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Automation of the assay development phase of drug discovery

12/98

Presentation:  Automation of the assay
development phase of drug discovery


Damien Dunnington (1), Anthony Lozada (1), Hsiu-Yu Tseng (1), Paul Taylor (2) and
Frances Stewart (2)

1. Hoechst Marion Roussel, Route 202-206, Bridgewater NJ 08807

2. SmithKline Beecham Pharmaceuticals, 709 Swedeland Road, King of Prussia PA 19406



The early phase of drug discovery, beginning with information and ending with lead
compounds, has been re-engineered in recent years to accommodate advances in combinatorial
chemistry and genomics. However, the reengineering has not been uniform and a
disproportionate effort has been devoted to the screening phase, with relatively little
attention to the assay development and hit follow-up stages where substantial bottlenecks
persist. As new technologies such as miniaturization and fluorescence are introduced, the
gap between an assay conceived by a disease group and the requirements for automated high
throughput screening is becoming ever wider. The assay development and reformatting
bottleneck has inspired an automated approach toward streamlining and ultimately
eliminating this problem. This approach combines established design-of-experiments
techniques with robotics and interfacing software, with the ultimate goal of assay
configuration in a virtual lab environment and direct interfacing with robotics for
execution. Examples will be presented to illustrate the impact of these approaches on
assay configuration, robustness and hit detection, and progress toward a fully automated
process will be discussed.

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