Category: Assay Development and Screening

1127-C - Differential Scanning Fluorimetry as a Predictive Tool for Qualitative Assessment of a HTS Project’s Likely Hit Output Prior to Commencement of Screening

Tuesday, February 6, 2018
2:00 PM - 3:00 PM

Differential Scanning Fluorimetry (DSF) has been successfully applied across a number of different activities within early drug discovery. These may range from assessment of protein stability prior to assay development through to buffer scouting for biophysical assays and hit finding in its own right. In this poster we evaluate the ability of the technology to act as a decision making mile stone prior to commencement of high throughput screening (HTS). The hit output from several HTS projects representing a range of target classes and assay technologies were profiled by DSF. We examine how these results compared with the overall assessment of the hit quality from a computational chemistry perspective. From this data we build a case for the early profiling by DSF of actives identified  during a HTS project’s validation stage.  We’ll show how such data can provide a valuable insight and qualitative assessment of a campaign’s likely hit output and the project’s overall chance of success. From this we’ll advocate incorporation of the approach as a standard pre-HTS activity to provide a go/no go decision point prior to the commitment of significant screening resource.

Jarrod Walsh

Senior Research Bio Scientist
AstraZeneca
Macclesfield Cheshire, England, United Kingdom

Graduated in 2000 from the University of Liverpool with a degree in Genetics and joined the High Throughput Screening (HTS)
department of AstraZeneca in 2001. Jarrod’s current role is a Senior Research Scientist within the Global High Throughput
Screening Centre that forms part of AstraZeneca’s Discovery Sciences function. During his 17 years in company Jarrod has
worked extensively with screening applications, assay development activities and biophysical technologies. Since 2012 Jarrod
has focused on devising approaches to identify and eliminate compounds that function via undesirable mechanisms of action to
improve the quality of hit to lead compounds. His work interests include the application of biophysical techniques and
development of new technologies to improve drug discovery screening and hit identification activities.