Protein kinases are key regulators of cell function that constitute one of the largest and most functionally diverse gene families, and knowledge of their three-dimensional structure could be of great help in the rational design of specific ligands. However, only about one quarter of human protein kinase structures has been experimentally defined; thus, kinase homology modeling techniques have been widely diffused. In this review, the most recent kinase homology models are reported, together with the most recent approaches and the main validation methods.