2-Aminoimidazoles inhibitors of TGF-beta receptor 1.
Article Details
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Bonafoux D, Chuaqui C, Boriack-Sjodin PA, Fitch C, Hankins G, Josiah S, Black C, Hetu G, Ling L, Lee WC
2-Aminoimidazoles inhibitors of TGF-beta receptor 1.
Bioorg Med Chem Lett. 2009 Feb 1;19(3):912-6. doi: 10.1016/j.bmcl.2008.11.119. Epub 2008 Dec 11.
- PubMed ID
- 19135364 [ View in PubMed]
- Abstract
The 4-(5-fluoro-6-methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-ylamine 3 is a potent and selective inhibitor of TGF-betaR1. Substitution of the amino group of 3 typically led to a slight decrease in the affinity for the receptor and in TGF-beta-inducted PAI-luciferase reporter activity. However, 2-acetamidoimidazoles were identified as attractive candidates for further optimization as a result of their significant activity combined to their superior pharmacokinetic profile.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) N-[4-(5-fluoro-6-methylpyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]acetamide TGF-beta receptor type-1 EC 50 (nM) 180 N/A N/A Details N-[4-(5-fluoro-6-methylpyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-yl]acetamide TGF-beta receptor type-1 Ki (nM) 7.1 N/A N/A Details