The ins and outs of selective kinase inhibitor development

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

(2014) Zheng Zhao et al.   ACS Chemical Biology

Recently targeted kinases and their inhibitors—the path to clinical trials

(2014) Stefan Knapp et al.   CURRENT OPINION IN PHARMACOLOGY

A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics

(2014) Apirat Chaikuad et al.   Nature Chemical Biology

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

(2014) Pietro Ciceri et al.   Nature Chemical Biology

Resistance Mechanisms for the Bruton's Tyrosine Kinase Inhibitor Ibrutinib

(2014) Jennifer A. Woyach et al.   NEW ENGLAND JOURNAL OF MEDICINE

Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

(2013) Qingsong Liu et al.   CHEMISTRY & BIOLOGY

Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK)

(2012) Jeffrey M. Axten et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting Diverse Signaling Interaction Sites Allows the Rapid Generation of Bivalent Kinase Inhibitors

(2011) Zachary B. Hill et al.   ACS Chemical Biology

Discovery and Characterization of a Cell-Permeable, Small-Molecule c-Abl Kinase Activator that Binds to the Myristoyl Binding Site

(2011) Jingsong Yang et al.   CHEMISTRY & BIOLOGY

Understanding the Impact of the P-loop Conformation on Kinase Selectivity

(2011) Cristiano R. W. Guimarães et al.   Journal of Chemical Information and Modeling

First-in-Man Clinical Trial of the Oral Pan-AKT Inhibitor MK-2206 in Patients With Advanced Solid Tumors

(2011) Timothy A. Yap et al.   JOURNAL OF CLINICAL ONCOLOGY

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor

(2011) Solveigh C Koeberle et al.   Nature Chemical Biology

Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors

(2010) Jianming Zhang et al.   NATURE

Specific Btk inhibition suppresses B cell– and myeloid cell–mediated arthritis

(2010) Julie A Di Paolo et al.   Nature Chemical Biology

The (un)targeted cancer kinome

(2010) Oleg Fedorov et al.   Nature Chemical Biology

Structure and allosteric effects of low-molecular-weight activators on the protein kinase PDK1

(2009) Valerie Hindie et al.   Nature Chemical Biology

Activation segment dimerization: a mechanism for kinase autophosphorylation of non-consensus sites

(2008) Ashley C W Pike et al.   EMBO JOURNAL