Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases.

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Chen N, Burli RW, Neira S, Hungate R, Zhang D, Yu V, Nguyen Y, Tudor Y, Plant M, Flynn S, Meagher KL, Lee MR, Zhang X, Itano A, Schrag M, Xu Y, Ng GY, Hu E

Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4137-41. doi: 10.1016/j.bmcl.2008.05.089. Epub 2008 May 28.

PubMed ID

18554909 [ View in PubMed

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Abstract

A potent and selective c-Kit inhibitor 20 was identified through a structure-activity relationship study. In an in vivo mouse model of mast cell activation, 20 blocked the SCF-induced histamine release with an EC(50) of 26 nM.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Imatinib	Tyrosine-protein kinase ABL1	IC 50 (nM)	110	N/A	N/A	Details
N'-(6-aminopyridin-3-yl)-N-(2-cyclopentylethyl)-4-methyl-benzene-1,3-dicarboxamide	Vascular endothelial growth factor receptor 2	IC 50 (nM)	>25000	N/A	N/A	Details