Discovery of 9-cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial.
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DOI: 10.1021/acs.jmedchem.0c00272
Abstract: GPR84 is a medium chain free fatty acid-binding G protein-coupled receptor associated with inflammatory and fibrotic diseases. As the only reported antagonist of GPR84 (PBI-4050) displays relatively low potency and selectivity, a clear need exists… read more here.
Keywords: discovery cyclopropylethynyl; glpg1205; gpr84; modulator ... See more keywords