Using bioactivity profiling to support the progression of phenotypic hits
ABOUT THIS WEBINAR
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. 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 in order to support candidate optimisation.
What you will learn…
In this webinar, you 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. During this webinar, speaker Arsenio Nueda gave an example of a recent case study.
About this case study
In this case study a phenotypic screen was performed using poly I:C / IL-4 stimulated human bronchial epithelial cells interrogated with a 44,974 compound library. This resulted in the identification of 7 representative hits which down regulated TSLP protein and mRNA levels and provided chemistry and biology starting points for new drug discovery opportunities.
Arsenio Nueda, Head of Molecular Biology at Almirall
Arsenio has a PhD in molecular biology, with a 10 year track record in Academia and 18 years experience in the Pharmaceutical Industry, where he has actively strived to introduce phenotypic screening strategies into the current drug discovery toolbox.