Combinatorial chemistry is one of the most important methodologies implemented on a wide scale to reduce the time and costs associated with drug development. Automated techniques enable the rapid synthesis of libraries of molecules, large collections of discrete compounds, which can be screened against disease targets. Producing larger and more diverse compound libraries increases the likelihood of discovering a useful drug within the library.

Traditional medicinal development has been described as carefully selecting one bullet at a time and carrying out extensive laboratory experiments to fine-tune the capability of the bullet to hit the target. Combinatorial chemistry is more like shooting thousands of bullets at a target all at once and then looking for the bullets that hit the target.

Combinatorial chemistry may be employed at several points in the discovery process. For example, an early screening of a library may detect molecular shapes that have superior capabilities to bind to a target and inactivate it. One or more of these shapes may be used as a "scaffold" to make further modifications, often using computers to analyze various qualities of a molecule of interest and see how it might be improved. Yet another library may be generated around this new compound or compounds and screened against the target to define even better candidates for testing.

Axys has put in place a combinatorial chemistry infrastructure that employs the most innovative hardware and software to produce diverse compounds in multi-milligram quantities for analysis in the company's high throughput screening facility. The company has created proprietary technologies in chemistry, data handling and software-based components of the technology used both to track the large numbers of compounds made and to analyze them for potential activity in high throughput screening tests.

Axys' Advanced Technologies Division is focusing on commercializing combinatorial chemistry. Axys currently has combinatorial contacts with Pharmacia & Upjohn, Parke-Davis, Rhône-Poulenc Rorer, and Signal Pharmaceuticals. The company intends to build on this success by licensing its combinatorial chemistry technologies to pharmaceutical and biotechnology companies wishing to screen Axys' combinatorial chemistry libraries.