Graphene based nanomaterials (GBN) have been recently applied in a broad range of science and technology fields such as nanobiomedicine, electronics, energy storage and power generation exploiting their unique electronic structure, physical properties, and opportunities for modifying their surface using covalent and non-covalent interactions. In the present review we systematised the origins of GBN functionalisation using organic and inorganic molecules, polymers, biomolecules, and anticancer drugs. We show that varying the procedure of GBN functionalisation allows to obtain nanomaterials with desired properties that can be applied to the development of materials with enhanced physicochemical properties, nanoplatforms for drug delivery, nanobiosensors for detection of various biomolecules, as well as nanomaterials for bioimaging and diagnostics. The review can be useful for experts in the fields of material science and nanobiomedicine.