Journal article
Structure-based design of tetrahydroisoquinoline-7-carboxamides as selective discoidin domain receptor 1 (DDR1) inhibitors
- Abstract:
- 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 for a panel of 400 non-mutated kinases. 6j also demonstrated rea-sonable pharmacokinetic properties and a promising oral therapeutic effect in a bleomycin-induced mouse pulmonary fibrosis model.
- Publication status:
- Published
- Peer review status:
- Peer reviewed
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(Preview, Version of record, pdf, 3.8MB, Terms of use)
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- Publisher copy:
- 10.1021/acs.jmedchem.6b00140
Authors
+ National Natural Science Foundation of China
More from this funder
- Grant:
- 81425021
- Grant:
- 21572230
- Publisher:
- American Chemical Society
- Journal:
- Journal of Medicinal Chemistry More from this journal
- Volume:
- 59
- Issue:
- 12
- Pages:
- 5911–5916
- Publication date:
- 2016-05-01
- Acceptance date:
- 2016-05-24
- DOI:
- EISSN:
-
1520-4804
- ISSN:
-
0022-2623
- Language:
-
English
- Pubs id:
-
pubs:625641
- UUID:
-
uuid:b5905067-daeb-4d7b-9fbe-d3e2e2b95f36
- Local pid:
-
pubs:625641
- Source identifiers:
-
625641
- Deposit date:
-
2016-06-14
- ARK identifier:
Terms of use
- Copyright holder:
- American Chemical Society
- Copyright date:
- 2016
- Notes:
- Copyright © 2016 American Chemical Society. This is an open access article published under a Creative Commons Attribution (CC-BY) License, which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
- Licence:
- CC Attribution (CC BY)
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