The Benefits of Constructing Leads from Fragment Hits

‘Fragments’ refer to particularly small molecular starting points in medicinal chemistry. The small size of fragments requires adapted techniques for their screening and subsequent elaboration. The detection of the weak binding affinity of fragments for their target, and associated screening issues, have been debated at length. The increasing ability to control and tailor this construction process highlights the potential benefits of fragment-based drug discovery.

This article is published online in Future Medicinal Chemistry and is free to view.