Abstract
Chemogenomics is an innovative approach in chemical biology that synergizes combinatorial chemistry and genomic and proteomic biology to systematically study the response of a biological system to a set of compounds, which can aid the identification and validation of biological targets as well as biologically active small-molecule agents responsible for a phenotypic outcome. Central to this strategy is a collection of chemically diverse compounds, a so-called chemogenomics library. Selection and annotation of vastly available chemogenomic compound candidates for an inclusion in such set present a challenge, but optimal compound selection is critical for success of chemogenomics. The library can be used in a wide variety of research applications from biological mechanism deconvolution to drug discovery. However, phenotypic screening methods are typically required to be high-throughput and equipped with a systematic analysis of complex biological-chemical interactions. This chapter provides a general outline to the chemogenomics approach, including concept and critical steps in all stages of this innovative chemical biology strategy.
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