The coprinoid mushrooms or coprini are species of former genus Coprinus Pers. (Coprinaceae, Agaricomycetes) currently divided into four new genera: Coprinus, Coprinopsis, Coprinellus, and Parasola. The presented review addresses literature data and findings from our recent observations on bioactive compounds (sesquiterpenes, proteins, lectins, phenolics, polysaccharides, fatty acids, etc.) and enzymes (proteases) of 21 coprinoid species distributed in Armenia possessing medicinal properties (antitumor, antibacterial, antifungal, antioxidant, mitogenic, antiprotozoal, hypoglycemic, and others) with potential biotechnological interest.