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 von 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

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Imidazolone as an Amide Bioisostere in the Development of β‑1,3‑N‑Acetylglucosaminyltransferase 2 (B3GNT2) Inhibitors von Jackson, Jeffrey J., Siegmund, Aaron C., Bai, Wen-Ju, Reed, Anthony B., Birkholz, Adam B., Campuzano, Iain D. G., Créquer-Grandhomme, Amandine, Hu, Ruozhen, Modak, Rucha V., Sudom, Athena, Javier, Noelle, Sanders, Christiana, Lo, Mei-Chu, Xie, Fang, Cee, Victor J., Manzanillo, Paolo, Allen, John G.

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The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement von 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.

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The optimization of aminooxadiazoles as orally active inhibitors of Cdc7 von 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.

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Design, Optimization, and Biological Evaluation of Novel Keto-Benzimidazoles as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A) von Hu, Essa, Kunz, Roxanne K, Chen, Ning, Rumfelt, Shannon, Siegmund, Aaron, Andrews, Kristin, Chmait, Samer, Zhao, Sharon, Davis, Carl, Chen, Hang, Lester-Zeiner, Dianna, Ma, Ji, Biorn, Christopher, Shi, Jianxia, Porter, Amy, Treanor, James, Allen, Jennifer R

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Structure-Based Design of Novel Class II c-Met Inhibitors: 2. SAR and Kinase Selectivity Profiles of the Pyrazolone Series von Liu, Longbin, Norman, Mark H, Lee, Matthew, Xi, Ning, Siegmund, Aaron, Boezio, Alessandro A, Booker, Shon, Choquette, Debbie, D’Angelo, Noel D, Germain, Julie, Yang, Kevin, Yang, Yajing, Zhang, Yihong, Bellon, Steven F, Whittington, Douglas A, Harmange, Jean-Christophe, Dominguez, Celia, Kim, Tae-Seong, Dussault, Isabelle

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Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase–Glucokinase Regulatory Protein (GK–GKRP) Binding: Strategic Use of a N → S (nN → σ... von 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

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Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase von Albrecht, Brian K, Harmange, Jean-Christophe, Bauer, David, Berry, Loren, Bode, Christiane, Boezio, Alessandro A, Chen, April, Choquette, Deborah, Dussault, Isabelle, Fridrich, Cary, Hirai, Satoko, Hoffman, Doug, Larrow, Jay F, Kaplan-Lefko, Paula, Lin, Jasmine, Lohman, Julia, Long, Alexander M, Moriguchi, Jodi, O’Connor, Anne, Potashman, Michele H, Reese, Monica, Rex, Karen, Siegmund, Aaron, Shah, Kavita, Shimanovich, Roman, Springer, Stephanie K, Teffera, Yohannes, Yang, Yajing, Zhang, Yihong, Bellon, Steven F

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Discovery of a Covalent Inhibitor of KRAS G12C (AMG 510) for the Treatment of Solid Tumors von Lanman, Brian A, Allen, Jennifer R, Allen, John G, Amegadzie, Albert K, Ashton, Kate S, Booker, Shon K, Chen, Jian Jeffrey, Chen, Ning, Frohn, Michael J, Goodman, Guy, Kopecky, David J, Liu, Longbin, Lopez, Patricia, Low, Jonathan D, Ma, Vu, Minatti, Ana E, Nguyen, Thomas T, Nishimura, Nobuko, Pickrell, Alexander J, Reed, Anthony B, Shin, Youngsook, Siegmund, Aaron C, Tamayo, Nuria A, Tegley, Christopher M, Walton, Mary C, Wang, Hui-Ling, Wurz, Ryan P, Xue, May, Yang, Kevin C, Achanta, Pragathi, Bartberger, Michael D, Canon, Jude, Hollis, L Steven, McCarter, John D, Mohr, Christopher, Rex, Karen, Saiki, Anne Y, San Miguel, Tisha, Volak, Laurie P, Wang, Kevin H, Whittington, Douglas A, Zech, Stephan G, Lipford, J Russell, Cee, Victor J

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Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors von Lanman, Brian A, Allen, Jennifer R, Allen, John G, Amegadzie, Albert K, Ashton, Kate S, Booker, Shon K, Chen, Jian Jeffrey, Chen, Ning, Frohn, Michael J, Goodman, Guy, Kopecky, David J, Liu, Longbin, Lopez, Patricia, Low, Jonathan D, Ma, Vu, Minatti, Ana E, Nguyen, Thomas T, Nishimura, Nobuko, Pickrell, Alexander J, Reed, Anthony B, Shin, Youngsook, Siegmund, Aaron C, Tamayo, Nuria A, Tegley, Christopher M, Walton, Mary C, Wang, Hui-Ling, Wurz, Ryan P, Xue, May, Yang, Kevin C, Achanta, Pragathi, Bartberger, Michael D, Canon, Jude, Hollis, L. Steven, McCarter, John D, Mohr, Christopher, Rex, Karen, Saiki, Anne Y, San Miguel, Tisha, Volak, Laurie P, Wang, Kevin H, Whittington, Douglas A, Zech, Stephan G, Lipford, J. Russell, Cee, Victor J

