Objective: The study was designed to evaluate the biological and phytochemical potential of Farsetia hamiltonii (Royle), a desert medicinal plant belongs to family Brassicaceae and is traditionally used by residents of Cholistan to treat diabetic, different infectious diseases and gastrointestinal problems. Method: Different biological/enzyme inhibition activities of crude extract of Farsetia hamiltonii were performed first time in this study. The dichloromethane and methanol extracts of aerial part of Farsetia hamiltonii were studied for anti-alphaglucosidase, anti-chymotrypsin, anti-urease, antibutyrylcholinesterase and anti-bacterial activities. The plant was explored first time regarding phytochemical constituents by using the GC-MS technique. Results: The results of crude extracts of Farsetia hamiltonii were significant and provide justification for the traditional therapeutic potential in treating the diabetes, infectious diseases and gastrointestinal problems. Nine (9) compounds were identified by GC-MS technique.