Mushrooms stand out as one of nature's best gifts among the natural product sources with their diversity, therapeutic values and increasing popularity. In this study, antioxidant (ABTS<sup>·+</sup> scavenging, β-carotene-bleaching, cupric-reducing antioxidant capacity (CUPRAC), DPPH<sup>·</sup> scavenging, and metal chelating assays), and enzyme (buty-rylcholinesterase (BChE) and acetylcholinesterase (AChE), α-amylase and α-glucosidase) inhibition activities of the extracts obtained from <i>Coprinus comatus</i> (O.F. Müll.) Pers., <i>Cerrena unicolor</i> (Bull.) Murrill, <i>Inocutis rheades</i> (Pers.) Fiasson & Niemela and <i>Leptoporus mollis</i> (Pers.) Quél. mushroom species were investigated. The presence of phenolic and organic acid compounds associated with the bioactive properties of the mushroom species was determined by HPLC-DAD. Fumaric acid was found to be prominent compound in <i>C. comatus</i> (43.90 μg/g dw) and <i>C. unicolor</i> (659.9 μg/g dw), vanillin in <i>L. mollis</i> (19.48 μg/g dw), and <i>p</i>-coumaric acid in <i>I. rheades</i> (21.32 μg/g dw). <i>L. mollis</i> methanol extract, as well as higher antioxidant activity than the standards in CUPRAC and β-carotene-bleaching assays, was noted as superior antioxidant active in all assays (except metal chelating). <i>C. comatus</i> possessed the highest inhibition activity on α-amylase (IC<sub>50</sub>: 0.23 mg/mL for methanol extract), AChE (IC<sub>50</sub>: 125.50 μg/mL for hexane extract), and BChE (IC<sub>50</sub>: 61.03 μg/mL for methanol extract). Also, <i>C. comatus</i> methanol (IC<sub>50</sub>: 0.09 mg/mL) and <i>L. mollis</i> hexane (IC<sub>50</sub> : 0.11 mg/ mL) extracts were better α-glucosidase inhibition active than the acarbose (IC<sub>50</sub>: 0.37 mg/mL). Our study ascertained that the studied mushroom species are particularly sources of biochemically active compounds with therapeutic potential.