alexa Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors.


Journal of Clinical & Cellular Immunology

Author(s): Snow RJ, Abeywardane A, Campbell S, Lord J, Kashem MA,

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Abstract Benzimidazole 1 was identified as a selective inhibitor of ITK by high throughput screening. Hit-to-lead studies defined the SAR at all three substituents. Reversing the amide linkage at C6 led to 16, with a fivefold improvement of potency. This enhancement is rationalized by the conformational preference of the substituent. A model for the binding of the benzimidazoles to the ATP-binding site of ITK is proposed. This article was published in Bioorg Med Chem Lett and referenced in Journal of Clinical & Cellular Immunology

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