Which description best defines a target-centered approach in drug discovery?

• A. Focusing on designing molecules to interact with a known biological target first.
• B. Identifying hits from broad screening before selecting a target.
• C. Relying solely on computer-aided design without any screening.
• D. Using only natural products.

Answer: (A)

A target-centered approach starts by identifying a specific biological target implicated in the disease—such as a receptor, enzyme, or other protein—and then designs or screens molecules to modulate that target’s activity. The emphasis is on a mechanistic goal: find compounds that directly influence the chosen target, and optimize them for potency, selectivity, and favorable pharmacokinetic properties. This path relies on knowledge of how the target works and uses target-specific assays and, often, structure-based design to guide improvements and understand the mechanism of action.

This focus helps reduce off-target effects and supports a more straightforward path to understanding why a compound works, which is helpful for predicting safety and efficacy. In contrast, starting with broad screening to find any hits before deciding on a target is more phenotypic or target-agnostic, not target-driven. Relying only on computer-aided design without empirical screening misses real biological activity, and using only natural products is about the source of compounds, not the strategy for choosing and optimizing a target.