The drug-likeness of a compound is a key factor during the initial phases of drug discovery. It can be defined as the similarity between compounds and drugs. Here, we collate research related to the fraction of sp³ carbon atoms (Fsp³), including related high-throughput screening (HTS) cases, structural modifications based on Fsp³, and strategies to improve it. We also introduce new synthetic methods for spirocyclic scaffolds. It is likely that the reasonable rigidity of spirocyclic scaffolds will provide a new generation of drug candidates.

中文翻译：

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Fsp3：药物相似性的新参数。

化合物的药物相似性是药物发现初始阶段的关键因素。它可以定义为化合物和药物之间的相似性。在这里，我们整理了与sp ³碳原子分数（Fsp ³）相关的研究，包括相关的高通量筛选（HTS）案例、基于Fsp ³的结构修改以及改进策略。我们还介绍了螺环支架的新合成方法。螺环支架的合理刚性很可能会提供新一代的候选药物。