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Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors. | LitMetric
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Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors.

Bowen Yang Qian Wu Xiajuan Huan Yingqing Wang Yin Sun Yueyue Yang Tongchao Liu Xin Wang Lin Chen Bing Xiong Dongmei Zhao Zehong Miao Danqi Chen

Bioorg Med Chem Lett

Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China. Electronic address:

Published: February 2021

In an in-house screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were designed and synthesized, among which some compounds had potent TNIK inhibition with IC values lower than 1 nM. Some compounds showed concentration-dependent characteristics of IL-2 inhibition. These results provided new applications of TNIK inhibitors and new prospects of TNIK as a drug target.

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http://dx.doi.org/10.1016/j.bmcl.2020.127749DOI Listing

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