Journal of Medicinal Chemistry
Article
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blood mononuclear cell; IL-1, interleukin-1; IoC, inhibition of
catalysis; ISA, inhibition in solution assay; LPS, lipopolysaccha-
ride; MBP, myelin basic protein; MES, 2-(N-morpholino)-
ethanesulfonic acid; MOPS, 3-(N-morpholino)propanesulfonic
acid; PGE2, prostaglandin E2; PoA, prevention of activation;
SEM, standard error of the mean; TBST, tris-buffered saline with
tween; TCEP, tris(2-carboxyethyl)phosphine; TDC, target
definition compound; TROSY-HSQC, transverse relaxation
optimized spectroscopy with heteronuclear single quantum
coherence
(20) Kosugi, T.; Mitchell, D. R.; Fujino, A.; Imai, M.; Kambe, M.;
Kobayashi, S.; Makino, H.; Matsueda, Y.; Oue, Y.; Komatsu, K.;
Imaizumi, K.; Sakai, Y.; Sugiura, S.; Takenouchi, O.; Unoki, G.;
Yamakoshi, Y.; Cunliffe, V.; Frearson, J.; Gordon, R.; Harris, C. J.;
Kalloo-Hosein, H.; Le, J.; Patel, G.; Simpson, D. J.; Sherborne, B.;
Thomas, P. S.; Suzuki, N.; Takimoto-Kamimura, M.; Kataoka, K.
Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAP-
KAP-K2) as an Antiinflammatory Target: Discovery and in Vivo Activity
of Selective Pyrazolo[1,5-a]pyrimidine Inhibitors Using a Focused
Library and Structure-Based Optimization Approach. J. Med. Chem.
2012, 55, 6700−6715.
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