Daniela Gabriel

TL;DR: The preclinical data show that NVP-BEZ235 is a potent dual PI3K/mTOR modulator with favorable pharmaceutical properties, and the compound was well tolerated, displayed disease stasis when administered orally, and enhanced the efficacy of other anticancer agents when used in in vivo combination studies.

TL;DR: A study comparing five different cAMP detection technologies in terms of sensitivity, robustness, and feasibility for HTS found DELFIA had the highest sensitivity, whereas ALPHAScreen and HTRF shared several advantages, including high sensitivity, broad dynamic range, and minimal reagent addition steps.

TL;DR: This report suggests an extension of the Z' factor, which integrates multiple readouts for assay quality assessment using linear projections, which is applicable during assay development, to optimize the image analysis, as well as during screening to monitor assay robustness.

TL;DR: An HCS-based profiling panel that serves as basis for characterizing the mode of action of compounds and was able to identify novel compound-target associations for selected compounds such as a submicromolar inhibitory activity of Silmitasertib on PI3K and mTOR.

TL;DR: This report presents examples of how simple steps can be applied to enhance the quality of TR-FRET screening campaigns, and recommends recording and visualization of differences in the donor/acceptor fluorescence, which allows the identification of compound artifacts.