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Rethinking screening

Bioactive compounds are most frequently identified via high-throughput screening campaigns. This article discusses the strengths and weaknesses of the most popular screening approaches and the utility of compounds derived from them.

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Figure 1: Examples of chemical syntheses used for the construction of combinatorial libraries that are simple enough for non-expert chemists to carry out.
Figure 2: Discovery of peptoid ligands for an integral membrane receptor via a two-color cell binding screen VEGF receptor 2 (VEGFR2) was the target of this screen.

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Acknowledgements

I thank G. Micalizo, P. MacDonald and P. LoGrasso (Scripps Florida) for comments on the manuscript and the US National Institutes of Health (DP10D00066301) for support.

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Correspondence to Thomas Kodadek.

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Kodadek, T. Rethinking screening. Nat Chem Biol 6, 162–165 (2010). https://doi.org/10.1038/nchembio.303

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