ABSTRACT
INTRODUCTION Drug discovery is a process by which drugs are designed and discovered through therapeutic target identification, efficacious assay development, identification of leads, lead optimization by synthesis, preclinical characterization, and drug safety assessment. The goal of drug discovery is to discover and develop safe and efficacious medicines for unmet medical needs. High-throughput screening (HTS) is an essential drug discovery strategy for biotechnology and pharmaceutical industries to find new leads that eventually will be developed into new drugs. HTS is an Enabling Technology for Drug Discovery and Biomedical Research. The goal of HTS is to accelerate drug discovery that relies on sound and best signal detection technologies. The preferred assay technologies therefore use homogeneous biochemical and cell-based assay formats that are adaptable for high-density microplate assays and automation. Advances in the assay technologies and instrument technologies are making it possible for the drug discovery marching towards ultra-HTS to keep pace with increasing demand to screen more targets in shorter time. Through this process one can rapidly identify active compounds or genes, which modulate a particular biomolecular pathway. The results provide starting points for drug lead discovery and design.
