Recent Trends and Observations in the Design of High Quality Screening Collections

The design of a high quality screening collection is of utmost importance for the early drug discovery process and provides in combination with high quality assay systems the foundation of future discoveries. Herein, we review recent trends and observations to successfully expand the access to bioactive chemical space, including: the feedback from hit assessment interviews of HTS (High-Throughput Screening) campaigns; recent successes with chemogenomics target family approaches; the identification of new relevant target/domain families; DOS (Diversity Oriented Synthesis) and new emerging compound classes; and non-classical approaches, like FBS (Fragment-based screening) and DELs (DNA encoded chemical libraries). The role of in silico library design approaches is emphasized