Fragment Screening

Fragment based screening is an important technique used in biophysics for understanding biomolecular interactions. Evotec has a wealth of experience and a proven track record in fragment based screening.

Evotec implemented fragment screening more than 15 years ago including biophysical, biochemical, crystallographic fragment screening approaches. NMR- and SPR-technologies are mainly applied for biophysical fragment screening. Currently, Evotec is expanding the fragment screening approach to GCI-technology. To date, Evotec has conducted more than 60 biophysical fragment screening campaigns.

Evotec can offer two fragment screening library sets:

• 3k fragment set with fragments showing a mean molecular weight of 200 Da and is applied for NMR-, SPR-, and GCI-based screening
• 20k fragment set containing so-called “decorated fragments” with a mean molecular weight of 250 Da - this fragment set is applied for SPR-based screening

Case studies applying Evotec’s biophysical fragment screening workflows have been published with collaborating partners:

Fragment screening of GPCRs using Grating Coupled Interferometry (GCI) technology 

Ligandability assessment of the C‐terminal Rel‐homology domain of NFAT1

Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS–SOS1 interaction

Fragment-based discovery of DNA gyrase inhibitors targeting the ATPase subunit of GyrB

Novel MK2 Inhibitors by fragment screening