High-throughput screening (HTS) has achieved widespread popularity over the last two to three decades in drug discovery. Characterized by its simplicity, rapidness, low cost, and high efficiency, HTS can minimize the time span of drug discovery noticeably. Robotic technologies and analytic technologies are two central components of HTS, and significant progress of the technologies has been reported recently. In addition, microfluidics has emerged as a promising technology in HTS with eligible potential. Lastly, although automated synthesis is not generally seen as a part of HTS, there is a great desire for the development of high throughput synthesis to generate compound libraries and its integration into HTS. Herein the most recent advancements in the four above mentioned fields are reviewed.