Kinase enzymes are a family of approximately 540 members that perform many important functions in metabolism and have therefore been identified as playing a role in the formation and development of disease. Studies conducted since these enzymes were identified as drug targets have shown that, despite the difficulties of target-oriented drug development, successful therapeutic agents can be produced. A review of current drug research reveals that mono- or combination therapy agents, particularly small molecule inhibitors, can improve quality of life and lifespan and, in some cases, prevent recurrence of the disease or the emergence of other comorbidities. Despite the clarification of the genetic map of kinases, the biochemical mechanisms involved, ranging from signal transmission to metabolic functions, remain poorly understood, which is still considered one of the most significant challenges in drug research. With the advancement of technology, the rapid and effective implementation of modeling and many other experimental methods is expected to lead to the development of more targeted kinase inhibitors in the near future, thereby providing more effective therapeutic options for clinical use.