Module 1: Overview of Strategies and Methods in HTS

This module will introduce the concept of high throughput screening and how screening campaigns are planned and executed. Concepts include the basic goals of screening campaigns and terminology commonly used in the field of HTS. The process of planning and conducting a high throughput screen from the selection, development and validation of assays to the analysis of screening data will be outlined. The elements of a screening laboratory such as assays, robotic tools and chemical collections will also be introduced.

Who would benefit: Scientists new to or learning the field of lead discovery and HTS would benefit from an overview of the HTS process in the context of relevant drug screening examples

Instructor – David Dunn


Module 2: Liquid Handling and Detection Technologies in HTS

This module will present an overview of common detectors used in HTS along with examples of commonly used assays formats and the major technologies used to detect a biological signal. This module will build on the concepts introduced in Module 1 by illustrating the process of validating assays for HTS with some common examples. Common liquid handlers used in HTS will also be presented. The process of determining the accuracy and precision of liquid handlers with emphasis on miniaturized (e.g. 1536-well) systems will also be shown.

Who would benefit: Scientists planning on developing assays for HTS. Scientist interested in liquid handlers and detectors for HTS.

Instructor – Dan Sipes


Module 3: Statistical Considerations in the Optimization and Validation of HTS Assays

This module will illustrate the use of multi-factorial experimental design for simultaneously optimizing multiple assay variables such as incubation time, antibody concentration, etc., to develop an optimal assay protocol in HTS. Its advantages over the commonly used one-factor-at-a-time approach will be illustrated. In addition, some important and fit-for-purpose performance characteristics needed for establishing the suitability of the assay for HTS will be described. If time permits, the use of multivariate computational models for prioritizing compound selection and for assessing the compound testing strategy will be illustrated.

Who would benefit: Scientists interested in learning about the multi-factorial optimization approach, meaningful validation parameters and multivariate correlations.

Instructor – Viswanath Devanarayan


Module 4: Issues in Storage and Management of Compound Collections

A medicinal chemist's view of the major issues residing in HTS data. Properties of DMSO and factors that affect the solubility of compounds as well as the best practices for storage of compounds in DMSO will be discussed. Common mechanisms of chemistry related false positives will also be illustrated.

Who would benefit: Scientists in HTS labs where compound libraries are maintained and arrayed. Scientist using HTS data in their research.

Instructor - Chris Lipinski


Module 5: HTS Case Studies and Lessons Learned

HTS Case studies and lessons learned. This module will show case studies where the principles of assay performance and sensitivity are illustrated. Both cell-based and cell-free systems will be shown. Examples will include case studies that illustrate the process of assay transfer and optimization. As well, the construction and use of databases detailing common assay interferences will be shown.

Who would benefit: Scientist developing both biochemical and cell-based assays for HTS.

Instructor - Doug Auld, Glenn Hofmann, Jeff Weidner, and Thompson Doman