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Quinoline and thiazolopyridine allosteric inhibitors of MALT1.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Jul2019, Vol. 29 Issue 14, p1694-1698. 5p. - Publication Year :
- 2019
-
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. [ABSTRACT FROM AUTHOR]
- Subjects :
- *QUINOLINE
*PROTEASE inhibitors
*MICE
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 29
- Issue :
- 14
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 136824810
- Full Text :
- https://doi.org/10.1016/j.bmcl.2019.05.040