Which method uses a relatively small number of precursor molecules to generate many compounds?

• A. High-Throughput Screening
• B. Structure-Based Drug Design
• C. Combinatorial Chemistry
• D. Analogues of natural ligands

Answer: (C)

Generating a wide variety of compounds from a small set of starting materials is the hallmark of combinatorial chemistry. By using a limited set of building blocks and combining them in many ways—often with split-and-pool or solid-phase synthesis—libraries containing hundreds to millions of distinct compounds can be created quickly. This broad exploration of chemical space makes it possible to identify promising hits through screening.

High-throughput screening, while it involves testing many compounds, is about the evaluation step rather than how the compounds are made. Structure-based drug design focuses on designing molecules from structural knowledge of the target, not on rapidly generating large libraries. Analogues of natural ligands involve making modifications to a known natural molecule, which tends to produce a smaller, more targeted set of compounds rather than a vast combinatorial library.