Target validation using chemical probes

 -Catenin 1 and  -catenin 2 play similar and distinct roles in left-right asymmetric development of zebrafish embryos

(2012) M. Zhang et al.   DEVELOPMENT

Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

(2012) Paul V. Fish et al.   JOURNAL OF MEDICINAL CHEMISTRY

Confirming Target Engagement for Reversible Inhibitors in Vivo by Kinetically Tuned Activity-Based Probes

(2012) Alexander Adibekian et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Kinetics of Inhibitor Cycling Underlie Therapeutic Disparities between EGFR-Driven Lung and Brain Cancers

(2012) Krister J. Barkovich et al.   Cancer Discovery

In Situ Kinase Profiling Reveals Functionally Relevant Properties of Native Kinases

(2011) Matthew P. Patricelli et al.   CHEMISTRY & BIOLOGY

Can the flow of medicines be improved? Fundamental pharmacokinetic and pharmacological principles toward improving Phase II survival

(2011) Paul Morgan et al.   DRUG DISCOVERY TODAY

Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains

(2011) Chun-wa Chung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain

(2011) K. Ahn et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Small Molecules Targeting Hepatitis C Virus-Encoded NS5A Cause Subcellular Redistribution of Their Target: Insights into Compound Modes of Action

(2011) P. Targett-Adams et al.   JOURNAL OF VIROLOGY

The Subcellular Distribution of Small Molecules: From Pharmacokinetics to Synthetic Biology

(2011) Nan Zheng et al.   MOLECULAR PHARMACEUTICS

Getting pharmaceutical R&D back on target

(2011) Mark E Bunnage   Nature Chemical Biology

Zebrafish developmental screening of the ToxCast™ Phase I chemical library

(2011) S. Padilla et al.   REPRODUCTIVE TOXICOLOGY

Probing the Probes: Fitness Factors For Small Molecule Tools

(2010) Paul Workman et al.   CHEMISTRY & BIOLOGY

Activity-based Proteomics of Enzyme Superfamilies: Serine Hydrolases as a Case Study

(2010) Gabriel M. Simon et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect

(2010) Min Gao et al.   NATURE

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

The art of the chemical probe

(2010) Stephen V Frye   Nature Chemical Biology

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

Identification of a Novel Retinoid by Small Molecule Screening with Zebrafish Embryos

(2008) Chetana Sachidanandan et al.   PLoS One