The P2Y2 receptor (P2Y2R) is a target fordiseases including cancer, idiopathic pulmonary fibrosis, and atherosclerosis.However, there are insufficient P2Y2R antagonists availablefor validating P2Y2R function and future drug development.Evaluation of how (R)-5-(7-chloro-2-((2-ethoxyethyl)amino)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-1-methyl-4-thioxo-3,4-dihydropyrimidin-2(1H)-one, a previously published thiazole-based analogue ofAR-C118925, binds in a P2Y2R homology model was used todesign new P2Y2R antagonist scaffolds. Here, P2RY2 is linked to cancer.