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Supporting the progression of phenotypic hits with bioactivity profiling

Posted: 4 June 2018 | | No comments yet

Bioactivity profiling has been traditionally used to assess the selectivity of new drug candidates in the context of target-based approaches, where pharmacological selectivity is a key requirement.

DNA and chromosomes

This webinar, with Eurofins Pharma Discovery Services, takes place on 28 June 2018 at 3:00PM (BST) and focuses on the use of bioactivity profiling to support the progression of phenotypic hits.

Phenotypic screening provides hit molecules where the only initial constrain is activity in a functional assay, without placing any limitation on the starting selectivity. Subsequent progression of these hits requires bioactivity profiling tools to pin-point relevant and not-relevant activities to support candidate optimisation.

What delegates will learn from this webinar

In this webinar, delegates will learn how to address the optimisation of hits derived from a target-agnostic phenotypic screen, using a strategy based on combining bioactivity profiling and reference compound characterisation. Keynote speaker Arsenio Nueda, Head of Molecular Biology at Almirall, will give an example of a recent case study featuring bioactivity profiling to support the progression of phenotypic hits.

Webinar case study

The webinar case study, to be presented by Arsenio Nueda, will feature a phenotypic screen that was performed using poly I:C / IL-4stimulated human bronchial epithelial cells interrogated with a 44,974 compound library. This resulted in the identification of seven representative hits, which downregulated thymic stromal lymphopoietin (TSLP) protein and Messenger RNA (mRNA) levels and provided chemistry and biology starting points for new drug discovery opportunities.

About the keynote speaker

Arsenio Nueda, Head of Molecular Biology at Almirall, has a PhD in molecular biology, with a 10-year track record in academia and 18 years’ experience in the pharmaceutical industry. Arsenio Nueda actively strived to introduce phenotypic screening strategies into the current drug discovery toolbox.

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