890922-80-2

Upstream product

• 890926-59-7 2-amino-5-tert-butylthiophene-3-carboxylic acid 
• 890664-87-6 6-tert-butyl-1H-thieno[2,3-d][1,3]oxazine-2,4-dione 
• 216574-71-9 2-amino-5-tert-butylthiophene-3-carboxylic acid methyl ester 
• 39093-93-1 thiomorpholine 1,1-dioxide 
• 890927-20-5 5-tert-butyl-2-(3-(4-chlorophenyl)ureido)thiophene-3-carboxylic acid 

Relevant academic research and scientific papers

Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD)

Discovery of a new class of DFG-out p38α kinase inhibitors with no hinge interaction is described. A computationally assisted, virtual fragment-based drug design (vFBDD) platform was utilized to identify novel non-aromatic fragments which make productive hydrogen bond interactions with Arg 70 on the αC-helix. Molecules incorporating these fragments were found to be potent inhibitors of p38 kinase. X-ray co-crystal structures confirmed the predicted binding modes. A lead compound was identified as a potent (p38α IC50 = 22 nM) and highly selective (≥150-fold against 150 kinase panel) DFG-out p38 kinase inhibitor.

UREA INHIBITORS OF MAP KINASES

The present invention is directed to a compound having the formula (I) wherein R1, R2, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such as MAP Kinases, in particular