Structure-based design of tetrahydroisoquinoline-7-carboxamides as selective discoidin domain receptor 1 (DDR1) inhibitors.

Structure-based design of tetrahydroisoquinoline-7-carboxamides as selective discoidin domain receptor 1 (DDR1) inhibitors.

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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...

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Príomhchruthaitheoirí: 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
Formáid: Journal article
Teanga:English
Foilsithe / Cruthaithe: American Chemical Society 2016
Cur síos
Achoimre: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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