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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
Version:
Publisher's version

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Publisher copy:
10.1021/acs.jmedchem.6b00140

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Publisher:
American Chemical Society Publisher's website
Journal:
Journal of Medicinal Chemistry Journal website
Volume:
59
Issue:
12
Pages:
5911–5916
Publication date:
2016-05-05
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
URN:
uuid:b5905067-daeb-4d7b-9fbe-d3e2e2b95f36
Source identifiers:
625641
Local pid:
pubs:625641
Paper number:
12
Language:
English

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