Combinatorial chemistry has not been the panacea for lead compound design that its inventors hoped, as it has turned out that quantity doesn't necessarily equal quality. But that doesn't mean that the search for better lead generation technologies should stop, as the coming deluge of targets would overwhelm conventional medicinal chemistry.

Triad Therapeutics Inc.'s response to the problem is structure-based drug design, using its Integrated Object-Oriented PharmacoEngineering (IOPE) technology to construct focused combinatorial libraries of small molecule inhibitors that are specific for selected gene families. Triad has integrated combinatorial chemistry, structure-based drug design and protein sequence analysis to quickly design enzyme inhibitors that are specific for enzyme family members, taking advantage of the fact that nature uses the same protein domains over and over.