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The need to combat human, agronomic and veterinary diseases or pests has sustained research interests directed at finding new medications from under-exploited biodiversity. The adoption of bioassay techniques, which correlate with prevention, inhibition and reversal of diseases or elimination of pests in screening natural products for bioactive compounds, is critical to the discovery of new medications. This study focuses on the chemistry and biological activity of fungal (including endophytes and soil fungi) secondary metabolites that connect academia with industry. It discusses the technical skills needed to find biologically active compounds from fungi.