Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series

Por Rudolph, Joachim, Aliagas, Ignacio, Crawford, James J., Mathieu, Simon, Lee, Wendy, Chao, Qi, Dong, Ping, Rouge, Lionel, Wang, Weiru, Heise, Christopher, Murray, Lesley J., La, Hank, Liu, Yanzhou, Manning, Gerard, Diederich, François, Hoeflich, Klaus P.
Publicado no ACS Med Chem Lett (2015)

Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK(a) Polar Moiety

Por Ndubaku, Chudi O., Crawford, James J., Drobnick, Joy, Aliagas, Ignacio, Campbell, David, Dong, Ping, Dornan, Laura M., Duron, Sergio, Epler, Jennifer, Gazzard, Lewis, Heise, Christopher E., Hoeflich, Klaus P., Jakubiak, Diana, La, Hank, Lee, Wendy, Lin, Baiwei, Lyssikatos, Joseph P., Maksimoska, Jasna, Marmorstein, Ronen, Murray, Lesley J., O’Brien, Thomas, Oh, Angela, Ramaswamy, Sreemathy, Wang, Weiru, Zhao, Xianrui, Zhong, Yu, Blackwood, Elizabeth, Rudolph, Joachim
Publicado no ACS Med Chem Lett (2015)

Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors

Por Wenglowsky, Steve, Ren, Li, Ahrendt, Kateri A., Laird, Ellen R., Aliagas, Ignacio, Alicke, Bruno, Buckmelter, Alex J., Choo, Edna F., Dinkel, Victoria, Feng, Bainian, Gloor, Susan L., Gould, Stephen E., Gross, Stefan, Gunzner-Toste, Janet, Hansen, Joshua D., Hatzivassiliou, Georgia, Liu, Bonnie, Malesky, Kim, Mathieu, Simon, Newhouse, Brad, Raddatz, Nicholas J., Ran, Yingqing, Rana, Sumeet, Randolph, Nikole, Risom, Tyler, Rudolph, Joachim, Savage, Scott, Selby, LeAnn T., Shrag, Michael, Song, Kyung, Sturgis, Hillary L., Voegtli, Walter C., Wen, Zhaoyang, Willis, Brandon S., Woessner, Richard D., Wu, Wen-I, Young, Wendy B., Grina, Jonas
Publicado em 2011