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Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-12-24 , DOI: 10.1016/j.bmcl.2020.127749 Bowen Yang 1 , Qian Wu 2 , Xiajuan Huan 2 , Yingqing Wang 2 , Yin Sun 3 , Yueyue Yang 4 , Tongchao Liu 4 , Xin Wang 4 , Lin Chen 4 , Bing Xiong 4 , Dongmei Zhao 3 , Zehong Miao 2 , Danqi Chen 4
中文翻译：
发现了一系列1 H-吡咯并[2,3- b ]吡啶化合物作为有效的TNIK抑制剂
更新日期：2020-12-24
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-12-24 , DOI: 10.1016/j.bmcl.2020.127749 Bowen Yang 1 , Qian Wu 2 , Xiajuan Huan 2 , Yingqing Wang 2 , Yin Sun 3 , Yueyue Yang 4 , Tongchao Liu 4 , Xin Wang 4 , Lin Chen 4 , Bing Xiong 4 , Dongmei Zhao 3 , Zehong Miao 2 , Danqi Chen 4
Affiliation
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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 IC50 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.
中文翻译：
发现了一系列1 H-吡咯并[2,3- b ]吡啶化合物作为有效的TNIK抑制剂
在内部筛选中，发现1 H-吡咯并[2,3- b ]吡啶支架对TNIK具有高度抑制作用。设计并合成了一系列化合物，其中一些化合物具有强的TNIK抑制作用，IC 50值低于1 nM。一些化合物表现出浓度依赖性的IL-2抑制特性。这些结果提供了TNIK抑制剂的新应用以及TNIK作为药物靶标的新前景。
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