Deconvoluting how macrocyclization affects the key pharmacological and pharmaceutical properties of kinase inhibitors is hampered by the relative paucity of data that directly compare the properties of macrocyclic compounds with their direct acyclic precursors. This problem is particularly acute when considering ADME properties, as these are often only assessed on later stage leads and thus are rarely reported for acyclic precursor compounds. Despite these limitations, sufficient data is now publicly available to provide some insight into the utility of macrocyclization as an approach to developing inhibitors against protein kinase targets.