This volume provides reviews of six topics demonstrating the breadth of the field and recent successes in medicinal chemistry. Each of the first five chapters takes an important biochemical target as its theme and provides an insight into current progress in drug design. The last chapter focuses on the vital subject of pharmacokinetics and the great strides that have been made in this discipline during the past decade. All chapters provide an insight into the skills required of the modern medicinal chemist, in particular, the use of an appropriate selection of the wide range of tools now available to solve key scientific problems.