Assay Development and Screening

Application of a robustness set to guide the development of 1536-well format assays for HTS

Tuesday, February 6
4:00 PM - 4:30 PM
Location: 6C

High Throughput Screening is susceptible to pick up compounds that show activity across a range of assay platforms and against a range of proteins, so called frequent hitters. The most common causes of frequent hitters are metal chelation, chemical aggregation, redox activity, compound fluorescence, cysteine oxidation or promiscuous binding. By changing assay conditions the effect of some of these liabilities can be minimized.
For this purpose, a robustness set was developed to evaluate an assay prior to screening on the likelihood of picking up frequent hitters. The robustness set consists of a 1536-well plate containing eight types of compounds based on their chemical/physical properties: Aggregators, Chelators, Coloured, Fluorescent, Luciferase, Reactive, Redox and Clean compounds, all dissolved in DMSO.
A statistical workflow was developed to analyse the results of the robustness set in a standardized manner.
Examples will be shown on how the application of the robustness set has helped to select the optimal assay conditions for screening and how it has helped to design an efficient hit-triaging cascade to deselect artefacts from the primary screen.

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Steven van Helden

Chief Technology Officer
Pivot Park Screening Centre B.V.

Steven van Helden studied chemistry at Utrecht University and, after obtaining his Ph.D. , worked in various roles in pharmaceutical industry for 20 years. Since 2003 he has been responsible for High Throughput Screening (HTS) operations and strategy at Organon/MSD. After the closure of those research facilities he developed a business plan for continuation of the screening activities in Oss, The Netherlands. This led to the formation of the Pivot Park Screening Centre (PPSC) and a central role of this company in the European Lead Factory. Steven is now Chief Technology Officer at PPSC.

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Application of a robustness set to guide the development of 1536-well format assays for HTS



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