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

Bioorganic & Medicinal Chemistry Letters
2008.0

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.

Knowledge Graph

Similar Paper

Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases
Bioorganic & Medicinal Chemistry Letters 2008.0
Discovery of Aryl Aminoquinazoline Pyridones as Potent, Selective, and Orally Efficacious Inhibitors of Receptor Tyrosine Kinase c-Kit
Journal of Medicinal Chemistry 2008.0
Discovery of amido-benzisoxazoles as potent c-Kit inhibitors
Bioorganic & Medicinal Chemistry Letters 2008.0
Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs)
Journal of Medicinal Chemistry 2016.0
Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I “Gatekeeper” Mutant of cKIT Kinase
Journal of Medicinal Chemistry 2016.0
Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants
Journal of Medicinal Chemistry 2019.0
Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors
Journal of Medicinal Chemistry 2019.0
Discovery of (E)-N<sup>1</sup>-(3-Fluorophenyl)-N<sup>3</sup>-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)malonamide (CHMFL-KIT-033) as a Novel c-KIT T670I Mutant Selective Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs)
Journal of Medicinal Chemistry 2019.0
Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs)
Journal of Medicinal Chemistry 2017.0
Development and Biological Evaluation of Potent and Selective c-KIT<sup>D816V</sup> Inhibitors
Journal of Medicinal Chemistry 2014.0