Chemical genomics aims to use small molecules to probe phenotypic and genetic variations. Specifically, experimental design in chemical genomic screening takes into account genetic and genomic differences in identifying cellular reactions to small molecules. Furthermore, this approach provides a temporary control over cellular states not achieved normally by molecular biology methods. Very recently we have started and expanded successfully programs to evaluate target- and diversity-driven synthetic approaches to provide small molecules. This focus furnishes vehicles to study biological interactions, which we envision as one of the main goals of our scientific work.