Chemical genomics is an exciting new field that aims to transform biolo- cal chemistry into a high-throughput industrialized process, much in the same way that molecular biology has been transformed by genomics. The inter- tion of small organic molecules with biological systems (mostly proteins) underpins drug discovery in the pharmaceutical and biotechnology industries, and therefore a volume of laboratory protocols that covers the key aspects of chemical genomics would be of use to biologists and chemists in these orga- zations. Academic scientists have been exploring the functions of proteins using small molecules as probes for many years and therefore would also b- efit from sharing ideas and laboratory procedures. Whatever the organizational backgrounds of the scientists involved, the challenges of extracting the ma- mum human benefit from genome sequencing projects remains considerable, and one where it is increasingly recognized that chemical genomics will play an important part. Chemical Genomics: Reviews and Protocols is divided into two sections, the first being a series of reviews to describe what chemical genomics is about and to set the scene for the protocol chapters. The subject is introduced by Paul Caron, who explains the various flavors of chemical genomics. This is f- lowed by Lutz Weber and Philip Dean who cover the interaction between organic molecules and protein targets from the different perspectives of la- ratory experimentation and in silico design. The protocols begin with the me- ods developed in Christopher Lowes’ laboratory (Roque et al.