Abstract: Screening of enzyme inhibitors is one of the important approaches for drug development. The three-dimensional structure of enzymes is susceptible to the interference of external factors such as temperature and salt concentration, leading to a decrease in its catalytic activity and stability and increasing the cost of drug screening. Therefore, immobilization through enzyme-carrier interactions to improve the stability of enzyme structure has become an important strategy to maintain the enzyme activity. Screening enzyme inhibitors from complex samples based on immobilized enzymes has also become a hot field of drug research and development. In recent years, metal-organic frameworks (MOFs) are known as the ideal carrier for enzyme immobilization due to their characteristics of adjustable aperture, large surface area, simple structure, stable environment, and so on, and it provides a novel method to achieve the efficient screening of enzyme inhibitors. The method of enzyme immobilization using MOFs as the carrier, the research progress of inhibitor screening and application were summarized. The opportunities and challenges of MOFs enzyme immobilization and drug screening were prospected.