High‐throughput screening as a tool for agrochemical discovery: automated synthesis, compound input, assay design and process management

High-throughput screening (HTS) is becoming increasingly important within the agrochemical industry as a means of sustaining and improving the flow of novel products to the marketplace. Technology changes within agrochemical research have to some extent followed progress in the pharmaceutical industry in adopting in-vitro-based HTS strategies for lead discovery. However, agrochemical invention faces the unique challenge of combining the opportunities made available by HTS technology with the key advantage of being able to work in the laboratory with real, commercial, whole-organism targets. This paper describes approaches taken within Zeneca to harness these opportunities effectively through development of novel assay procedures for agrochemical discovery. Quality and quantity of chemical input to the HTS process is of paramount importance for the successful discovery of leads. Approaches employing the application of automated chemical synthesis to achieve this aim are reviewed. Adoption of a high-throughput screening strategy requires a fundamental change in areas such as process management, data manipulation and data analysis. Some of our experiences to date in managing these issues are described. © 1998 Society of Chemical Industry