用小型的、自动机技术针对靶蛋白、细胞或组织筛选大量化合物文库以识别潜在新药。结合基因组学和组合化学，大规模筛选为药物和生物技术公司识别潜在新药的能力带来了革命。大规模筛选有赖于对要识别的靶子的数量和药物相关分析的发展，然后可以在大量样本中重复。一般，大规模筛选依赖于96孔板，尽管更高密度的形式也是可能的。最近，小型化和微流体方面的进展允许在一个芯片上每天对一个靶子筛选10万个化合物，使得从前不可想象的大量化合物筛选成为可能。

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.