Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors von Blake, James F, Xu, Rui, Bencsik, Josef R, Xiao, Dengming, Kallan, Nicholas C, Schlachter, Stephen, Mitchell, Ian S, Spencer, Keith L, Banka, Anna L, Wallace, Eli M, Gloor, Susan L, Martinson, Matthew, Woessner, Richard D, Vigers, Guy P.A, Brandhuber, Barbara J, Liang, Jun, Safina, Brian S, Li, Jun, Zhang, Birong, Chabot, Christine, Do, Steven, Lee, Leslie, Oeh, Jason, Sampath, Deepak, Lee, Brian B, Lin, Kui, Liederer, Bianca M, Skelton, Nicholas J

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Consensus scoring for ligand/protein interactions von Clark, Robert D., Strizhev, Alexander, Leonard, Joseph M., Blake, James F., Matthew, James B.

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RET Solvent Front Mutations Mediate Acquired Resistance to Selective RET Inhibition in RET-Driven Malignancies von Solomon, Benjamin J., Tan, Lavinia, Lin, Jessica J., Wong, Stephen Q., Hollizeck, Sebastian, Ebata, Kevin, Tuch, Brian B., Yoda, Satoshi, Gainor, Justin F., Sequist, Lecia V., Oxnard, Geoffrey R., Gautschi, Oliver, Drilon, Alexander, Subbiah, Vivek, Khoo, Christine, Zhu, Edward Y., Nguyen, Michele, Henry, Dahlia, Condroski, Kevin R., Kolakowski, Gabrielle R., Gomez, Eliana, Ballard, Joshua, Metcalf, Andrew T., Blake, James F., Dawson, Sarah-Jane, Blosser, Wayne, Stancato, Louis F., Brandhuber, Barbara J., Andrews, Steve, Robinson, Bruce G., Rothenberg, S. Michael

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A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors von Drilon, Alexander, Nagasubramanian, Ramamoorthy, Blake, James F, Ku, Nora, Tuch, Brian B, Ebata, Kevin, Smith, Steve, Lauriault, Veronique, Kolakowski, Gabrielle R, Brandhuber, Barbara J, Larsen, Paul D, Bouhana, Karyn S, Winski, Shannon L, Hamor, Robyn, Wu, Wen-I, Parker, Andrew, Morales, Tony H, Sullivan, Francis X, DeWolf, Walter E, Wollenberg, Lance A, Gordon, Paul R, Douglas-Lindsay, Dorothea N, Scaltriti, Maurizio, Benayed, Ryma, Raj, Sandeep, Hanusch, Bethany, Schram, Alison M, Jonsson, Philip, Berger, Michael F, Hechtman, Jaclyn F, Taylor, Barry S, Andrews, Steve, Rothenberg, S Michael, Hyman, David M

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Discovery of pyrrolopyrimidine inhibitors of Akt von Blake, James F., Kallan, Nicholas C., Xiao, Dengming, Xu, Rui, Bencsik, Josef R., Skelton, Nicholas J., Spencer, Keith L., Mitchell, Ian S., Woessner, Richard D., Gloor, Susan L., Risom, Tyler, Gross, Stefan D., Martinson, Matthew, Morales, Tony H., Vigers, Guy P.A., Brandhuber, Barbara J.

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Discovery and SAR of spirochromane Akt inhibitors von Kallan, Nicholas C., Spencer, Keith L., Blake, James F., Xu, Rui, Heizer, Justin, Bencsik, Josef R., Mitchell, Ian S., Gloor, Susan L., Martinson, Matthew, Risom, Tyler, Gross, Stefan D., Morales, Tony H., Wu, Wen-I, Vigers, Guy P.A., Brandhuber, Barbara J., Skelton, Nicholas J.

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Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity von Fell, Jay B, Fischer, John P, Baer, Brian R, Ballard, Joshua, Blake, James F, Bouhana, Karyn, Brandhuber, Barbara J, Briere, David M, Burgess, Laurence E, Burkard, Michael R, Chiang, Harrah, Chicarelli, Mark J, Davidson, Kevin, Gaudino, John J, Hallin, Jill, Hanson, Lauren, Hee, Kenneth, Hicken, Erik J, Hinklin, Ronald J, Marx, Matthew A, Mejia, Macedonio J, Olson, Peter, Savechenkov, Pavel, Sudhakar, Niranjan, Tang, Tony P, Vigers, Guy P, Zecca, Henry, Christensen, James G

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Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors von Bencsik, Josef R., Xiao, Dengming, Blake, James F., Kallan, Nicholas C., Mitchell, Ian S., Spencer, Keith L., Xu, Rui, Gloor, Susan L., Martinson, Matthew, Risom, Tyler, Woessner, Richard D., Dizon, Faith, Wu, Wen-I, Vigers, Guy P.A., Brandhuber, Barbara J., Skelton, Nicholas J., Prior, Wei Wei, Murray, Lesley J.

