Peer-reviewed veterinary case report
Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.
- Journal:
- Journal of medicinal chemistry
- Year:
- 2016
- Authors:
- Wang, Zhen et al.
- Affiliation:
- State Key Laboratory of Respiratory Diseases · China
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.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/27219676/