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Morphology and Proton Transport in Humidified Phosphonated Peptoid Block Copolymers von Sun, Jing, Jiang, Xi, Siegmund, Aaron, Connolly, Michael D, Downing, Kenneth H, Balsara, Nitash P, Zuckermann, Ronald N

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Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 3. Structure–Activity Relationships within the Aryl Carbinol Region of the N‑Arylsulfonamid... von Nishimura, Nobuko, Norman, Mark H, Liu, Longbin, Yang, Kevin C, Ashton, Kate S, Bartberger, Michael D, Chmait, Samer, Chen, Jie, Cupples, Rod, Fotsch, Christopher, Helmering, Joan, Jordan, Steven R, Kunz, Roxanne K, Pennington, Lewis D, Poon, Steve F, Siegmund, Aaron, Sivits, Glenn, Lloyd, David J, Hale, Clarence, St. Jean, David J

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Application of the sulfonamide functional group as an anchor for solid phase organic synthesis (SPOS) von Beaver, Krista A, Siegmund, Aaron C, Spear, Kerry L

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Phospshoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors: Discovery and Structure–Activity Relationships of a Series of Quinoline and Quinoxaline Deri... von Nishimura, Nobuko, Siegmund, Aaron, Liu, Longbin, Yang, Kevin, Bryan, Marian C, Andrews, Kristin L, Bo, Yunxin, Booker, Shon K, Caenepeel, Sean, Freeman, Daniel, Liao, Hongyu, McCarter, John, Mullady, Erin L, San Miguel, Tisha, Subramanian, Raju, Tamayo, Nuria, Wang, Ling, Whittington, Douglas A, Zalameda, Leeanne, Zhang, Nancy, Hughes, Paul E, Norman, Mark H

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Discovery of a Potent, Selective, and Orally Bioavailable c-Met Inhibitor: 1-(2-Hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-di... von Liu, Longbin, Siegmund, Aaron, Xi, Ning, Kaplan-Lefko, Paula, Rex, Karen, Chen, April, Lin, Jasmine, Moriguchi, Jodi, Berry, Loren, Huang, Liyue, Teffera, Yohannes, Yang, Yajing, Zhang, Yihong, Bellon, Steven F, Lee, Matthew, Shimanovich, Roman, Bak, Annette, Dominguez, Celia, Norman, Mark H, Harmange, Jean-Christophe, Dussault, Isabelle, Kim, Tae-Seong

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Design, Synthesis, and Biological Evaluation of Potent c-Met Inhibitors von D’Angelo, Noel D, Bellon, Steven F, Booker, Shon K, Cheng, Yuan, Coxon, Angela, Dominguez, Celia, Fellows, Ingrid, Hoffman, Douglas, Hungate, Randall, Kaplan-Lefko, Paula, Lee, Matthew R, Li, Chun, Liu, Longbin, Rainbeau, Elizabeth, Reider, Paul J, Rex, Karen, Siegmund, Aaron, Sun, Yaxiong, Tasker, Andrew S, Xi, Ning, Xu, Shimin, Yang, Yajing, Zhang, Yihong, Burgess, Teresa L, Dussault, Isabelle, Kim, Tae-Seong

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Piperazine Oxadiazole Inhibitors of Acetyl-CoA Carboxylase von 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

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Abstract 711: Small molecule compounds that target cell division cycle 7 (Cdc7) kinase inhibit cell proliferation and tumor growth von Bailis, Julie, Fang, Li, Orf, Jessica, Heller, Scott, Bush, Tammy, Bourbeau, Matthew, Escobar, Sonia, Frohn, Michael, Harrington, Paul, Hsieh, Faye, Pickrell, Alexander, Sham, Kelvin, Siegmund, Aaron, Tan, Helming, Zalameda, Leeanne, Allen, John, Wickramasinghe, Dineli

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An efficient one-pot construction of substituted pyrimidinones von Lu, Yuelie, Xiang, Tingjian, Bartberger, Michael D., Bernard, Charles, Bostick, Tracy, Huang, Liang, Liu, Longbin, Siegmund, Aaron, Sukay, Gregory, Guo, Gary, Elipe, Maria Silva, Tormos, Wanda, Dominguez, Celia, Koch, Kevin, Burgess, Laurence E., Basil, Thomas C., Ibrahim, Prabha, Hummel, Conrad

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Discovery of a Potent, Selective, and Orally Bioavailable c-Met Inhibitor: 1-(2-Hydroxy-2-methylpropyl)- N -(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-... von Liu, Longbin, Siegmund, Aaron, Xi, Ning, Kaplan-Lefko, Paula, Rex, Karen, Chen, April, Lin, Jasmine, Moriguchi, Jodi, Berry, Loren, Huang, Liyue, Teffera, Yohannes, Yang, Yajing, Zhang, Yihong, Bellon, Steven F., Lee, Matthew, Shimanovich, Roman, Bak, Annette, Dominguez, Celia, Norman, Mark H., Harmange, Jean-Christophe, Dussault, Isabelle, Kim, Tae-Seong

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