High throughput physicochemical profiling for drug discovery

The drug development bottlenecks of attrition and development time are bein g addressed by acquiring a profile of the candidate's physicochemical and p hysiological properties during early discovery phases. This information ass ists selection and optimization of pharmaceutical properties in parallel wi th activity. High throughput methods to measure the properties: solubility, permeability, lipophilicity, pKa, stability and integrity are described an d compared in this article. The underlying discovery requirements, needs an d application strategies are discussed. (C) 2001 Wiley-Liss, Inc. and the A merican Pharmaceutical Association.