Optimization of the screening hit 1 led to the identification of novel 1, 5-naphthyridine
aminothiazole and pyrazole derivatives, which are potent and selective inhibitors of the …

Screening of our internal compound collection for inhibitors of the transforming growth factor
β1 (TGF-β1) type I receptor (ALK5) identified several hits. Optimization of the …

Small molecule inhibitors have proven extremely useful for investigating signal transduction
pathways and have the potential for development into therapeutics for inhibiting signal …

A series of 2-pyridinyl-[1, 2, 3] triazoles have been synthesized and evaluated for their ALK5
inhibitory activity in the luciferase reporter assays. Compound 8d showed significant ALK5 …

Inhibitors of transforming growth factor β (TGF-β) type I receptor (ALK5) offer a novel
approach for the treatment of fibrotic diseases such as renal, hepatic, and pulmonary …

A new series of imidazo [2, 1-b][1, 3, 4] thiadiazoles 5 (a–g), 6 (a–g), 9 (a–i) and 12 (a–h)
were synthesized as transforming growth factor-β (TGF-β) type I receptor (also known as …

Clinically, there is a great need for small molecule inhibitors that could control pathogenic
effects of transforming growth factor (TGF-β) and/or modulate effects of TGF-β in normal …

A series of 2-substituted-4-([1, 2, 4] triazolo [1, 5-a] pyridin-6-yl)-5-(6-methylpyridin-2-yl)
imidazoles was synthesized and evaluated to optimize a prototype inhibitor of TGF-β type I …

Novel dihydropyrrolopyrazole-substituted benzimidazoles were synthesized and evaluated
in vitro as inhibitors of transforming growth factor-β type I receptor (TGF-β RI), TGF-β RII, and …

We developed a pharmacophore model for type II inhibitors that was used to guide the
construction of a library of kinase inhibitors. Kinome-wide selectivity profiling of the library …