Scaffold mining of kinase hinge binders in crystal structure database

Kinase Drug Discovery – What’s Next in the Field?

(2013) Philip Cohen et al.   ACS Chemical Biology

The Evolution of Protein Kinase Inhibitors from Antagonists to Agonists of Cellular Signaling

(2011) Arvin C. Dar et al.   Annual Review of Biochemistry

Analysis of Imatinib and Sorafenib Binding to p38α Compared with c-Abl and b-Raf Provides Structural Insights for Understanding the Selectivity of Inhibitors Targeting the DFG-Out Form of Protein Kinases

(2010) Haridasan V. Namboodiri et al.   BIOCHEMISTRY

Biochemical Characterization of TAK-593, a Novel VEGFR/PDGFR Inhibitor with a Two-Step Slow Binding Mechanism

(2010) Hidehisa Iwata et al.   BIOCHEMISTRY

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

(2010) L. A. Honigberg et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

An enriched structural kinase database to enable kinome-wide structure-based analyses and drug discovery

(2010) Natasja Brooijmans et al.   PROTEIN SCIENCE

The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo

(2009) Joel M. Kremer et al.   ARTHRITIS AND RHEUMATISM

Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success

(2009) Frank Lovering et al.   JOURNAL OF MEDICINAL CHEMISTRY

p38α MAP Kinase C-Terminal Domain Binding Pocket Characterized by Crystallographic and Computational Analyses

(2009) J. Jefferson P. Perry et al.   JOURNAL OF MOLECULAR BIOLOGY

Development of a Fluorescent-Tagged Kinase Assay System for the Detection and Characterization of Allosteric Kinase Inhibitors

(2009) Jeffrey R. Simard et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Potent and selective pyrazole-based inhibitors of B-Raf kinase

(2008) Joshua D. Hansen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Small Molecule Recognition of c-Src via the Imatinib-Binding Conformation

(2008) Arvin C. Dar et al.   CHEMISTRY & BIOLOGY