The Macrotyloma uniflorum seed (Horse gram) has been underutilized pulse around the world. Nevertheless, it contains most valuable nutritional and pharmacological phytochemicals. Thus, this research was performed to evaluate the antioxidant, anticancer, and hepatoprotective potential of horse gram methanol extract. Interestingly, methanol extract of horse gram demonstrated dose dependent antioxidant, anticancer, and hepatoprotective activities. Since, at increased (100 mg mL-1) concentration the methanolic extract scavenged the DPPH radical up to 93.5% and reduced the ferric (Fe3+) into ferrous (Fe2+) up to 95%. Similarly, the methanol extract also possess considerable anticancer activities up to 75.64% at 300 mg mL-1 concentration. Furthermore, at increased concentration (300 mg mL-1), the methanol extract effectively protect (hepatoprotective) the HEK293 cells (95.71%), which exposed to 100 mM glucose (hepatotoxicity). The obtained results conclude that the horse gram methanol extract contains pharmacologically valuable phytochemicals and that regular intake of horse gram can be recommended to improve human health