化学
吡啶
药物发现
IC50型
组合化学
药理学
立体化学
体外
药物化学
生物化学
生物
作者
Bowen Yang,Qian Wu,Xia‐Juan Huan,Ying-Qing Wang,Yin Sun,Yueyue Yang,Tongchao Liu,Xin Wang,Lin Chen,Bing Xiong,Dongmei Zhao,Ze‐Hong Miao,Danqi Chen
标识
DOI:10.1016/j.bmcl.2020.127749
摘要
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.
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