Debra Gallant

Molecular Devices

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Michael Briskin

National Bureau of Economic Research

Nancy A. Cochran

Millennium Engineering and Integration (United States)

Charles F. Schwender

KalVista Pharmaceuticals (United States)

Hitesh N. Shroff

Center for Drug Evaluation and Research

A. D. BAXTER

Worcestershire Royal Hospital

Geraldine Harriman

Japan Breast Cancer Research Group

John M. Proctor

Sir Charles Gairdner Hospital

Ryan McGuinness

Fordham University

Loren Payne

KalVista Pharmaceuticals (United States)

Frederick A. Brookfield

Evotec (United Kingdom)

Cooperative Institutions

Millennium Engineering and Integration (United States)

KalVista Pharmaceuticals (United States)

Molecular Devices

Oxford Policy Management

AstraZeneca (United States)

University of California, San Francisco

Stanford University

Pfizer (United States)

Merck & Co., Inc., Rahway, NJ, USA (United States)

Springhouse

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Development of inhibitors of MAdCAM-1/α4β7 interactions

Kluwer Academic Publishers eBooks (2005)

Hitesh N. Shroff Charles F. Schwender A. D. BAXTER N. Hone Nancy A. Cochran

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10.1007/0-306-46862-x_82

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Enhanced Selectivity Screening of GPCR Ligands Using a Label-Free Cell Based Assay Technology

Combinatorial Chemistry & High Throughput Screening (2009)

Ryan McGuinness John M. Proctor Debra Gallant Carlo van Staden Jenny Ly

Drug discovery efforts advance in step with advancements in assay technologies, as new technologies provide new lenses through which biology can be viewed. The novel information gathered results in the better understanding of drug-target interactions leading to better decision making during the drug discovery process. One area of rapid development is within label-free technologies. Label-free technologies offer many distinct advantages to the drug discovery workflow. One such novel technology is the CellKey System, an impedance-based label-free live cell assay platform. The system is based on impedance technology and is a universal platform for the functional measurement of all classes of G-protein coupled receptors (GPCRs). Data are generated in a kinetic fashion on both endogenously expressed and transfected receptors in a wide variety of cell types. In the studies detailed here, we used the system to perform an enhanced selectivity screen of a small panel of compounds simultaneously against two unrelated GPCR targets signaling through different pathways. Utilizing both the quantitative measures of cellular activation and the qualitative information inherent in the rich output data, we gained knowledge not only about the relative selectivity of each compound across both targets, but also about the character of the interaction of each with the cellular target. In this manner, we successfully demonstrated proof of principal for using an impedance-based technology to perform selectivity analyses and to triage lead compounds in a simplified format.

10.2174/138620709789104861

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Citations (20)

The CellKey® System: A Label‐Free Cell‐Based Assay Platform for Early Drug Discovery Applications

Ryan McGuinness Debra Gallant Yen‐Wen Chen Trisha A. Tutana Donna L. Wilson

This chapter contains sections titled: Introduction Cellular Impedance Technology Target Identification and Validation Screening and Lead Optimization Conclusion References

10.1002/9780470979129.ch4

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ChemInform Abstract: Cell Adhesion Antagonists: Synthesis and Evaluation of a Novel Series of Phenylalanine Based Inhibitors.

ChemInform (2000)

Geraldine Harriman Charles F. Schwender Debra Gallant Nancy A. Cochran Michael Briskin

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

10.1002/chin.200045191

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Novel modified tripeptide inhibitors of α4β7 mediated lymphoid cell adhesion to MAdCAM-1

Bioorganic & Medicinal Chemistry Letters (1998)

Hitesh N. Shroff Charles F. Schwender A. D. BAXTER Frederick A. Brookfield Loren Payne

Tripeptide

Addressin

10.1016/s0960-894x(98)00286-8

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Citations (14)

Cell adhesion antagonists: synthesis and evaluation of a novel series of phenylalanine based inhibitors