James Inglese

发表

Figure 17: [Clinical Supplies Manufacture].

Christopher P. Austin, Michael Hughes, Jeffrey Strovel, 2016 .

Assay Operations for SAR Support -- Assay Guidance Manual

James Inglese, Sittampalam Gs, Nathan P. Coussens, 2004 .

Figure 22, [– Development Plan].

Christopher P. Austin, Michael Hughes, Jeffrey Strovel, 2016 .

Data Standardization for Results Management -- Assay Guidance Manual

James Inglese, Sittampalam Gs, Nathan P. Coussens, 2004 .

HTS technologies to facilitate chemical genomics

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

Automated Electrophysiology Assays -- Assay Guidance Manual

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

Method with high throughput

James Inglese, Daniel Chelsky, Jonathan J. Burbaum, 1998 .

A robotic platform for quantitative high-throughput screening.

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

Compound Management for Quantitative High-Throughput Screening

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

Figure 11: [Summary of Decision Points for Drug Repurposing].

Christopher P. Austin, Michael Hughes, Jeffrey Strovel, 2016 .

Technology Review A Robotic Platform for Quantitative High-Throughput Screening

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

IP-3/IP-1 Assays -- Assay Guidance Manual

James Inglese, Jeffrey R. Weidner, Lisa Minor, 2004 .

Assay Validation, Operations and Quality Control

Christopher P. Austin, James Inglese, G. Sitta Sittampalam, 2004 .

Figure 10: [Decision Point #11 in Detail].

Christopher P. Austin, Michael Hughes, Jeffrey Strovel, 2012 .

Figure 2: [Target Identification and Target Validation].

Christopher P. Austin, Michael Hughes, Jeffrey Strovel, 2016 .

Figure 1: [General strategies to identify assay...].

James Inglese, Douglas S. Auld, 2016 .

Expanding the HTS paradigm.

James Inglese, 2002, Drug discovery today.

Impedance-Based Technologies -- Assay Guidance Manual

James Inglese, Sittampalam Gs, Nathan P. Coussens, 2004 .

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 .

A Practical Guide to Assay Development and High‐Throughput Screening in Drug Discovery. Edited by Taosheng Chen.

James Inglese, 2010 .

In Vitro and In Vivo Assessment of ADME and PK Properties During Lead Selection and Lead Optimization – Guidelines, Benchmarks and Rules of Thumb -- Assay Guidance Manual

James Inglese, Sittampalam Gs, Nathan P. Coussens, 2004 .

Development and Applications of the Bioassay Ontology (BAO) to Describe and Categorize High-Throughput Assays -- Assay Guidance Manual

James Inglese, Sittampalam Gs, Nathan P. Coussens, 2004 .

Figure 7: [Selection of a Development Candidate].

Christopher P. Austin, Michael Hughes, Jeffrey Strovel, 2016 .

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

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

Figure 16: [Preclinical Safety Data Package].

Christopher P. Austin, Michael Hughes, Jeffrey Strovel, 2016 .

Figure 24, [– Preclinical Safety Package].

Christopher P. Austin, Michael Hughes, Jeffrey Strovel, 2016 .

Basics of Assay Equipment and Instrumentation for High Throughput Screening -- Assay Guidance Manual

James Inglese, Sittampalam Gs, Nathan P. Coussens, 2004 .

Figure 20: [Summary of Decision Points for Drug Delivery Platform Technology].

Christopher P. Austin, Michael Hughes, Jeffrey Strovel, 2016 .

Figure 14: [Gap Analysis/Development Plan].

Christopher P. Austin, Michael Hughes, Jeffrey Strovel, 2016 .

Figure 27: [Clinical Proof of Concept].

Christopher P. Austin, Michael Hughes, Jeffrey Strovel, 2016 .

Figure 19: [Human Proof of Concept].

Christopher P. Austin, Michael Hughes, Jeffrey Strovel, 2016 .

Figure 1: [Composite Gantt Chart Roll-up Representing Target ID through Clinical POC].

Christopher P. Austin, Michael Hughes, Jeffrey Strovel, 2016 .

[Table, List of PubChem bioassay identifiers generated for this screening project (AIDs)].

James Inglese, Noel Southall, Douglas S. Auld, 2010 .

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

Jeffrey Strovel, Sitta Sittampalam, James Inglese, 2016 .

New in Assay Guidance Manual

Christopher P. Austin, James Inglese, G. Sitta Sittampalam, 2004 .

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.

Figure 15: [Clinical Formulation Development].

Christopher P. Austin, Michael Hughes, Jeffrey Strovel, 2016 .

Scheme 4, [General procedure for the synthesis of analogues].

Noel Southall, James Inglese, Douglas S. Auld, 2010 .

[Table], PubChem Primary Bioassay Identifier (AID): 1631

James Inglese, Noel Southall, Douglas S. Auld, 2010 .

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

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

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.

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

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

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

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

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

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

Assay Interference by Aggregation

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

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.

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.

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.

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

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

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.

Interferences with Luciferase Reporter Enzymes -- Assay Guidance Manual

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

Assay Interference by Chemical Reactivity -- Assay Guidance Manual

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

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.

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

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

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.

Comprehensive Characterization of Cytochrome P450 Isozyme Selectivity across Chemical Libraries

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

Interference with Fluorescence and Absorbance -- Assay Guidance Manual

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

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

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

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

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

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

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

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.

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.

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

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

Monitoring Compound Integrity With Cytochrome P450 Assays and qHTS

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

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.

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.

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

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

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

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

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 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.

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

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

The increasing urgency for standards in basic biologic research.

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

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

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

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

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

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

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

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.

Interferences with Luciferase Reporter Enzymes

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

Mitigating risk in academic preclinical drug discovery

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

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.

Cell Viability Assays -- Assay Guidance Manual

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

The pilot phase of the NIH Chemical Genomics Center.

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

Compound Cytotoxicity Profiling Using Quantitative High-Throughput Screening

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

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 .

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.

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.

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.

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.

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.

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

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

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

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

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.

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.

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.

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

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

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

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

Differentiating Alzheimer disease-associated aggregates with small molecules

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

A High Throughput Screening Assay System for the Identification of Small Molecule Inhibitors of gsp

Juan J. Marugan, Noel Southall, Christopher P. Austin, 2014, PloS one.