Discovery of Clinical Candidate 1‑(4-(3-(4-(1H‑Benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), A Potent, Selective, and Efficacious Inhibitor of Phosphodiesterase 10A (PDE10A)
Hu, Essa, Chen, Ning, Bourbeau, Matthew P, Harrington, Paul E, Biswas, Kaustav, Kunz, Roxanne K, Andrews, Kristin L, Chmait, Samer, Zhao, Xiaoning, Davis, Carl, Ma, Ji, Shi, Jianxia, Lester-Zeiner, Dianna, Danao, Jean, Able, Jessica, Cueva, Madelyn, Talreja, Santosh, Kornecook, Thomas, Chen, Hang, Porter, Amy, Hungate, Randall, Treanor, James, Allen, Jennifer R
Published in Journal of medicinal chemistry (14.08.2014)
Published in Journal of medicinal chemistry (14.08.2014)
Get full text
Journal Article
Nonracemic Synthesis of GK–GKRP Disruptor AMG-3969
Bourbeau, Matthew P, Ashton, Kate S, Yan, Jie, St. Jean, David J
Published in Journal of organic chemistry (18.04.2014)
Published in Journal of organic chemistry (18.04.2014)
Get full text
Journal Article
The optimization of aminooxadiazoles as orally active inhibitors of Cdc7
Harrington, Paul E., Bourbeau, Matthew P., Fotsch, Christopher, Frohn, Michael, Pickrell, Alexander J., Reichelt, Andreas, Sham, Kelvin, Siegmund, Aaron C., Bailis, Julie M., Bush, Tammy, Escobar, Sonia, Hickman, Dean, Heller, Scott, Hsieh, Faye, Orf, Jessica N., Rong, Minqing, San Miguel, Tisha, Tan, Helming, Zalameda, Leeanne, Allen, John G.
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
Get full text
Journal Article
2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics
Zeng, Qingping, Bourbeau, Matthew P., Wohlhieter, G. Erich, Yao, Guomin, Monenschein, Holger, Rider, James T., Lee, Matthew R., Zhang, Shiwen, Lofgren, Julie, Freeman, Daniel, Li, Chun, Tominey, Elizabeth, Huang, Xin, Hoffman, Douglas, Yamane, Harvey, Tasker, Andrew S., Dominguez, Celia, Viswanadhan, Vellarkad N., Hungate, Randall, Zhang, Xiaoling
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Get full text
Journal Article
Discovery of AM-6494: A Potent and Orally Efficacious β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2
Pettus, Liping H, Bourbeau, Matthew P, Bradley, Jodi, Bartberger, Michael D, Chen, Kui, Hickman, Dean, Johnson, Michael, Liu, Qingyian, Manning, James R, Nanez, Adrian, Siegmund, Aaron C, Wen, Paul H, Whittington, Douglas A, Allen, Jennifer R, Wood, Stephen
Published in Journal of medicinal chemistry (12.03.2020)
Published in Journal of medicinal chemistry (12.03.2020)
Get full text
Journal Article
Azole-based inhibitors of AKT/PKB for the treatment of cancer
Zeng, Qingping, Allen, John G., Bourbeau, Matthew P., Wang, Xianghong, Yao, Guomin, Tadesse, Seifu, Rider, James T., Yuan, Chester C., Hong, Fang-Tsao, Lee, Matthew R., Zhang, Shiwen, Lofgren, Julie A., Freeman, Daniel J., Yang, Suijin, Li, Chun, Tominey, Elizabeth, Huang, Xin, Hoffman, Douglas, Yamane, Harvey K., Fotsch, Christopher, Dominguez, Celia, Hungate, Randall, Zhang, Xiaoling
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Get full text
Journal Article
Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe
Tamayo, Nuria A, Bourbeau, Matthew P, Allen, Jennifer R, Ashton, Kate S, Chen, Jian Jeffrey, Kaller, Matthew R, Nguyen, Thomas T, Nishimura, Nobuko, Pettus, Liping H, Walton, Mary, Belmontes, Brian, Moriguchi, Jodi, Chen, Kui, McCarter, John D, Hanestad, Kelly, Chung, Grace, Ninniri, Maria Stefania S, Sun, Jan, Poppe, Leszek, Spahr, Chris, Hui, John, Jia, Lei, Wu, Tian, Dahal, Upendra P, Edson, Katheryne Z, Payton, Marc
Published in Journal of medicinal chemistry (24.03.2022)
Published in Journal of medicinal chemistry (24.03.2022)
Get full text
Journal Article
AMG 193, a Clinical Stage MTA-Cooperative PRMT5 Inhibitor, Drives Antitumor Activity Preclinically and in Patients With MTAP-Deleted Cancers
Belmontes, Brian, Slemmons, Katherine K, Su, Chun, Liu, Siyuan, Policheni, Antonia N, Moriguchi, Jodi, Tan, Hong, Xie, Fang, Aiello, Daniel Andrew, Yang, Yajing, Lazaro, Raul, Aeffner, Famke, Rees, Matthew G, Ronan, Melissa M, Roth, Jennifer A, Vestergaard, Mikkel, Cowland, Sanne, Andersson, Jan, Sarvary, Ian, Chen, Qing, Sharma, Pooja, Lopez, Patricia, Tamayo, Nuria, Pettus, Liping H, Ghimire-Rijal, Sudipa, Mukund, Susmith, Allen, Jennifer R, DeVoss, Jason, Coxon, Angela, Rodon, Jordi, Ghiringhelli, Francois, Penel, Nicolas, Prenen, Hans, Glad, Sanne, Chuang, Chen-Hua, Keyvanjah, Kiana, Townsley, Danielle M, Butler, John R, Bourbeau, Matthew P, Caenepeel, Sean, Hughes, Paul E
Published in Cancer discovery (16.09.2024)
Published in Cancer discovery (16.09.2024)
Get full text
Journal Article
The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement
Frohn, Michael, Liu, Longbin, Siegmund, Aaron C., Qian, Wenyuan, Amegadzie, Albert, Chen, Ning, Tan, Helming, Hickman, Dean, Wood, Stephen, Wen, Paul H., Bartberger, Michael D., Whittington, Douglas A., Allen, Jennifer R., Bourbeau, Matthew P.
