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Quinoline and thiazolopyridine allosteric inhibitors of MALT1.

Bioorg. Med. Chem. Lett.. 2019;

ScottDavid A，HatcherJohn M，LiuHongyan，FuMingpeng，DuGuangyan，FontánLorena，UsIlkay，CasalenaGabriella，QiaoQi，WuHao，MelnickAri，GrayNathana

Products/Services Used	Details	Operation
Biochemicals	… Mouse PK studies were conducted at the Drug Metabolism and Pharmacokinetics laboratory at The Scripps Research Institute, under the supervision of Dr Mike Cameron. Protease profiling was conducted at Genscript USA …	Get A Quote

摘要

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.