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ID: ALA4665658
Journal: Bioorg Med Chem Lett
Title: Quinoline and thiazolopyridine allosteric inhibitors of MALT1.
Authors: Scott DA,Hatcher JM,Liu H,Fu M,Du G,Fontán L,Us I,Casalena G,Qiao Q,Wu H,Melnick A,Gray NS
Abstract: Quinolines and thiazolopyridines were developed as allosteric inhibitors of MALT1, with good cellular potency and exquisite selectivity. Mouse pharmacokinetic (PK) profiling showed these to have low in vivo clearance, and moderate oral exposure. The thiazolopyridines were less lipophilic than the quinolines, and one thiazolopyridine example was active in our hIL10 mouse pharmacodynamic (PD) model upon oral dosing.
CiteXplore: 31129051