Objectives : We analysed Gyejibongnyeong-hwan's compatibility principle and investigated biological activities by categorizing with molecular level, cellular level, animal level and human level based on Korean study for this formula. Methods : Gyejibongnyeong-hwan's compatibiltity principle was examined by the system of chief, deputy, assistant, and envoy. We looked into studies that presented in Korea from 1956 to 2016 about Gyejibongnyeong-hwan through Korea Institute of Oriental Medicine, Korean medicine information system (OASIS). Then classify into molecular level, cellular level, animal level and human level to analyse. Results : According to the system of chief, deputy, assistant, and envoy, chief herb is Cinnamomi Ramulus, deputy herb is Persicae Semen, assistant herb is Moutan Cortex, Paeoniae Radix, Poria, and envoy herb is Mel. Biological activities can be detected in transcription factors, enzymes, and inflammatory mediators for molecular level. For cellular level, it can be determined in human uterine endometrial cancer cell, human hepatocarcinoma cell, and human platelets. In mouse and rats for animal level, in overian cystoma, menorrhalgia, quality of life improvement in postmenopausal women, and blood stasis with motor vehicle accident for human level, biological activities was caught. Conclusions : From above results, Gyejibongnyeong-hwan is composed in line with the system of chief, deputy, assistan, and envoy. Biological activities are effective to improvement of menorrhalgia, anti-cancer, anti-oxidative, anti-inflammation, improvement of atherosclerosis, analgesic, anti-convulsion, wound healing, and improvement of liver function.