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 t he 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 indust ry in adopting in-vitro-based HTS strategies for lead discovery. However, a grochemical invention faces the unique challenge of combining the opportuni ties made available by HTS technology with the key advantage of being able to work in the laboratory with real, commercial, whole-organism targets. Th is paper describes approaches taken within Zeneca to harness these opportun ities effectively through development of novel assay procedures for agroche mical discovery. Quality and quantity of chemical input to the I-ITS proces s is of paramount importance for the successful discovery of leads. Approac hes employing the application of automated chemical synthesis to achieve th is aim are reviewed. Adoption of a high-throughput screening strategy requi res a fundamental change in areas such as process management, data manipula tion and data analysis. Some of our experiences to date in managing these i ssues are described. (C) 1998 Society of Chemical Industry.