Structure-based design of tetrahydroisoquinoline-7-carboxamides as selective discoidin domain receptor 1 (DDR1) inhibitors.
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 Kd value of 4.7 nM and suppresses its kinase activity with an IC50 value of 9.4 nM, but it is significantly less potent...
Full description
Bibliographic Details
Main Authors: |
Wang, Z,
Bian, H,
Bartual, S,
Du, W,
Luo, J,
Zhao, H,
Zhang, S,
Mo, C,
Zhou, Y,
Xu, Y,
Tu, Z,
Ren, X,
Lu, X,
Brekken, R,
Yao, L,
Bullock, A,
Su, J,
Ding, K |
Format: | Journal article
|
Language: | English |
Published: |
American Chemical Society
2016
|