![]() This process, commonly referred to as hit-to-lead, involves a series of chemical modifications to the hit molecules to enhance their potency, selectivity, and other drug-like properties. ![]() The next step is to convert these hits into lead compounds that can potentially become effective drugs. The conventional approach to searching for potential drug candidates involves high-throughput screening, which utilizes automated equipment to rapidly screen vast collections of small molecules to identify potential hits with the desired activity against the target. Apart from inducing the desired biological response, the compound must possess several other vital ‘drug-like’ characteristics, such as non-toxicity, solubility, and stability within the body, to establish its efficacy as a successful drug. Medicinal chemists then embark on a quest to discover a small molecule that can modify the target's activity. The initial step in the process involves biologists identifying a potential drug target, such as an enzyme that has a critical role in a disease. Discovering novel small molecule drugs is a long, iterative process that involves scrutinizing thousands of chemical compounds to identify the most suitable one. ![]()
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