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A weak antagonist of the pyrimidinergic receptor P2Y 14 containing a dihydropyridopyrimidine core was identified through high-throughput screening. Subsequent optimization led to potent, non-UTP competitive antagonists and represent the first reported non-nucleotide antagonists of this receptor. Compound 18q was identified as a 10nM P2Y 14 antagonist with good oral bioavailability...
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