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Bioorg Med Chem Lett. 2012 Mar 15;22(6):2266-70. doi: 10.1016/j.bmcl.2012.01.077. Epub 2012 Jan 31.

Discovery of a series of imidazopyrazine small molecule inhibitors of the kinase MAPKAPK5, that show activity using in vitro and in vivo models of rheumatoid arthritis.

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  • 1Galapagos NV, Generaal de Wittelaan L11 A3, 2800 Mechelen, Belgium.


MAPKAPK5 has been proposed to play a role in regulation of matrix metalloprotease expression and so to be a potential target for intervention in rheumatoid arthritis. We present here the identification of a series of compounds against this target which are effective in both biochemical and cell assays. The expansion of the series is described, along with early SAR and pharmacokinetics for some representative compounds.

Copyright © 2012 Elsevier Ltd. All rights reserved.

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