Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants

Discovery of (E)-N1-(3-Fluorophenyl)-N3-(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)

(2019) Xuesong Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2019) Yun Wu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Effects of rigidity on the selectivity of protein kinase inhibitors

(2018) Amir Assadieskandar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Efficacy of Larotrectinib in TRK Fusion–Positive Cancers in Adults and Children

(2018) Alexander Drilon et al.   NEW ENGLAND JOURNAL OF MEDICINE

Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application

(2018) Wei Yan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors

(2018) Jason G. Kettle et al.   JOURNAL OF MEDICINAL CHEMISTRY

Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations

(2018) Alexander Drilon et al.   Cancer Discovery

Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants including T315I for chronic myeloid leukemia

(2018) Xuesong Liu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

NTRK fusion-positive cancers and TRK inhibitor therapy

(2018) Emiliano Cocco et al.   Nature Reviews Clinical Oncology

Targeting TRK family proteins in cancer

(2017) Yekaterina B. Khotskaya et al.   PHARMACOLOGY & THERAPEUTICS

A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion–Positive Solid Tumors

(2017) Alexander Drilon et al.   Cancer Discovery

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

(2016) Binhua Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor

(2016) Maria Menichincheri et al.   JOURNAL OF MEDICINAL CHEMISTRY

Acquired Resistance to the TRK Inhibitor Entrectinib in Colorectal Cancer

(2015) M. Russo et al.   Cancer Discovery

Exploration of Type II Binding Mode: A Privileged Approach for Kinase Inhibitor Focused Drug Discovery?

(2014) Zheng Zhao et al.   ACS Chemical Biology

The landscape of kinase fusions in cancer

(2014) Nicolas Stransky et al.   Nature Communications

Classification of scaffold-hopping approaches

(2011) Hongmao Sun et al.   DRUG DISCOVERY TODAY

Vascular Endothelial Growth Factor Receptor 2 Controls Blood Pressure by Regulating Nitric Oxide Synthase Expression

(2009) Carie S. Facemire et al.   HYPERTENSION