'kinase-activating' originates from Modern English, formed from 'kinase' (from Greek 'kinein' meaning 'to move' combined with the enzyme suffix '-ase' via New Latin/French usage) and 'activating' (from Latin 'activus' / Late Latin 'activare' meaning 'to make active').

'kinase-activating' developed in 20th-century biomedical writing as a compound combining 'kinase' (a term coined for enzymes that transfer phosphate groups) and the present participle 'activating'; it emerged from phrases like 'kinase activator' and 'activation of kinase' into the concise adjectival form 'kinase-activating'.

Initially, 'kinase' names enzymes involved in phosphorylation, and related phrases described activation events; over time the compound 'kinase-activating' came to be used specifically to describe mutations, proteins, or events that directly increase kinase activity.