Shuang-Huang-Lian (SHL) is a famous modern formula prepared from three medicinal herbs including Flos Lonicerae, Radix Scutellariae and Fructus Forsythiae. Currently, SHL has been developed a variety of dosage forms due to its proved clinical efficacy. However, the in-depth research on targets and pharmacological mechanisms of SHL preparations was scarce. In the presented study, the bioinformatics approaches were adopted to integrate relevant data and biological information. As a result, a PPI network was built and the common topological parameters were characterized. The reuslts suggested that the PPI network of SHL exhibited a scale-free property and modular architecture. The drug target network of SHL was structured with 21 functional clusters as modules naturally. According to certain modules and pharmacological effects distribution, an anti-tumor effect and protented durg targets were predicted. In conclutions, a bioinformatics approach was established for exploring the drug targets and pharmacological activity distribution. The results offered a novel anti-tumor effect of SHL and provide a clue for further research and development.