Chapter 5: Principles and Applications of Fragment-based Drug Discovery for Chemical Probes

Chemical probes are useful tool molecules that allow for interrogation of a given target biomolecule, such as an enzyme or ion channel. Ultimately these tools can be used to ask fundamental questions about the biology surrounding a target and provide early target validation in the drug-discovery process. Fragment-based drug discovery (FBDD) is gaining popularity in the field of chemical probe development owing, in part, to its time- and resource-efficient nature for identifying an initial hit molecule. The following is a collection of reports of the development of chemical probes using a FBDD approach, which highlight its utility in addressing a broad variety of targets.