Abstract: Oncogenic B-Raf has been identified in a variety of cancers with high incidence, especially in malignant melanoma and thyroid cancer. In 2011, selective B-Raf kinase inhibitor vemurafenib was approved by FDA, and that stimulated increasing interest in B-Raf inhibitors as anticancer agents. Through analyzing the X-ray crystal structure of vemurafenib bound to B-Raf kinase, new classification of B-Raf kinase inhibitors was proposed. This review focuses on diverse small-molecule inhibitors of B-Raf kinase published in protein data bank(PDB)from 2011 to date based on the new classification. The binding modes and structure-activity relationship(SAR)as well as the future development of these inhibitors are discussed.