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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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Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2016
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5053573/
https://www.ncbi.nlm.nih.gov/pubmed/27219676
http://dx.doi.org/10.1021/acs.jmedchem.6b00140