Finding the molecules to fuel chemogenomics

Within the pharmaceutical industry, chemogenomics focuses on obtaining maximum benefit from the small molecules created in the drug-discovery process. Part of this discipline is the application of small-molecule inhibitors to aid in the characterization of the biological function of targets. The wider application of these approaches is hampered by a lack of reagents – that is, small molecules that have been thoroughly characterized and have appropriate potency and specificity for the target of interest. This review focuses on approaches used in the pharmaceutical industry to produce compounds for use in chemogenomics and on the challenges encountered in quickly characterizing their effects on biological activity.