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  • Title: Design, synthesis and optimization of 7-substituted-pyrazolo[4,3-b]pyridine ALK5 (activin receptor-like kinase 5) inhibitors.
    Author: Sabat M, Wang H, Scorah N, Lawson JD, Atienza J, Kamran R, Hixon MS, Dougan DR.
    Journal: Bioorg Med Chem Lett; 2017 May 01; 27(9):1955-1961. PubMed ID: 28359790.
    Abstract:
    A series of potent ALK5 inhibitors were designed using a SBDD approach and subsequently optimized to improve drug likeness. Starting with a 4-substituted quinoline screening hit, SAR was conducted using a ALK5 binding model to understand the binding site and optimize activity. The resulting inhibitors displayed excellent potency but were limited by high in vitro clearance in rat and human microsomes. Using a scaffold morphing strategy, these analogs were transformed into a related pyrazolo[4,3-b]pyridine series with improved ADME properties.
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