Drug discovery is a complex, multistep process, in which many challenges need to be overcome at each stage, from the discovery of a biomolecular target to the ensuring of the efficacy and safety of a compound in humans. Today's analytical methods allow tens of thousands of drug candidates to be screened for their ability to inhibit specific enzymes and the miniaturization of these approaches is highly desirable, accelerating the drug discovery process and reducing the associated costs. Herein, it is reviewed the miniaturized techniques currently used to evaluate enzymatic activity and inhibition giving special attention to microplate formats, microarrays, nanoarrays, and microfluidic technologies. It is, also, highlighted some of the characteristics and their abilities for potential uses are compared and discussed. In addition, the challenges of their applications in diagnosis, analysis, and therapy, which should help to improve the quality of healthcare globally are also pointed out.

药物发现是一个复杂的多步骤过程，从发现生物分子靶点到确保化合物在人体内的效力和安全性，每个阶段都需要克服许多挑战。当今的分析方法可以筛选成千上万的候选药物抑制特定酶的能力，因此，迫切需要这些方法的小型化，从而加快药物开发过程并降低相关成本。本文中，综述了目前用于评估酶活性和抑制作用的小型化技术，特别关注微孔板形式，微阵列，纳米阵列和微流体技术。还强调并比较了一些特征及其潜在用途的能力。此外，