Modern drug design and discovery is an increasingly complex process, where a wide range of actors with many different backgrounds work together toward the unifying goal of developing drugs. Their success is highly dependent on insights and advances from the combined use of particularly chemical and biological research, and it is clearly important to have the worlds of chemistry and biology to work in a concerted effort. Similarly, research at academic institutions is becoming increasingly interdisciplinary, which is driven by the increasing complexity that modern research is facing. Multi- or interdisciplinary research disciplines are having a growing impact and boundaries between traditional natural sciences are vanishing. Chemical biology is just one example of such a cross-disciplinary science; others include nanosciences and systems biology, which encompass research from physics, chemistry, biology, and computer sciences.

Chemical biology is a contemporary scientific discipline that integrates biomedical sciences such as chemistry, pharmacology, biochemistry, biophysics, and molecular biology. Chemical biology is generally defined as the application of chemical approaches to study biological problems. In other words, chemical biology is the scientific discipline for chemists who are applying the principles, language, and tools of chemistry to biological systems and for biologists who are interested in understanding biological processes at the molecular level. Although research in chemical biology is characterized by encompassing a very broad range of both chemical and biological approaches, it can generally be classified into two main classes of research:

1. Applying small molecules to perturb biomacromolecules

2. Modifying biomacromolecules by chemical methods, and employing such molecules to probe biological activity

The application of small molecules in biological studies started with the isolation of individual natural products, and is one of the cornerstones of traditional medicinal chemistry. In the chemical biology context the application of small molecules is called chemical genetics, where small molecules are used in a systematic manner to probe biology. Although there is no strict definition of a small molecule, it is generally a small organic molecule, with a molecular weight between 300 and 700 Da and it is not a biomacromolecule. The modification of biomacromol-ecules (proteins, nucleic acids, and polysaccharides) has emerged as a result of primarily two things: the understanding of biological systems is reaching a level, where much more detailed studies are required and at the same time a range of chemically inspired techniques have developed to modify and study biomacromolecules, which in some cases has surpassed traditional genetic methodologies.

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