The successful conversion of natural products (NPs) into lead compounds and novel pharmacophores has
emboldened the researchers to harness the drug discovery process with a lot more enthusiasm. However, forfeit of
bioactive NPs resulting from an overabundance of metabolites and their wide dynamic range have created the bottleneck
in NP researches. Similarly, the existence of multidimensional challenges, including the evaluation of pharmacokinetics,
pharmacodynamics, and safety parameters, has been a concerning issue. Advancement of technology has
brought the evolution of traditional natural product researches into the computer-based assessment exhibiting pretentious
remarks about their efficiency in drug discovery. The early attention to the quality of the NPs may reduce the
attrition rate of drug candidates by parallel assessment of ADMET profiling. This article reviews the status, challenges,
opportunities, and integration of advanced technologies in natural product research. Indeed, emphasis will be
laid on the current and futuristic direction towards the application of newer technologies in early-stage ADMET
profiling of bioactive moieties from the natural sources. It can be expected that combinatorial approaches in ADMET
profiling will fortify the natural product-based drug discovery in the near future.
