Conceptual and technological advances in chemistry and biology have transformed the drug discovery process. Evolutionary pressure among the diverse scientific and engineering disciplines that contribute to the identification of biologically active compounds has resulted in synergistic improvements at every step in the process. Exploiting Chemical Diversity for Drug Discovery encompasses the many components of this transformation and presents the current state-of-the-art of this critical endeavour. From the theoretical and operational considerations 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, subsequent chapters address topics that include the design of chemical libraries and methods for optimizing their diversity; automated and accelerated chemistry; high throughput assay design and detection techniques; and strategies for data analysis and property optimization. Written by experts in the field, both academic and industrial, and illustrated in full colour, this book provides an excellent overview for current practitioners and will also serve as a stimulating resource for future generations. Researchers in organic and medicinal chemistry, biological and pharmacological sciences, as well as those interested in allied computational and engineering disciplines, will value the comprehensive and up-to-date coverage. TOC:Operational Developments in Chemistry: The Use of Polymer-assisted Solution-phase Synthesis and Automation for the High-throughput Preparation of Biologically Active Compounds.- Accelerated Chemistry: Microwave, Sonochemical, and Fluorous Phase Techniques.- Conceptual Advances in Synthesis Prospecting: Design of Discovery Libraries and the Search for Hits: Biosynthesis of "Unnatural" Natural Products.- Combinatorial Synthetic Design: the Balance of Novelty and Familiarity.- Compound Collections: Acquisition, Annotation, and Access.- Chemical Diversity: Definition and Quantification.- Conceptual Advances in Synthesis Mining: Turning a Hit into a Lead: Focused Libraries: the Evolution in Strategy from Large Diversity Libraries to the Focused Library Approach.- Translating Peptides into Small Molecules.- Operational Developments in Screening and High Throughput Assays: High Density Plates, Microarrays, Microfluidics.- Fluorescence Technologies for the Investigation of Chemical Libraries.- The Use of Genetically Engineered Cell-based Assays in in-vitro Drug Discovery.- NMR Based Screening, a Powerful Tool in Fragment-based Drug Discovery.- Screening Chemical Microarrays: Methods and Applications.- Conceptual Advances in Lead Evaluation: Screen Early and Often: Screen/Counter-screen: Early Assessment of Selectivity.- Concepts for in-vitro Profiling - Drug Activity, Selectivity and Liability.- In silico Surrogates for in vivo Properties: Profiling for ADME and Toxicological Behavior.- Use of High Content Screening in Chemical Optimization.- Subject Index.