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The absolute most encouraging scaffold ended up being optimized through medicinal chemistry resulting in improved strength and selectivity. The optimized compound, ML417 (2, potently promotes D3R-mediated β-arrestin translocation, G protein activation, and ERK1/2 phosphorylation (pERK) while lacking task at various other dopamine receptors. Screening of ML417 against multiple G protein-coupled receptors unveiled excellent global selectivity. Molecular modeling suggests
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