Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4

Jay P Powers; Shyun Li; Juan C Jaen; Jinqian Liu; Nigel P C Walker; Zhulun Wang; Holger Wesche

doi:10.1016/j.bmcl.2006.03.020

Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4

Bioorg Med Chem Lett. 2006 Jun 1;16(11):2842-5. doi: 10.1016/j.bmcl.2006.03.020. Epub 2006 Mar 24.

Authors

Jay P Powers¹, Shyun Li, Juan C Jaen, Jinqian Liu, Nigel P C Walker, Zhulun Wang, Holger Wesche

Affiliation

¹ Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. jppowers@amgen.com

PMID: 16563752
DOI: 10.1016/j.bmcl.2006.03.020

Abstract

High-throughput screening of a small-molecule compound library resulted in the identification of a novel series of N-acyl 2-aminobenzimidazoles that are potent inhibitors of interleukin-1 receptor-associated kinase-4.

MeSH terms

Alkylation
Amides / chemistry
Benzimidazoles / chemistry
Cross-Linking Reagents / chemistry
Interleukin-1 Receptor-Associated Kinases
Intracellular Signaling Peptides and Proteins / antagonists & inhibitors*
Intracellular Signaling Peptides and Proteins / metabolism*
Molecular Structure
Protein Kinase Inhibitors / chemistry*
Protein Kinase Inhibitors / pharmacology*
Protein Serine-Threonine Kinases / antagonists & inhibitors*
Protein Serine-Threonine Kinases / metabolism*
Structure-Activity Relationship

Substances

Amides
Benzimidazoles
Cross-Linking Reagents
Intracellular Signaling Peptides and Proteins
Protein Kinase Inhibitors
benzimidazole
Interleukin-1 Receptor-Associated Kinases
Protein Serine-Threonine Kinases