Final answer:
Fragment-based lead discovery (FBLD) is a technique in drug discovery that starts with screening small chemical fragments to find those that weakly bind to biological targets and uses these as a base for developing potent compounds through optimization.
Step-by-step explanation:
Fragment-Based Lead Discovery
Fragment-based lead discovery (FBLD) is a method used in medicinal chemistry to identify lead compounds in drug discovery. This technique involves screening small chemical fragments, which bind with weak affinity to biological targets. These fragments serve as starting points to develop more potent compounds. Compared to high-throughput screening (HTS) of large molecules, FBLD allows for the exploration of chemical space with a smaller number of molecules. The process involves several steps, starting with fragment screening, using techniques like X-ray crystallography, NMR spectroscopy, or surface plasmon resonance to identify binding interactions. After identifying the promising fragments, medicinal chemists will then optimize these fragments to enhance their binding affinity and pharmacological properties. This optimization often involves growing the fragments or merging them, based on the detailed understanding of their interaction with the target.