In vitro screening of medicinal active ingredients is a course for undergraduates of Shenyang Pharmaceutical University. Through the study of the course, students can master the basic theories, knowledge and methods of active screening, deeply understand the application of active screening in the process of drug research and development so as to cultivate their rigorous scientific attitude and a meticulous learning style for their future studies and careers in pharmacy. The course adheres to the teaching philosophy of “student-centered, research-study integration, and continuous improvement”, and innovates the teaching model to shift from knowledge transfer to competency development. By constructing a hierarchical teaching mode of “asking questions in each class-theoretical learning-deepening understanding with practical tools, videos and cartoons- recording related videos with group cooperation”, the organic integration of knowledge, ability and quality is realized, and the innovative thinking and teamwork ability of students are cultivated. The teaching process, combined with online platforms such as Chaoxing Xuexi Tong, reshapes the course’s teaching model, builds a new course assessment system, further improves the teaching quality and offers significant potential for widespread implementation.