Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives.

Article Details

Citation

Copy to clipboard

Horio T, Hamasaki T, Inoue T, Wakayama T, Itou S, Naito H, Asaki T, Hayase H, Niwa T

Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives.

Bioorg Med Chem Lett. 2007 May 15;17(10):2712-7. Epub 2007 Mar 3.

PubMed ID

17376680 [ View in PubMed

]

Abstract

To investigate why 3-substituted benzamide derivatives show dual inhibition of Abl and Lyn protein tyrosine kinases, we determined their inhibitory activities against Abl and Lyn, carried out molecular modeling, and conducted a structure-activity relationship study with the aid of a newly determined X-ray structure of the Abl/Lyn dual inhibitor INNO-406 (formerly known as NS-187) bound to human Abl. We found that this series of compounds interacted with both kinases in very similar ways, so that they can inhibit both kinases effectively.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Imatinib	Tyrosine-protein kinase ABL1	IC 50 (nM)	470	N/A	N/A	Details