Fungal metabolites are worthily taken into account as a pool of synthetically interesting and remarkably important new lead compounds for medical, agricultural, and chemical industries. Humicola species are known to have biotechnological and industrial potentials. Humicola genus (family Chaetomiaceae) is a prosperous fountainhead of unique and structurally diverse metabolites that have various bioactivities. Moreover, Humicola species attract substantial attention for their marked ability to produce thermostable enzymes with biotechnological and industrial importance. This review highlights the published researches on the isolated metabolites from the genus Humicola and their biological activities as well as the industrial importance of Humicola species. In the current review, more than 50 compounds are described and 84 references are cited.