published in association with BIBRA.

Compound Management for Quantitative High-Throughput Screening

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

Identification of small molecule compounds that inhibit the HIF-1 signaling pathway

Ruili Huang, Christopher P Austin, Menghang Xia, 2009, Molecular Cancer.

A coincidence reporter-gene system for high-throughput screening

James Inglese, K. Cheng, 2012, Nature Methods.

A Cell-Based PDE4 Assay in 1536-Well Plate Format for High-Throughput Screening

Christopher P Austin, Noel Southall, Wei Zheng, 2008, Journal of biomolecular screening.

A Cell-based PDE 4 Assay in 1536-well Plate format for High Throughput Screening

Noel Southall, C. Austin, Wei Zheng, 2008 .

Directed evolution of PDZ variants to generate high-affinity detection reagents.

James Inglese, Marc Ferrer, M. Ferrer, 2005, Protein engineering, design & selection : PEDS.

Methylsulfonylnitrobenzoates, a New Class of Irreversible Inhibitors of the Interaction of the Thyroid Hormone Receptor and Its Obligate Coactivators That Functionally Antagonizes Thyroid Hormone*

Ruili Huang, C. Austin, James Inglese, 2011, The Journal of Biological Chemistry.

Titration-based screening for evaluation of natural product extracts: identification of an aspulvinone family of luciferase inhibitors.

James Inglese, David H Sherman, Min Shen, 2011, Chemistry & biology.

Differentiating Alzheimer disease-associated aggregates with small molecules

Wenwei Huang, James Inglese, Jeff Kuret, 2007, Neurobiology of Disease.

Assay Guidance Manual: Quantitative Biology and Pharmacology in Preclinical Drug Discovery

Sam Michael, Anton Simeonov, Menghang Xia, 2018, Clinical and translational science.

Ca-dependent Interaction of Recoverin with Rhodopsin Kinase (*)

J B Hurley, J. Hurley, R. Lefkowitz, 1995, The Journal of Biological Chemistry.

Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase.

Noel Southall, C. Austin, L. Cantley, 2010, Bioorganic & medicinal chemistry letters.

Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening.

Ruili Huang, Christopher P Austin, Wenwei Huang, 2009, Biochemistry.

Erratum: Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis (Nature Chemical Biology (2012) 8 (839-847))

Abhishek K. Jha, G. Stephanopoulos, Noel Southall, 2012 .

Pharmacokinetics and Drug Metabolism

C. Austin, O. J. Trask, G. Sittampalam, 2004 .

Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.

Christopher P Austin, Noel Southall, James Inglese, 2010, Journal of medicinal chemistry.

Assay Interference by Chemical Reactivity -- Assay Guidance Manual

James Inglese, Sittampalam Gs, Michelle R. Arkin, 2004 .

In vitro 3D Spheroids and Microtissues: ATP-based Cell Viability and Toxicity Assays -- Assay Guidance Manual

Christopher P. Austin, James Inglese, Sittampalam Gs, 2004 .

Actinoramide A Identified as a Potent Antimalarial from Titration-Based Screening of Marine Natural Product Extracts.

X. Su, R. Guha, J. Clardy, 2015, Journal of Natural Products.

Monitoring Compound Integrity With Cytochrome P450 Assays and qHTS

Christopher P Austin, Paul Shinn, Noel Southall, 2009, Journal of biomolecular screening.

Minimum Significant Ratio – A Statistic to Assess Assay Variability -- Assay Guidance Manual

C. Austin, N. Coussens, M. Arkin, 2013 .

A β-Lactamase-Dependent Gal4-Estrogen Receptor β Transactivation Assay for the Ultra-High Throughput Screening of Estrogen Receptor β Agonists in a 3,456-Well Format

M. Ferrer, B. Strulovici, L. Mitnaul, 2003 .

A fully automated [35S]GTPgammaS scintillation proximity assay for the high-throughput screening of Gi-linked G protein-coupled receptors.

M. Ferrer, B. Strulovici, James Inglese, 2003, Assay and drug development technologies.

Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk).

T. Misteli, P. Shinn, C. Austin, 2009, Bioorganic & medicinal chemistry letters.

Comparison of bioluminescent kinase assays using substrate depletion and product formation.

James Inglese, Min Shen, Cordelle Tanega, 2009, Assay and drug development technologies.

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.

Identification of drug modulators targeting gene-dosage disease CMT1A.

James Inglese, J. Svaren, R. Macarthur, 2012, ACS chemical biology.

Rapid RNA–ligand interaction analysis through high-information content conformational and stability landscapes

A. Ferré-D’Amaré, James Inglese, N. Baird, 2015, Nature Communications.

A cell-based β-lactamase reporter gene assay for the identification of inhibitors of hepatitis C virus replication

James Inglese, Marc Ferrer, Berta Strulovici, 2004 .

Measuring biological responses with automated microscopy

James Inglese, 2006 .

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

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

A high content screening approach to identify molecules neuroprotective for photoreceptor cells.

D. Zack, James Inglese, C. Berlinicke, 2014, Advances in experimental medicine and biology.

Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation.

