Alexander Alex
Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT 13 9 NJ, United Kingdom
This presentation describes a number of aspects in the hit to lead process in drug design, for example the relationship between biological targets and molecular properties of compounds (lipophilicity, pKa, ligand efficiency), and the distribution of series of compounds and their activity against classes of biological targets and gene families. This approach is underlined by examples of HTS analysis and hit selection as well as library design. In addition, the aspect of utilising screening subsets for enhanced screening efficiency is highlighted and also underlined with examples.