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As the first histone acetyltransferase to be cloned and identified in yeast, general control non-depressible 5 (GCN5) plays a crucial role in epigenetic and chromatin modifications. It has been extensively studied for its essential role in regulating and causing various diseases. There is mounting evidence to suggest that GCN5 plays an emerging role in human diseases and its therapeutic potential is promising. In this paper, we begin by providing an introduction GCN5 including its structure, catalytic mechanism, and regulation, followed by a review of the current research progress on the role of GCN5 in regulating various diseases, such as cancer, diabetes, osteoporosis. Thus, we delve into the various aspects of GCN5 inhibitors, including their types, characteristics, means of discovery, activities, and limitations from a medicinal chemistry perspective. Our analysis highlights the importance of identifying and creating inhibitors that are both highly selective and effective inhibitors, for the future development of novel therapeutic agents aimed at treating GCN5-related diseases. [Display omitted] • Introduce structure, catalytic mechanism, and regulation of GCN5. • GCN5 modulating the acetylation levels of histones, non-histones and numerous transcription factors. • Systematic reviewing GCN5 inhibitors from a medicinal chemistry perspective. • The current challenges and future perspectives of GCN5 inhibitors. • Regulating GCN5 actions can be a promising treatments on some human diseases. [ABSTRACT FROM AUTHOR]