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The present study on Phyllanthus virgatus, known traditionally for its remedial potential, for the first time provides descriptions of the antioxidant and inhibition of α‐amylase enzyme activity first by in vitro analyses, followed by a confirmatory in silico study to create a stronger biochemical rationale. Our results illustrated that P. virgatus methanol extract exhibited strong antioxidant and oxidative DNA damage protective activity than other extracts, which was well correlated with its total phenolic content. In addition, P. virgatus methanol extract strongly inhibited the α‐amylase activity (IC₅₀ 33.20 ± 0.556 μg/mL), in a noncompetitive manner, than acarbose (IC₅₀ 76.88 ± 0.277 μg/mL), which showed competitive inhibition. Moreover, this extract stimulated the glucose uptake activity in 3T3‐L1 cells and also showed a good correlation between antioxidant and α‐amylase activities. The molecular docking studies of the …