Small Molecule Selectivity and Specificity Profiling Using Functional Protein Microarrays

  • Peter R. Kraus
  • Lihao Meng
  • Lisa Freeman-CookEmail author
Part of the Methods in Molecular Biology book series (MIMB, volume 632)


Small molecules interact with proteins to perturb their functions, a property that has been exploited both for research applications and to produce therapeutic agents for disease treatment. Commonly utilized approaches for identifying the target proteins for a small molecule have limitations in terms of throughput and resource consumption and lack a mechanism to broadly assess the selectivity profile of the small molecule. Here we describe how protein microarray technology can be applied to the study of small molecule-protein interactions using tritiated small molecules. Protein arrays comprising thousands of full-length functional proteins facilitate target identification for those small molecules discovered in cell-based phenotypic assays and both target validation and off-target binding assessment for compounds discovered in target-based screens. The assays are highly reproducible, sensitive, and scalable, and provide an enabling technology for small molecule selectivity profiling in the context of drug development.

Key words

Protein-small molecule interaction Small molecule Protein microarray Off target effect Selectivity profiling Specificity profiling 


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Copyright information

© Humana Press, a part of Springer Science+Business Media, LLC 2010

Authors and Affiliations

  • Peter R. Kraus
    • 1
  • Lihao Meng
    • 1
  • Lisa Freeman-Cook
    • 1
    Email author
  1. 1.Life TechnologiesCarlsbadUSA

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