Abstract
High throughput screening towards chemical libraries is the primary way to discover lead compounds in developing innovative drugs, especially new molecular entities. Accordingly, the preparation of chemical libraries is the key step for drug development. Now, conventional small molecule chemical libraries and DNA‐encoded chemical libraries are the main models of chemical libraries for high‐throughput screening. Recently, a new model of chemical library, called modular click chemistry library, was proposed, which gives us an alternative choice to construct chemical libraries for high throughput screening and exhibits broad prospects to accelerate drug development. Herein, this article mainly focuses on the strategy to prepare the modular click chemistry library.
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