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Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors

[Image: see text] The structure-based design of 1, 2, 3, 4-tetrahydroisoquinoline derivatives as selective DDR1 inhibitors is reported. One of the representative compounds, 6j, binds to DDR1 with a K(d) value of 4.7 nM and suppresses its kinase activity with an IC(50) value of 9.4 nM, but it is sign...

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Bibliografiske detaljer
Udgivet i:J Med Chem
Main Authors: Wang, Zhen, Bian, Huan, Bartual, Sergio G., Du, Wenting, Luo, Jinfeng, Zhao, Hu, Zhang, Shasha, Mo, Cheng, Zhou, Yang, Xu, Yong, Tu, Zhengchao, Ren, Xiaomei, Lu, Xiaoyun, Brekken, Rolf A., Yao, Libo, Bullock, Alex N., Su, Jin, Ding, Ke
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2016
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5053573/
https://ncbi.nlm.nih.gov/pubmed/27219676
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b00140
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