Medical community and pharmaceutical companies are currently facing a dire need for discovery and identification of new druggable targets.  However, the discovery of small-molecule target is an important and arduous task for the biological and medical scientists.  To overcome the bottlenecks for target validation, many new approaches are being developed, such as chemical proteomics.  As a part of proteomics approaches, chemical proteomics employs small-molecule compounds that can specifically interact with the target protein to interfere with and detect proteomics.  Therefore, new target identification, drug discovery and research on multi-target-directed drugs will all be benefited from the further advances in chemical proteomics approaches.  Chemical proteomics has the potential to greatly enhance the efficiency of the drug discovery process.