Abstract: Chemogenomics/chemical genomics has been widely used in novel drug research and discovery. Firstly, the concept of chemogenomics was introduced briefly. Secondly, we reviewed the progress of novel drug research and discovery based on forward chemogenomics, reverse chemogenomics and predictive chemogenomics. Finally, we showed progress of the research that chemogenomics has been used to novel drug research and discovery in pharmaceuticals companies.