Fragment-Based Drug Discovery — Hitting Targets Using the Right Chemistry and Expertise Alliances

Circle Oncodesign Services

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with Dr Thomas Schubert (2bind), Dr Serghei Glinca (CrystalsFirst), Dr Yann Lamotte (Oncodesign Services), Dr Nir London (Weizmann Institute)

Fragment Based Drug Discovery (FBDD) has become of increasing importance and interest in the past decade for hit finding and optimization. FBDD led to approved therapeutics and numerous drug candidates. It has empowered the industry to address targets that had previously been deemed “undruggable”.

FBDD uses the advantages of biophysical, biostructural and biochemical methods for the detection of low molecular weight molecules, so-called “fragments”, that bind to a target. FBDD exhibits several advantages over high-throughput screening campaigns in terms of cost, chemical diversity, and broader sampling for potential follow-up compounds.

Numerous case studies of covalent and non-covalent screening fragment strategies have led to successful applications in druggability assessment of protein. In this talk, experts in the field of FBDD will present case studies and potential of a spectrum of cutting-edge strategies for a successful hit identification and optimization campaigns.

In addition, Dr Nir London (Weizmann Institute of Science, Israel) will present how electrophilic fragment screening can accelerate the discovery of a new generation of covalent probes for challenging targets. Here he will describe application of this method for the discovery of the first in-vivo active chemical probe for the proline isomerase Pin1, as well as against the SARS-CoV-2 main protease.