Propargylamine, due to its distinctive properties, holds significant prominence in medicinal chemistry and chemical biology. Its notable reactivity has long fostered the creation of propargylamine derivatives through diverse synthetic approaches. These strategies have notably eased accessibility to these compounds, enabling extensive exploration of their biomedical capabilities. This comprehensive review delves into and evaluates the diverse applications of propargylamine-derived compounds in drug discovery. It encompasses perspectives from both medicinal chemistry and chemical biology, identifying key therapeutic domains influenced by these compounds. Additionally, it discusses their current influence and burgeoning potential within these fields