Combinatorial chemistry has become a prominent field due to the rapid technological advancements in chemistry and industrial manufacturing. The production of large numbers of synthetic molecules at surprisingly high rate is possible with combinatorial chemistry. It has played a significant role in materials science for exploration and development of novel materials. This book presents the complex techniques in the most comprehensible and easy to understand language. The aim of this book is to present researches that have transformed this discipline and aided its advancement. It will provide an in-depth knowledge about the discovery and optimization of biologically active compounds, and methodologies widely used in combinatorial chemistry. Those in search of information to further their knowledge will be greatly assisted by this book.