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Updated: Jun 27, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

High-throughput biochemical kinase selectivity assays: panel development and screening applications.

Amy Card¹, Chris Caldwell, Hyunsuk Min

¹Pfizer Research Technology Center, Cambridge, Massachusetts, USA.

Journal of Biomolecular Screening

|December 17, 2008

Summary

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Researchers developed a biochemical kinase assay panel to profile small-molecule inhibitors. Mobility shift assays provided higher data quality than radiometric assays, aiding rational drug design for oncology kinase inhibitors.

Area of Science:

Biochemistry
Pharmacology
Drug Discovery

Background:

Kinase inhibitors are crucial in oncology drug discovery, with eight marketed and many in clinical trials.
Understanding inhibitor selectivity is vital for effective patient targeting and minimizing off-target toxicity.

Purpose of the Study:

To develop and validate a biochemical kinase assay panel for selectivity profiling of small-molecule inhibitors.
To compare the performance of radiometric and non-radiometric assay formats for kinase inhibitor screening.

Main Methods:

Development of a 29-assay radiometric Flashplate panel.
Transition of 13 assays to a non-radiometric Caliper mobility shift assay format.
Generation and quality assessment of selectivity data using both assay formats.

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Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

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Main Results:

Both radiometric Flashplate and Caliper mobility shift assays are suitable for kinase inhibitor panel screening.
Mobility shift assays demonstrated superior data quality compared to radiometric assays.
The generated selectivity data are valuable for computational modeling and rational inhibitor design.

Conclusions:

The developed kinase assay panel provides high-quality selectivity data for small-molecule inhibitors.
Mobility shift assays offer advantages in data quality for kinase inhibitor profiling.
These findings support the rational design of kinase inhibitors with improved selectivity profiles for oncology applications.