Moving beyond Rules: The Development of a Central Nervous System Multiparameter Optimization (CNS MPO) Approach To Enable Alignment of Druglike Properties

Por Wager, Travis T., Hou, Xinjun, Verhoest, Patrick R., Villalobos, Anabella
Publicado em 2010

Defining Desirable Central Nervous System Drug Space through the Alignment of Molecular Properties, in Vitro ADME, and Safety Attributes

Por Wager, Travis T., Chandrasekaran, Ramalakshmi Y., Hou, Xinjun, Troutman, Matthew D., Verhoest, Patrick R., Villalobos, Anabella, Will, Yvonne
Publicado em 2010

Late-Stage Microsomal Oxidation Reduces Drug–Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189

Por Stepan, Antonia F., Tran, Tuan P., Helal, Christopher J., Brown, Maria S., Chang, Cheng, O’Connor, Rebecca E., De Vivo, Michael, Doran, Shawn D., Fisher, Ethan L., Jenkinson, Stephen, Karanian, David, Kormos, Bethany L., Sharma, Raman, Walker, Gregory S., Wright, Ann S., Yang, Edward X., Brodney, Michael A., Wager, Travis T., Verhoest, Patrick R., Obach, R. Scott
Publicado no ACS Med Chem Lett (2018)

Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions

Por Tuttle, Jamison B., Anderson, Marie, Bechle, Bruce M., Campbell, Brian M., Chang, Cheng, Dounay, Amy B., Evrard, Edelweiss, Fonseca, Kari R., Gan, Xinmin, Ghosh, Somraj, Horner, Weldon, James, Larry C., Kim, Ji-Young, McAllister, Laura A., Pandit, Jayvardhan, Parikh, Vinod D., Rago, Brian J., Salafia, Michelle A., Strick, Christine A., Zawadzke, Laura E., Verhoest, Patrick R.
Publicado em 2012

Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability

Por Pettersson, Martin, Johnson, Douglas S., Humphrey, John M., Butler, Todd W., am Ende, Christopher W., Fish, Benjamin A., Green, Michael E., Kauffman, Gregory W., Mullins, Patrick B., O’Donnell, Christopher J., Stepan, Antonia F., Stiff, Cory M., Subramanyam, Chakrapani, Tran, Tuan P., Vetelino, Beth Cooper, Yang, Eddie, Xie, Longfei, Bales, Kelly R., Pustilnik, Leslie R., Steyn, Stefanus J., Wood, Kathleen M., Verhoest, Patrick R.
Publicado no ACS Med Chem Lett (2015)

Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy

Por Pettersson, Martin, Johnson, Douglas S., Rankic, Danica A., Kauffman, Gregory W., am Ende, Christopher W., Butler, Todd W., Boscoe, Brian, Evrard, Edelweiss, Helal, Christopher J., Humphrey, John M., Stepan, Antonia F., Stiff, Cory M., Yang, Eddie, Xie, Longfei, Bales, Kelly R., Hajos-Korcsok, Eva, Jenkinson, Stephen, Pettersen, Betty, Pustilnik, Leslie R., Ramirez, David S., Steyn, Stefanus J., Wood, Kathleen M., Verhoest, Patrick R.
Publicado no Medchemcomm (2016)

Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia

Por Dounay, Amy B., Anderson, Marie, Bechle, Bruce M., Campbell, Brian M., Claffey, Michelle M., Evdokimov, Artem, Evrard, Edelweiss, Fonseca, Kari R., Gan, Xinmin, Ghosh, Somraj, Hayward, Matthew M., Horner, Weldon, Kim, Ji-Young, McAllister, Laura A., Pandit, Jayvardhan, Paradis, Vanessa, Parikh, Vinod D., Reese, Matthew R., Rong, SuoBao, Salafia, Michelle A., Schuyten, Katherine, Strick, Christine A., Tuttle, Jamison B., Valentine, James, Wang, Hong, Zawadzke, Laura E., Verhoest, Patrick R.
Publicado em 2012