Drug discovery is a dynamic and vital process aimed at developing new therapeutic compounds to address unmet medical needs. This chapter provides an overview of the evolving landscape, tracing the journey from traditional medicinal practices to modern scientific approaches. Key methods include ethnopharmacology, natural product screening, serendipitous discoveries, and the synthesis of compound derivatives for pharmacological testing. With advances in technology, the field now relies on high-throughput screening (HTS), along with omics-based approaches such as genomics, proteomics, and metabolomics. In silico methods, including computer-aided drug design and the integration of artificial intelligence (AI) and machine learning (ML), are revolutionizing how potential drug candidates are identified and optimized. Additionally, chromatographic techniques play a crucial role in the rapid and efficient screening of bioactive metabolites. Together, these tools and strategies represent a comprehensive, multidisciplinary framework that continues to drive innovation in modern drug discovery.