This book systemically summarizes the concepts and therapeutic application of allosteric modulation, providing an in-depth and yet easily understandable reference for any drug discovery scientist. A virtual bridge for industrial and academic collaborations, the book thoroughly overviews allosteric drug discovery. It explains why allosteric modulation has gained a tremendous amount of momentum in drug discovery, technologies and methodologies used to discover allosteric modulators, and existing and novel compound entities of allosteric modulators. Specific coverage includes the major drug target classes with demonstrated allosteric modulation: GPCRs, ligand-gated ion channels, transporters, and other targets. Color images and protocols that readers can access are hosted on a companion website.