Elucidation and characterisation of high throughput degrader screening outputs
Poster
8
Elucidation and characterisation of high throughput degrader screening outputs
Authors
L Bell1; G Davies1; G Holdgate1; J Kastl1; M Packer1; 1 Hit Discovery, Discovery Sciences, BioPharmaceuticals R&D, AstraZeneca, Alderley Park, UK
Abstract
Targeted protein degradation is an important function of the cellular machinery that is gaining momentum as an exploitable strategy for drug discovery. Molecules that are able to induce proximity between intractable therapeutic targets and the proteasomal degradation machinery are slowly changing the druggable target landscape. Having the ability to detect and understand the mechanism of action of hit molecules identified from a direct screen for degraders is becoming increasingly attractive. We have established a post-HTS cascade of experiments including cell-based assays as well as orthogonal triage steps to provide annotation on the selectivity and mechanism of action for primary screening hits against a high value oncology target. We will describe our current position on the analysis of these novel outputs and highlight challenges encountered.
The European Laboratory Research & Innovation Group
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