The completion of the Human Genome Project defined new challenges in biomedical research. One such challenge is the interface between Chemistry and Biology, formulated as Chemical Biology. With epigenetics coming into forefront as the mechanism of inheritance without the change in the DNA sequence and the emergence of the epigenome as the state of the cell controlled by epigenetic processes, the need for intervention in these processes by using small molecules became of major importance. The goals of a training environment in Chemical Biology are to create opportunities for chemists to develop expertise in biology and for biologists to receive a fundamental education in chemistry. In the CBI Training Program students are educated and trained to discover new synthetic compounds with the capacity to modulate the function of selected biological systems. The trainees gain a thorough understanding of the biological systems that are modulated by the small molecules. They are trained to investigate the molecular basis for the interaction of small molecules with the biological target using structural, computational and biological approaches. They utilize their understanding of molecular recognition to redesign and synthesize molecules with potentially improved biological properties. Finally, they explore the effect of the newly developed molecules on molecular and cellular processes with the overall goal of developing new therapeutic approaches. The training at the biology - chemistry interface endows the new scientists with the theoretical and practical underpinnings to examine new research directions that encompass the fields of chemical biology, experimental therapeutics and translational research.