Fragment Screening

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Fragment Screening

[/vc_column_text][dt_gap height=”10″][vc_column_text]Fragment screening frequently provides high quality starting points. In several of our projects it succeeded after other methods (including HTS) failed. Thus, fragment screening should be regarded among first-line approaches for hit identification. We have advanced numerous targets from fragments hits (micromolar affinity) through final optimization (nanomolar activity). We do this through focus on:

  • Identifying the most appropriate screening and hit validation assays
  • Identifying the right set of high quality fragments to screen
  • Selecting the best initial hits to advance
  • Efficiently progressing the hits while retaining low lipophilicity, high ligand efficiency and high
    druggability
[/vc_column_text][/vc_column][vc_column width=”1/2″][dt_gap height=”10″][vc_column_text]Fragment-hit[/vc_column_text][vc_column_text]References

  • Albert, JS; Edwards, PD; Identification of high-affinity beta-secretase inhibitors using fragment-based lead generation.  Fragment-Based Drug Discovery, 2008, Wiley (Link)
  • Albert, JS; Blomberg, N; et al. An integrated approach to fragment-based lead generation: philosophy, strategy and case studies from AstraZeneca’ Curr. Top. Med. Chem. 2007, 7, 1600 (Link)
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