Traumatic injuries to the nervous system often lead to a permanent and irreversible general functional deficit affecting the survivor’s quality of life. Currently, there is no effective treatment to restore the catastrophic loss of functions. Our team aims to identify novel bioactive small molecules that can improve the functional outcomes in patients with nervous system injuries. We successfully identified two FDA-approved drugs and one bioactive small molecule that can promote sensory and motor functional restoration after nervous system injuries. Ultimately, we believe the development of these drugs will address unmet clinical demand to restore functional deficits in patients at an affordable price.