Discovery of hydroxyaniline amides as selective Extracellular Regulated Kinase (Erk) inhibitors.

Bioorg Med Chem Lett

Discovery Oncology, Merck Research Laboratories, 2015 Galloping Hill Rd, Kenilworth, NJ 07033, United States.

Published: April 2015

Starting from weak μM hits identified through affinity based Automated Ligand Identification System (ALIS) screenings, double digit nM hydroxyaniline amide Erk inhibitors were discovered. This class of compounds had the unique dual mechanism of inhibiting activated and non-activated forms of Erk. They generally had high degree of selectivity in kinase panel tested.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2015.01.049DOI Listing

Publication Analysis

Top Keywords

erk inhibitors
8
discovery hydroxyaniline
4
hydroxyaniline amides
4
amides selective
4
selective extracellular
4
extracellular regulated
4
regulated kinase
4
kinase erk
4
inhibitors starting
4
starting weak
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!