Published in Bioorganic & medicinal chemistry letters (15.07.2020)
Published in Bioorganic & medicinal chemistry letters (15.07.2020)
Get full text
Journal Article
Discovery and Optimization of Chromenotriazolopyrimidines as Potent Inhibitors of the Mouse Double Minute 2−Tumor Protein 53 Protein−Protein Interaction
Allen, John G, Bourbeau, Matthew P, Wohlhieter, G. Erich, Bartberger, Michael D, Michelsen, Klaus, Hungate, Randall, Gadwood, Robert C, Gaston, Rick D, Evans, Bruce, Mann, Larry W, Matison, Michael E, Schneider, Stephen, Huang, Xin, Yu, Dongyin, Andrews, Paul S, Reichelt, Andreas, Long, Alexander M, Yakowec, Peter, Yang, Evelyn Y, Lee, Tani Ann, Oliner, Jonathan D
Published in Journal of medicinal chemistry (26.11.2009)
Published in Journal of medicinal chemistry (26.11.2009)
Get full text
Journal Article
Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase–Glucokinase Regulatory Protein (GK–GKRP) Binding: Strategic Use of a N → S (nN → σS–X) Interaction for Conformational Constraint
Pennington, Lewis D, Bartberger, Michael D, Croghan, Michael D, Andrews, Kristin L, Ashton, Kate S, Bourbeau, Matthew P, Chen, Jie, Chmait, Samer, Cupples, Rod, Fotsch, Christopher, Helmering, Joan, Hong, Fang-Tsao, Hungate, Randall W, Jordan, Steven R, Kong, Ke, Liu, Longbin, Michelsen, Klaus, Moyer, Carolyn, Nishimura, Nobuko, Norman, Mark H, Reichelt, Andreas, Siegmund, Aaron C, Sivits, Glenn, Tadesse, Seifu, Tegley, Christopher M, Van, Gwyneth, Yang, Kevin C, Yao, Guomin, Zhang, Jiandong, Lloyd, David J, Hale, Clarence, St. Jean, David J
Published in Journal of medicinal chemistry (24.12.2015)
Published in Journal of medicinal chemistry (24.12.2015)
Get full text
Journal Article
Small-molecule inhibition of kinesin KIF18A reveals a mitotic vulnerability enriched in chromosomally unstable cancers
Payton, Marc, Belmontes, Brian, Hanestad, Kelly, Moriguchi, Jodi, Chen, Kui, McCarter, John D, Chung, Grace, Ninniri, Maria Stefania, Sun, Jan, Manoukian, Raffi, Chambers, Stuart, Ho, Seok-Man, Kurzeja, Robert J M, Edson, Katheryne Z, Dahal, Upendra P, Wu, Tian, Wannberg, Sharon, Beltran, Pedro J, Canon, Jude, Boghossian, Andrew S, Rees, Matthew G, Ronan, Melissa M, Roth, Jennifer A, Minocherhomji, Sheroy, Bourbeau, Matthew P, Allen, Jennifer R, Coxon, Angela, Tamayo, Nuria A, Hughes, Paul E
Published in Nature cancer (01.01.2024)
Published in Nature cancer (01.01.2024)
Get more information
Journal Article
Piperazine Oxadiazole Inhibitors of Acetyl-CoA Carboxylase
Bourbeau, Matthew P, Siegmund, Aaron, Allen, John G, Shu, Hong, Fotsch, Christopher, Bartberger, Michael D, Kim, Ki-Won, Komorowski, Renee, Graham, Melissa, Busby, James, Wang, Minghan, Meyer, James, Xu, Yang, Salyers, Kevin, Fielden, Mark, Véniant, Murielle M, Gu, Wei
Published in Journal of medicinal chemistry (27.12.2013)
Published in Journal of medicinal chemistry (27.12.2013)
Get full text
Journal Article
Cytochrome P450-Mediated Epoxidation of 2-Aminothiazole-Based AKT Inhibitors: Identification of Novel GSH Adducts and Reduction of Metabolic Activation through Structural Changes Guided by in Silico and in Vitro Screening
Subramanian, Raju, Lee, Matthew R, Allen, John G, Bourbeau, Matthew P, Fotsch, Christopher, Hong, Fang-Tsao, Tadesse, Seifu, Yao, Guomin, Yuan, Chester C, Surapaneni, Sekhar, Skiles, Gary L, Wang, Xianghong, Wohlhieter, G. Erich, Zeng, Qingping, Zhou, Yihong, Zhu, Xiaochun, Li, Chun
Published in Chemical research in toxicology (15.03.2010)
Published in Chemical research in toxicology (15.03.2010)
Get full text
Journal Article