Emerging Technologies for Fragment Screening

Abstract

The most established technologies in fragment-based drug discovery (FBDD) in the pharma industry and to some extent in academia are NMR, SPR, and X-ray crystallography. However, there are a number of emerging technologies that hold promise to remedy some of the deficiencies of the more established methods. These methods have now been complemented by other approaches to fragment screening. This chapter covers some new approaches including weak affinity chromatography (WAC), mass spectroscopy (MS), and microscale thermophoresis (MST). Probably the most efficient way to perform fragment screening on a wider scale is to rely on several orthogonal methods working in concert. This will allow the user to evaluate the different aspects of fragment screening and to conclude more firmly the results of a screening campaign. Furthermore, it will give the investigator more choices of qualified hits to work from when developing useful leads.