This was possiblethanks to a streamlined medicinal chemistry campaign on chemicallytractable early hits underpinned by an ad-hoc, in-house assay that allowed for the rapid elucidation of their mode of action.In summary, the identification of NAMs of A2AR representsan exciting step toward the development of novel agents for saferimmunotherapies in specific tumor settings, and the series hasthe potential for a fast progression toward the clinic. The gene discussed is ADORA2A; the disease is neoplasm.