Lichens are a rich source of diverse secondary metabolites, with depsides playing a crucial role in their biological properties. Atranorin, a prominent depside, has been widely studied due to its significant pharmacological effects. This review explores the biosynthesis of atranorin, elucidates its molecular structure, and presents insights from docking studies that reveal its interactions with key biological targets. Furthermore, the diverse biological effects of atranorin including anti-cancer, anti-inflammatory, antiviral, antioxidant, and antifungal activities are discussed. These findings highlight atranorin's broad therapeutic potential, making it a promising candidate for drug development.