ABSTRACT
INTRODUCTION High-throughput screening (HTS) is a scalable methodology for identifying modulators of biological activity from vast libraries of potential modulators through automation and miniaturization. It employs a specialized, highly sensitive biological test system (assay, e.g., a reconstituted protein activity or a cellular system) to measure the specific activity of a biological process in response to perturbations by a library of samples, either chemical compounds or natural product extracts (a compound library), or even libraries of siRNAs. HTS opened a new, broad avenue for pharmacological research (1,2) alongside rational drug design approaches (3-8), and recently, it has been used to search the vast area of chemical, genomic, and biological space for bioactive samples of potential in probing complex biological systems and pathways (9).
