Fragment‐Based Ligand Discovery

In this chapter, we have focused on the practical aspects fragment‐based discovery and provided some examples of its successful application. The methods are now firmly established in most pharmaceutical companies, particu- larly as the number of “fragment‐inspired” compounds entering clinical trials has increased [5]. Most of the examples that have been published to date have been of the “conventional” use of fragments, either linking, grow- ing, or merging. However, as the methods become increasingly integrated and adopted by medicinal chem- ists, other attributes of fragment‐based discovery are becoming apparent.