Kinetic target-guided synthesis (KTGS) is a promising tool for the discovery of biologically active compounds. It relies on the identification of potent ligands that are covalently assembled by the biological targets themselves from a pool of reagents. Significant effort is devoted to developing new KTGS strategies; however, only a handful of biocompatible reactions are available, which may be insufficient to meet the specificities (stability, dynamics, active site topology, etc.) of a wide range of biological targets with therapeutic potential. This Topical Review proposes a retrospective analysis of existing KTGS ligation tools, in terms of their kinetics and analogy with other biocompatible reactions, and provides new clues to expand the KTGS toolkit. By way of examples, a nonexhaustive selection of such chemical ligation tools belonging to different classes of reactions as promising candidate reactions for KTGS are suggested.

中文翻译：

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量身定制的生物正交和生物共轭化学：开发动力学靶标引导合成策略的灵感来源

动力学靶标引导合成 (KTGS) 是发现生物活性化合物的有前途的工具。它依赖于从试剂池中识别由生物靶标本身共价组装的有效配体。致力于开发新的 KTGS 战略；然而，只有少数生物相容性反应可用，这可能不足以满足具有治疗潜力的广泛生物靶点的特异性（稳定性、动力学、活性位点拓扑等）。本专题评论建议对现有 KTGS 连接工具的动力学和与其他生物相容性反应的类比进行回顾性分析，并为扩展 KTGS 工具包提供新线索。举例来说，