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Bioorg Med Chem Lett. 2008 Oct 15;18(20):5541-4. doi: 10.1016/j.bmcl.2008.09.016. Epub 2008 Sep 7.

5-Aminomethyl-1H-benzimidazoles as orally active inhibitors of inducible T-cell kinase (Itk).

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1
Johnson & Johnson Pharmaceutical Research and Development, 665 Stockton Drive, Exton, PA 19341, USA.

Abstract

A series of novel 5-aminomethyl-1H-benzimidazole based inhibitors of Itk were prepared. Structure-activity relationships, selectivity and cell activity are reported for this series. Compound 2, a potent and selective antagonist of Itk, inhibited anti-CD3 antibody induced IL-2 production in vivo in mice.

PMID:
18823779
DOI:
10.1016/j.bmcl.2008.09.016
[Indexed for MEDLINE]

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