This book presents the state-of-the-art in drug discovery. From the theoretical and operational considerations involved in generating a collection of compounds to screen, to the design and implementation of high-capacity and high-quality assays, this book provides a comprehensive overview of modern approaches to lead identification. Beginning with an introductory overview, the book addresses the design of chemical libraries and methods for optimizing diversity; automated and accelerated chemistry; high throughput assay design and detection techniques; and strategies for data analysis and property optimization.