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Journal of Biomolecular Screening
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High-Throughput Biochemical Kinase Selectivity Assays: Panel Development and Screening Applications

Amy Card

Pfizer Research Technology Center, Cambridge, Massachusetts

Chris Caldwell

Pfizer Research Technology Center, Cambridge, Massachusetts

Hyunsuk Min

Pfizer Research Technology Center, Cambridge, Massachusetts

Bina Lokchander

Pfizer Research Technology Center, Cambridge, Massachusetts

Hualin Xi

Pfizer Research Technology Center, Cambridge, Massachusetts

Simone Sciabola

Pfizer Research Technology Center, Cambridge, Massachusetts

Ajith V. Kamath

Pfizer Research Technology Center, Cambridge, Massachusetts

Susan L. Clugston

Pfizer Research Technology Center, Cambridge, Massachusetts

William R. Tschantz

Pfizer Research Technology Center, Cambridge, Massachusetts

Leyu Wang

Pfizer Research Technology Center, Cambridge, Massachusetts

Deborah J. Moshinsky

Pfizer Research Technology Center, Cambridge, Massachusetts, deborah.moshinsky{at}pfizer.com

Kinases represent attractive targets for drug discovery. Eight small-molecule kinase inhibitors are currently marketed in the area of oncology, and numerous others are in clinical trials. Characterization of the selectivity profiles of these compounds is important to target appropriate patient populations and to reduce the potential of toxicity due to off-target effects. The authors describe the development, validation, and utilization of a biochemical kinase assay panel for the selectivity profiling of inhibitors. The panel was developed as 29 radiometric FlashplateTM assays, and then an initial 13 were transitioned to a nonradiometric Caliper mobility shift assay format. Generation of high-quality data from the panel is detailed along with a comparison of the assay formats. Both assay technologies were found to be suitable for panel screening, but mobility shift assays yielded higher data quality. The selectivity data generated here should be useful in computational modeling and help facilitate, in conjunction with sequence and structural information, the rational design of inhibitors with well-defined selectivity profiles. (Journal of Biomolecular Screening 2009:31-42)

Key Words: kinase • panel • screening • profiling • mobility shift assay

This version was published on January 1, 2009

Journal of Biomolecular Screening, Vol. 14, No. 1, 31-42 (2009)
DOI: 10.1177/1087057108326663
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