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

[Display omitted] 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-activate...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 25; no. 7; pp. 1627 - 1629
Main Authors:	Zhu, Hugh Y., Desai, Jagdish, Deng, Yongqi, Cooper, Alan, Wang, James, Shipps, Jerry, Samatar, Ahmed, Carr, Donna, Windsor, William
Format:	Journal Article
Language:	English
Published:	England Elsevier Ltd 01-04-2015
Subjects:	ALIS Amides - chemical synthesis Amides - chemistry Amides - pharmacology Aminophenols - chemical synthesis Aminophenols - chemistry Aminophenols - pharmacology Dose-Response Relationship, Drug Drug Discovery Erk Extracellular regulated kinase Humans MAPK Mitogen-Activated Protein Kinase 1 - antagonists & inhibitors Mitogen-Activated Protein Kinase 1 - metabolism Molecular Structure NeoMorph Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Structure-Activity Relationship Extracellular regulated kinase ALIS MAPK NeoMorph Erk
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Summary:	[Display omitted] 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.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2015.01.049