In India, Bada Gokhru (Pedalium murex L.) stands out as a highly prized traditional medicinal plant, with every part of the neem tree offering valuable medicinal properties ripe for commercial exploitation. Over the past five decades, significant strides have been made in understanding the chemical composition of Pedalium murex compounds, alongside notable advancements in elucidating its diverse biological activities and medicinal uses. Recognized as a rich source of unique natural products, this plant holds promise for the development of pharmaceuticals targeting various diseases and industrial applications. This review provides a comprehensive overview of the biological activities of isolated compounds, pharmacological effects of extracts, clinical research findings, and potential medicinal applications of Gokhru, accompanied by safety assessments.