Presentation: P02030

A major aim of optimizing the preclinical drug discovery process is to reduce the attrition rate on INDs entering the clinical phase. A big step forward in this process is to take full advantage of high content screening data, which enables to account for many read-out parameters referring to various biological responses.

In this study a cell-based Endothelin-A-Receptor internalization assay was screened on the EVOscreen® uHTS system, combined with the high-content confocal imaging system Opera™. A multitude of parameters were extracted from the images by the analysis tool Acapella™. Subsequently analyzed with the Genedata Screener® software, the multi-parametric data is used to systematically discriminate process artifacts from reliable signals and to predict mechanisms of action of active compounds. We show how the integration of high-precision measurement, sophisticated image analysis, automated QC, and statistical analysis generates reliable, detailed activity information on complete libraries and permits an early mechanistic classification of compounds.

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