In the last two decades, the role of physicochemical parameters has come to the forefront of early stage
drug discovery. The primary driver behind this revolution is the fact that the pharmacokinetic properties of hit
and lead compounds have become worse and worse. In this chapter, the theoretical background and measurement
techniques for the more important physicochemical parameters are introduced from the perspective of the
ADME/T processes. Finally, during the last decade a number of significant ADME/T-physicochemical-based
structure relationships have been shown to be relevant.
