Abstract: N-myristoyltransferase (NMT) is present in eukaryotes such as fungi and protozoa. N-myristoylation, a NMT-catalyzed process of protein lipid modification and co-translational modification, plays an important role in such cellular processes as signal cascade transduction, membrane vesicular transport, and protein localization. Research has confirmed the vital importance of NMT for the survival of fungi, parasites, viruses, and tumor cells, making it a promising new target for antifungal, antiparasitic, antiviral, and anticancer interventions. This review summarizes the research progress of small molecule inhibitors targeting NMT, aiming to provide some reference for the development of novel NMT inhibitors.