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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 nonmutated kinases. 6j also demonstrated reasonable 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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Publisher copy:
10.1021/acs.jmedchem.6b00140

Authors


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Bayer Pharma AG More from this funder
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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:
2016-05-01
Acceptance date:
2016-05-24
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
Pmid:
27219676
Source identifiers:
625641

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