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. 2014 Sep 16;289(47):32937–32951. doi: 10.1074/jbc.M114.602318

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© 2014 by The American Society for Biochemistry and Molecular Biology, Inc.

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FIGURE 3. — Optimization of potency for G2019S-selective TPZ-LRRK2 inhibitors. G2019S-LRRK2 kinase inhibition (IC₅₀) for trans-peptide phosphorylation (peptide phos) or cis-autophosphorylation (Autophos) activities. Ratios for G2019S-LRRK2 to WT-LRRK2 autophosphorylation inhibition are given. A and B, side chain (A) and pendant (B) heterocycle structure-activity-relationships with respect to potency and G2019S-LRRK2 selectivity. The indicated values were derived from at least three independent assays. Chemical synthesis schemes are given in the supplemental information and Figs. 1 and 2.