The techniques highlighted in this volume are introduced with concise theoretical background that prepares the reader for subsequent illustrative examples from the literature. The theoretical and methodological information is rather limited, but the reader is directed to useful references for further reading. This book will be helpful for medicinal, synthetic, and biophysical chemists urveying an array of tools for their specific drug discovery projects, especially to those who do not want to be inundated with theoretical details. Even though most chapters in this book are written in a manner suitable for an audience with intermediate to advance knowledge of biophysics, Chapter1 will pique the interest of beginners in the field, and is a nice introductory reading for medicinal chemistry graduate students, as it provides a historical perspective and overview of biophysical techniques used at various phases of the drug discovery workflow, namely, hit generation, validation, and drug structure optimization.