用小型的、自動機技術針對靶蛋白、細胞或組織篩選大量化合物文庫以識別潛在新藥。結合基因組學和組合化學，大規模篩選為藥物和生物技術公司識別潛在新藥的能力帶來了革命。大規模篩選有賴于對要識別的靶子的數量和藥物相關分析的發展，然后可以在大量樣本中重復。一般，大規模篩選依賴于96孔板，盡管更高密度的形式也是可能的。最近，小型化和微流體方面的進展允許在一個芯片上每天對一個靶子篩選10萬個化合物，使得從前不可想象的大量化合物篩選成為可能。

The use of miniaturized, robotics-based technology to screen large compound libraries against an isolated target protein, cell or tissue in order to identify binders that may be potential new drugs. In conjunction with genomics (the identification of large numbers of potential therapeutic targets), and combinatorial chemistry (the production of large numbers of medicinally relevant compounds), high-throughput screening has revolutionized the capacity of pharmaceutical and biotechnology companies to identify potential new drugs. High-throughput screening depends on the development of a quantitative, pharmacologically relevant assay for the identified target, which can then be reproduced across a large number of samples. Typically, high-throughput screening has relied on 96-well plates as the standard, although higher-density formats (356, 712) are possible. Recently, advances in miniaturization and microfluidics have allowed screening of up to 100,000 compounds against a target on a single chip daily, allowing previously unimaginable amounts of compounds to be screened.