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Synthesis of new 18F-radiolabeled silicon-based nitroimidazole compounds
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Synthesis, in vivo occupancy, and radiolabeling of potent phosphodiesterase subtype-10 inhibitors as candidates for positron emission tomography imaging
Andres, J-I.; De Angelis, M.; Alcazar, J.; Iturrino, L.; Langlois, X.; Dedeurwaerdere, S.; Lenaerts, I.; Vanhoof, G.; Celen, S.; Bormans, G.; J. Med. Chem., 2011, 54, 5820-5835
Discovery and synthesis of hydronaphthoquinones as novel proteasome inhibitors
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Structure-based design of potent and ligand-efficient inhibitors of CTX-M class A β-lactamase
Nichols, D. A.; Jaishankar, P.; Larson, W.; Smith, E.; Liu, G.; Beyrouthy, R.; Bonnet, R.; Renslo, A. R.; Chen, Y.; J. Med. Chem., 2012, 55(5), 2163-2172
Synthesis and biological evaluation of an orally active glycosylated endomorphin-1
Varamini, P.; Mansfeld, F. M.; Blanchfield, J. T.; Wyse, B. D.; Smith, M. T.; Toth, I.; J. Med. Chem., 2012, 55(12), 5859-5867
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2
Zak, M.; Mendonca, R.; Balazs, M.; Barrett, K.; Bergeron, P.; Blair, W. S.; Chang, C.; Deshmukh, G.; DeVoss, J.; Dragovich, P. S.; Eigenbrot, C.; Ghilardi, N.; Gibbons, P.; Gradl, S.; Hamman, C.; Hanan, E.; Harstad, E.; Hewitt, P. R.; Hurley, C. A.; Jin, T.; Johnson, A.; Johnson, T.; Kenny, J. R.; Koehler, M. F. T.; Kohli, P. B.; Kulagowski, J.; Labadie, S.; Liao, J.; Liimatta, M.; Lin, Z.; Lupardus, P. J.; Maxey, R. J.; Murray, J. M.; Pulk, R.; Rodriguez, M.; Savage, S.; Shia, S.; Steffek, M.; Ubhayakar, S.; Ultsch, M.; Van-Abbema, A.; Ward, S.; Xiao, L.; Xiao, Y.; J. Med. Chem., 2012, 55(13), 6176-6193
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK)
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Discovery and optimization of a novel spiropyrrolidine inhibitor of β-secretase (BACE1) through fragment-based drug design
Efremov, I. V.; Vajdos, F. F.; Borzilleri, K. A.; Capetta, S.; Chen, H.; Dorff, P. H.; Dutra, J. K.; Goldstein, S. W.; Mansour, M.; McColl, A.; Noell, S.; Oborski, C. E.; O’Connell, T. N.; O’Sullivan, T. J.; Pandit, J.; Wang, H.; Wei, B.; Withka, J. M.; J. Med. Chem., 2012, 55(21), 9069-9088
Synthesis, evaluation, and radiolabeling of new potent positive allosteric modulators of the metabotropic glutamate receptor 2 as potential tracers for positron emission tomography imaging
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