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. 2008 Feb 1;18(3):938-41.
doi: 10.1016/j.bmcl.2007.12.037. Epub 2007 Dec 23.

Pyrazinoindolone inhibitors of MAPKAP-K2

D R Goldberg  1 , Y Choi, D Cogan, M Corson, R DeLeon, A Gao, L Gruenbaum, M H Hao, D Joseph, M A Kashem, C Miller, N Moss, M R Netherton, C P Pargellis, J Pelletier, R Sellati, D Skow, C Torcellini, Y-C Tseng, J Wang, R Wasti, B Werneburg, J P Wu, Z Xiong
Affiliations

Pyrazinoindolone inhibitors of MAPKAP-K2

D R Goldberg et al. Bioorg Med Chem Lett. .

Abstract

Optimization of pyrazinoindolone inhibitors of MAPKAP-K2 (MK2) provides a reasonable balance of cellular potency and physicochemical properties. Mechanistic studies support the inhibition of MK2 which is responsible for the sub-micromolar cellular efficacy.

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