Abstract: Sphingosine-1-phosphate (S1P) is an important signaling molecule that regulates multiple biological functions inside and outside cells.It mediates multiple downstream signaling pathways through binding to five G protein-coupled receptor subtypes to produce related physiological functions of cells.In recent years, the study of selective sphingosine-1-phosphate receptor 1 (S1PR1) modulators has become a hot spot in the discovery of therapeutic drugs against immune diseases.This review summarizes the research progress of S1PR1 modulators in recent years, and discusses the structure-activity relationship and the development direction of such modulators.