Hit generation is where we aim to identify promising compounds that have the potential to become therapeutic drugs. The term "hit" refers to a chemical compound or biologic that exhibits a specific activity of interest, such as inhibiting a disease-related protein or modulating a biological pathway. For small molecules, this phase involves screening medium (1,000 – 10,000) to large (10,000 – 1,000,000) libraries of compounds, which may include natural products, synthetic chemicals including small fragments, or molecules generated through computational approaches for their biological activity. Once hits are identified, they then undergo further optimisation in the lead generation and lead optimisation phases to enhance their drug-like properties, such as efficacy, selectivity, and safety. The ultimate goal of hit generation is to provide a starting point for the development of a drug candidate that can progress through preclinical and clinical testing. The success of hit generation is crucial for the overall success of the drug discovery process, as it lays the foundation for the subsequent stages of drug discover and development.