MCs have also found applications as drugs against conventionally druggable targets, which do not necessarily require special "beyond Ro5" chemotypes. This observation raises the question of why a macrocycle strategy was employed in these instances, given that the medicinal chemistry of MCs is typically more complex and laborious than that of non-macrocyclic compounds. In some cases, the motivation could simply be the desire to establish new chemical matter for patent reasons. But it is important to ask whether macrocyclization can also confer significant pharmacological and pharmaceutical benefits, even when applied to conventionally druggable targets. Here, we address this question, using kinase inhibitors as an example of a readily druggable target class for which multiple macrocyclic drugs and clinical candidates have been reported.