In the past 5 years the world of high-throughput screening (HTS), which targets lead discovery for both pharmaceutical and agrochemical applications, is in a highly rapid developmental stage. Today, restructuring the drug discovery programs to develop highest performance is a key issue of pharmaceutical companies. In an increasingly competitive environment prioritizing innovation has become of major strategic importance. Driving forces are the pressure to discover more innovative and even better drugs, as well as time to market. Driven by technological innovation the hybrid “science” HTS [1, 2] depends on and merges latest developments in molecular biology, chemistry, pharmacology, laboratory automation, bioinformatics, and computing to meet “economics,” “big numbers,” “high speed,” and “high information content” necessary for the discovery of new and innovative drugs.