Discovery of Triazolopyrimidine-Based PDE8B Inhibitors: Exceptionally Ligand-Efficient and Lipophilic Ligand-Efficient Compounds for the Treatment of Diabetes.
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A high throughput screening hit is deconstructed to optimize for ligand efficiency against PDE8B.
[1] S. Wright,et al. Discovery of triazolopyrimidine-based PDE8B inhibitors: exceptionally ligand-efficient and lipophilic ligand-efficient compounds for the treatment of diabetes. , 2012, Bioorganic & medicinal chemistry letters.