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)
Axten, J. M.; Medina, J. R.; Feng, Y.; Shu, A.; Romeril, S. P.; Grant, S. W.; Li, W. H. H.; Heerding, D. A.; Minthorn, E.; Mencken, T.; Atkins, C.; Liu, Q.; Rabindran, S.; Kumar, R.; Hong, X.; Goetz, A.; Stanley, T.; Taylor, J. D.; Sigethy, S. D.; Tomberlin, G. H.; Hassell, A. M.; Kahler, K. M.; Shewchuk, L. M.; Gampe, R. T.; J. Med. Chem., 2012, 55(16), 7193-7207
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
Andres, J. I.; Alcazar, J.; Cid, J. M.; De Angelis, M., Iturrino, L.; Langlois, X.; Lavreysen, H.; Trabanco, A. A.; Celen, S.; Bormans, G.; J. Med. Chem., 2012, 55, 8685-8699
Synthesis and biological evaluation of halogenated curcumin analogs as potential nuclear receptor selective agonists
Batie, S.; Lee, J. H.; Jama, R. A:; Browder, D. O.; Montano, L. A.; Huynh, C. C.; Marcus, L. M.; Tsosie, D. G.; Mohammed, Z.; Trang, V.; Marshall, P. A.; Jurutka, P. W.; Wagner, C. E.; Bioorg. Med. Chem., 2013, 21, 693-702
Discovery of selective biaryl ethers as PDE10A inhibitors: Improvement in potency and mitigation of Pgp-mediated efflux
Rzasa, R. M.; Hu, E.; Rumfelt, S.; Chen, N.; Andrews, K. L.; Chmait, S.; Falsey, J. R.; Zhong, W.; Jones, A. D.; Porter, A.; Louie, S. W.; Zhao, X.; Treanor, J. J. S.; Allen, J. R.; Bioorg. Med. Chem. Lett., 2012, 22, 7371-7375
Identification and Characterization of Carprofen as a Multitarget Fatty Acid Amide Hydrolase/Cyclooxygenase Inhibitor
Favia, A. D.; Habrant, D.; Scarpelli, R.; Migliore, M.; Albani, C.; Bertozzi, S. M.; Dionisi, M.; Tarozzo, G.; Piomelli, D.; Cavalli, A.; De Vivo, M.; J. Med. Chem., 2012, 55, 8807-8826
Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform
Desai, B.; Dixon, K.; Farrant, E.; Feng, Q.; Gibson, K. R.; van Hoorn, W. P.; Mills, J.; Morgan, T.; Parry, D. M.; Ramjee, M. K.; Selway, C. N.; Tarver, G. J.; Whitlock, G.; Wright, A. G.; J. Med. Chem., 2013, 56(7), 3033-3047
Discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2-one-containing phosphoinositide 3-kinase (PI3K) p110β isoform inhibitors through structure-based fragment optimisation
Giordanetto, F.; Wallberg, A.; Cassel, J.; Ghosal, S.; Kossenjans, M.; Yuan, Z. Q.; Wang, X.; Liang, L.; Bioorg. Med. Chem. Lett., 2012, 22, 6665-6670
