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New opportunities to use small molecules both as probes for deciphering the control mechanism of living organisms and as potential leads for developing new therapeutics for disease treatment are ushering in a new era of chemical biology. Summarizing the major issues and approaches to chemical biology and the applications in drug design and development, Small Molecules for Protein Targeting provides chemical biologists and medicinal chemists with a detailed review of chemical genomics, target profiling immobilization technology, detection methods, and much more.