Advances in combinatorial chemistry and high-throughput screening continue to introduce poorly water-soluble active ingredient (API) chemistries into pharmaceutical development. For more than 25 years, high-throughput chemistries and techniques have driven a dramatic increase in the number of poorly water-soluble drug candidates in development. Anshul Gupte at Metrics Contract Services discusses how pharmacologists are now better able to successfully synthesize more potential candidate compounds and efficiently optimize drug-receptor binding to achieve better selectivity.