L. Staudt, R. Davis, Noel Southall, 2008, Bioorganic & medicinal chemistry letters.

Interferences with Luciferase Reporter Enzymes

James Inglese, Douglas S. Auld, D. Auld, 2016 .

Activation of the cloned muscarinic potassium channel by G protein beta gamma subunits.

Y. Jan, L. Jan, H. Bourne, 1994, Nature.

Genome Editing Using Engineered Nucleases and Their Use in Genomic Screening -- Assay Guidance Manual

Jayme L. Dahlin, Devanaryan, Timothy L. Foley, 2004 .

A Cell-Based Assay for IκBα Stabilization Using A Two-Color Dual Luciferase-Based Sensor

Noel Southall, Christopher P. Austin, James Inglese, 2007 .

Basics of Enzymatic Assays for HTS -- Assay Guidance Manual

C. Austin, N. Coussens, M. Arkin, 2004 .

Identification of small molecule antagonists of the neuropeptide S receptor

Noel Southall, Wei Zheng, J. Marugan, 2010 .

FLIPR™ Assays for GPCR and Ion Channel Targets -- Assay Guidance Manual

Jayme L. Dahlin, Devanaryan, Timothy L. Foley, 2012 .

Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease

Christopher P Austin, Anton Simeonov, Wei Zheng, 2007, Proceedings of the National Academy of Sciences.

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.

Advanced Assay Development Guidelines for Image-Based High Content Screening and Analysis -- Assay Guidance Manual

Christopher P. Austin, James Inglese, Sittampalam Gs, 2004 .

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.

gamma-Fluoromethotrexate: synthesis and biological activity of a potent inhibitor of dihydrofolate reductase with greatly diminished ability to form poly-gamma-glutamates.

James Inglese, J. Coward, J. Galivan, 1985, Proceedings of the National Academy of Sciences of the United States of America.

Engineering Bacterial Transcription Regulation To Create a Synthetic in Vitro Two-Hybrid System for Protein Interaction Assays

James Inglese, James Inglese, P. Dranchak, 2014, Journal of the American Chemical Society.

A miniaturized glucocorticoid receptor translocation assay using enzymatic fragment complementation evaluated with qHTS.

Christopher P Austin, James Inglese, Ajit Jadhav, 2008, Combinatorial chemistry & high throughput screening.

An AlphaScreenTM-Based High-Throughput Screen to Identify Inhibitors of Hsp90-Cochaperone Interaction

L. Regan, Noel Southall, C. Austin, 2009, Journal of biomolecular screening.

Assay Interference by Aggregation

James Inglese, Jayme L. Dahlin, Douglas S. Auld, 2017 .

A cell-based beta-lactamase reporter gene assay for the identification of inhibitors of hepatitis C virus replication.

James Inglese, Marc Ferrer, Berta Strulovici, 2004, Analytical biochemistry.

HTS technologies to facilitate chemical genomics

Christopher P. Austin, James Inglese, James McGee, 2007 .

Biology-driven library design for probe discovery.

James Inglese, Samuel A. Hasson, 2011, Chemistry & biology.

Histone Acetyltransferase Assays in Drug and Chemical Probe Discovery -- Assay Guidance Manual

Jayme L. Dahlin, Devanaryan, Timothy L. Foley, 2018 .

Bioluminescence Methods for Assaying Kinases in Quantitative High-Throughput Screening (qHTS) Format Applied to Yes1 Tyrosine Kinase, Glucokinase, and PI5P4Kα Lipid Kinase.

Mindy I. Davis, D. Auld, James Inglese, 2016, Methods in molecular biology.

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 .

High-throughput screening identifies cell cycle-associated signaling cascades that regulate a multienzyme glucosome assembly in human cells

James Inglese, T. Voss, P. Dranchak, 2023, PloS one.

Automated Electrophysiology Assays -- Assay Guidance Manual

Menghang Xia, Christopher P. Austin, James Inglese, 2004 .

HTS Assay Validation -- Assay Guidance Manual

C. Austin, N. Coussens, M. Arkin, 2004 .

Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice

B. Raaka, Noel Southall, C. Austin, 2009, Proceedings of the National Academy of Sciences.

Mechanism of PTC124 activity in cell-based luciferase assays of nonsense codon suppression

D. Auld, James Inglese, Natasha Thorne, 2009, Proceedings of the National Academy of Sciences.

A 1536-well cAMP assay for Gs- and Gi-coupled receptors using enzyme fragmentation complementation.

M. Ferrer, B. Strulovici, Wei Zheng, 2004, Assay and drug development technologies.

Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124

A. Simeonov, D. Auld, James Inglese, 2010, Proceedings of the National Academy of Sciences.

Firefly luciferase in chemical biology: a compendium of inhibitors, mechanistic evaluation of chemotypes, and suggested use as a reporter.

A. Simeonov, D. Auld, James Inglese, 2012, Chemistry & biology.

Interference with Fluorescence and Absorbance -- Assay Guidance Manual

Christopher P. Austin, James Inglese, Sittampalam Gs, 2004 .