Helicoverpa armigera sterol carrier protein-2 (HaSCP-2) is a validated target for development of novel insecticides due to its divergent protein structure and function from the vertebrate SCP-2. HaSCP-2 is important for normal development and fertility in Helicoverpa armigera (Hübner). The discovery of chemical inhibitors of HaSCP-2 through a structure-based virtual screening is reported here. Bioassay indicated that H1 and H14 had inhibitory effect on the growth of H. armigera larvae. The results suggest that H1 and H14 are promising as useful lead compounds for further optimization and development of novel SCP-2-specific pesticides.