Smart screening: approaches to efficient HTS

Faced with the prospect of a rising number of potential drug targets and given almost unlimited access to internal and external chemistry resources, the 'brute-force' approach to high-throughput screening (HTS) is becoming increasingly unattractive. Pharmaceutical companies realize that they have both to increase the scope of screening experiments and improve on the efficiency of the screening process per se. In acknowledging this development, hybrid screening strategies have been suggested that unite in silico and in vitro screening in one integrated process. The partnering of both screening approaches in one process is believed to exploit the potential of HTS in much smarter and more cost-efficient ways. This review will describe some recent applications of this new screening paradigm and discuss the impact of integrating these novel strategies in the drug discovery process.