This book is a practical guide for those engaged in small-molecule combinatorial chemistry as well as those wishing to learn the field. Aimed at nonspecialists, the chapters are written in a tutorial style by internationally recognized experts. The text reviews the use of computational tools to analyse molecular diversity and presents a detailed survey of solid-phase peptide synthesis and the tools used for small-molecule synthesis. Up-to-date automated approaches and equipment for synthesizing solid- and solution-phase libraries are reviewed, including synthesis, analytical, and deconvolution tools. This book will be useful to medicinal chemists, organic chemists, biochemists engaged in high-throughput screening, materials scientists, patent professionals, and science writers.