Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4.
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.
Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. jppowers@amgen.com
Jay P
JP
Powers
Shyun
S
Li
Juan C
JC
Jaen
Jinqian
J
Liu
Nigel P C
NP
Walker
Zhulun
Z
Wang
Holger
H
Wesche
D000478:Alkylation; D000577:Amides / Q000737:chemistry; D001562:Benzimidazoles / Q000737:chemistry; D003432:Cross-Linking Reagents / Q000737:chemistry; D053592:Interleukin-1 Receptor-Associated Kinases; D047908:Intracellular Signaling Peptides and Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000577:Amides; D001562:Benzimidazoles; D003432:Cross-Linking Reagents; D047908:Intracellular Signaling Peptides and Proteins; D047428:Protein Kinase Inhibitors; C031000:benzimidazole; D053592:Interleukin-1 Receptor-Associated Kinases; D017346:Protein Serine-Threonine Kinases