Coffee is known to be one of the popular beverages today on the globe. Due to its easy availability and preparation, it is consumed by the population of almost all countries. This wonder crop was discovered in the 6th century in Ethiopia. Since then, people have also used various brewing methods to extract hundreds of the bioactive compounds present in these aromatic seeds. No doubt, excessive consumption of the same can be harmful too. As a functional food, coffee is known to have multiple health benefits. Coffee beans contain vitamins, minerals, caffeine, chlorogenic acid, and various other biologically active ingredients. This review briefly describes the major biologically active compounds present in these seeds – caffeine, trigonelline, diterpenes, and chlorogenic acid (CGA). It also aims to describe various bioactive activities such as antioxidant, antiproliferative, antibacterial, antiviral, etc., against variable hallmarks. Thus, explaining different pharmacological effects for the welfare of the human population.