Acid sensing ion channels (ASIC) are Na+ channels activated by external protons. Number of neurological (pathological pain, expression of fear, anxiety, depression, and neurodegeneration after ischemic stroke etc) and non -neurological (brain tumor, cardiovascular mechanosensation, hypoxia induced hypertension, glaucoma, etc.) disorders are implica ed by various ASICs subtypes. Due o heir known and potential roles in many disease pathologies, it is very authentic o explore he importance of new and selective small molecule inhibitors and even activators of ASICs as a research tool in clinical uses for treating these diseases pathogenesis. This review is aimed to find out the therapeutic potentialities of ASICs targeted novel drugs in con ex of heir pa hophysiological role in human body. Fluorescent dyes and optical sensors as a means of fast and efficient screening approaches would certainly be used to improve he discovery technology of ASICs modulated drugs.