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  • Title: Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk).
    Author: Moriarty KJ, Takahashi H, Pullen SS, Khine HH, Sallati RH, Raymond EL, Woska JR, Jeanfavre DD, Roth GP, Winters MP, Qiao L, Ryan D, DesJarlais R, Robinson D, Wilson M, Bobko M, Cook BN, Lo HY, Nemoto PA, Kashem MA, Wolak JP, White A, Magolda RL, Tomczuk B.
    Journal: Bioorg Med Chem Lett; 2008 Oct 15; 18(20):5545-9. PubMed ID: 18819799.
    Abstract:
    A series of novel potent benzimidazole based inhibitors of interleukin-2 T-cell kinase (Itk) were prepared. In this report, we discuss the structure-activity relationship (SAR), selectivity, and cell-based activity for the series. We also discuss the SAR associated with an X-ray structure of one of the small-molecule inhibitors bound to ITK.
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