European ScreeningPort, Hamburg, Germany
5th HTRF Symposium, Avignon, France
The sequencing of the human genome has led to the identification of a large number of protein targets for therapeutic intervention. Subsequently, significant effort has been expended by "industry" to design and develop both simple biochemical and phenotypic cell based assays for a range of these targets for use in High Throughput Screening (HTS) campaigns against small molecule libraries. Although the outputs of many of these HTS campaigns are small molecules that act upon the target in the assay format chosen for the HTS, their activities all too often do not translate when investigated in an in vivo setting. It is noteworthy that there has been an increase in drug discovery activities outside industry. We have been actively engaged in assisting academic drug discovery efforts and will present case studies for a range of target classes demonstrating that the choice of biological reagent and the assay format itself will have a significant bearing upon the types of small molecules that are identified as actives in HTS campaigns. Particular focus will paid to how the combined capabilities of "academia" and "industry" can allow the development of innovative, physiologically relevant biological reagents for developing appropriately miniaturized assays that will conserve the consumption of precious biological reagents without compromising data quality in HTS campaigns. The ultimate aim being that the use of appropriate biological reagents and assays in HTS campaigns will increase the probability that the activities of the small molecules that are identified can be translated into therapeutic agents.