Abstract: Chiral pesticide enantiomers often show different bioactivity in controlling harmful organisms. It is of great significance to pay attention to the selective activity of chiral pesticide enantiomers to promote the reduction and efficiency of pesticides and to develop green agriculture. In this paper, according to the research status of enantioselective activity of chiral pesticides, the research on enantioselective activity mechanism is summarized into two aspects: On the one hand, computer simulation technology is used to analyze the binding ability between enantiomers and active sites of target molecules, and a few of them have also carried out biological experiments; on the other hand, the study explored the differences in absorption, transportation and metabolism of chiral pesticide enantiomers in biological systems by means of radioisotope tracing and quantitative analysis of metabolites. This paper aims to provide reference for the identification of highly active activity chiral pesticide monomers and the development of new green pesticides with high efficiency and low risk.