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Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS G12D Inhibitor von Wang, Xiaolun, Allen, Shelley, Blake, James F, Bowcut, Vickie, Briere, David M, Calinisan, Andrew, Dahlke, Joshua R, Fell, Jay B, Fischer, John P, Gunn, Robin J, Hallin, Jill, Laguer, Jade, Lawson, J David, Medwid, James, Newhouse, Brad, Nguyen, Phong, O'Leary, Jacob M, Olson, Peter, Pajk, Spencer, Rahbaek, Lisa, Rodriguez, Mareli, Smith, Christopher R, Tang, Tony P, Thomas, Nicole C, Vanderpool, Darin, Vigers, Guy P, Christensen, James G, Marx, Matthew A

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Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor von Wang, Xiaolun, Allen, Shelley, Blake, James F, Bowcut, Vickie, Briere, David M, Calinisan, Andrew, Dahlke, Joshua R, Fell, Jay B, Fischer, John P, Gunn, Robin J, Hallin, Jill, Laguer, Jade, Lawson, J. David, Medwid, James, Newhouse, Brad, Nguyen, Phong, O’Leary, Jacob M, Olson, Peter, Pajk, Spencer, Rahbaek, Lisa, Rodriguez, Mareli, Smith, Christopher R, Tang, Tony P, Thomas, Nicole C, Vanderpool, Darin, Vigers, Guy P, Christensen, James G, Marx, Matthew A

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Examination of the Computed Molecular Properties of Compounds Selected for Clinical Development von Blake, James F

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Computation of Brain−Blood Partitioning of Organic Solutes via Free Energy Calculations von Lombardo, Franco, Blake, James F, Curatolo, William J

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Use of QSPR Modeling to Characterize In Vitro Binding of Drugs to a Gut-Restricted Polymer von Brew, Christine Taylor, Blake, James F., Mistry, Anita, Liu, Fengling, Carreno, Diana, Madsen, Deidre, Mu, YongQi, Mayo, Martha, Stahl, Wilhelm, Matthews, David, Maclean, Derek, Harrison, Steve

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Discovery of 5‑Azaquinoxaline Derivatives as Potent and Orally Bioavailable Allosteric SHP2 Inhibitors von Elsayed, Mohamed S. A., Blake, James F., Boys, Mark L., Brown, Eric, Chapsal, Bruno D., Chicarelli, Mark J., Cook, Adam W., Fell, Jay B., Fischer, John P., Hanson, Lauren, Lemieux, Christine, Martinson, Matthew C., McCown, Joseph, McNulty, Oren T., Mejia, Macedonio J., Neitzel, Nickolas A., Otten, Jennifer N., Rodriguez, Martha E., Wilcox, Daniel, Wong, Christina E., Zhou, Yeyun, Hinklin, Ronald J.

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Discovery of Highly Potent, Selective, and Efficacious Small Molecule Inhibitors of ERK1/2 von Ren, Li, Grina, Jonas, Moreno, David, Blake, James F, Gaudino, John J, Garrey, Rustam, Metcalf, Andrew T, Burkard, Michael, Martinson, Matthew, Rasor, Kevin, Chen, Huifen, Dean, Brian, Gould, Stephen E, Pacheco, Patricia, Shahidi-Latham, Sheerin, Yin, Jianping, West, Kristina, Wang, Weiru, Moffat, John G, Schwarz, Jacob B

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Identification of the Clinical Development Candidate MRTX849 , a Covalent KRAS G12C Inhibitor for the Treatment of Cancer von Fell, Jay B, Fischer, John P, Baer, Brian R, Blake, James F, Bouhana, Karyn, Briere, David M, Brown, Karin D, Burgess, Laurence E, Burns, Aaron C, Burkard, Michael R, Chiang, Harrah, Chicarelli, Mark J, Cook, Adam W, Gaudino, John J, Hallin, Jill, Hanson, Lauren, Hartley, Dylan P, Hicken, Erik J, Hingorani, Gary P, Hinklin, Ronald J, Mejia, Macedonio J, Olson, Peter, Otten, Jennifer N, Rhodes, Susan P, Rodriguez, Martha E, Savechenkov, Pavel, Smith, Darin J, Sudhakar, Niranjan, Sullivan, Francis X, Tang, Tony P, Vigers, Guy P, Wollenberg, Lance, Christensen, James G, Marx, Matthew A

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Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer von Fell, Jay B, Fischer, John P, Baer, Brian R, Blake, James F, Bouhana, Karyn, Briere, David M, Brown, Karin D, Burgess, Laurence E, Burns, Aaron C, Burkard, Michael R, Chiang, Harrah, Chicarelli, Mark J, Cook, Adam W, Gaudino, John J, Hallin, Jill, Hanson, Lauren, Hartley, Dylan P, Hicken, Erik J, Hingorani, Gary P, Hinklin, Ronald J, Mejia, Macedonio J, Olson, Peter, Otten, Jennifer N, Rhodes, Susan P, Rodriguez, Martha E, Savechenkov, Pavel, Smith, Darin J, Sudhakar, Niranjan, Sullivan, Francis X, Tang, Tony P, Vigers, Guy P, Wollenberg, Lance, Christensen, James G, Marx, Matthew A

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Discovery of (S)‑1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl‑1H‑pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)‑one (GDC-0994), an Extracellular Signal-Regulated... von Blake, James F, Burkard, Michael, Chan, Jocelyn, Chen, Huifen, Chou, Kang-Jye, Diaz, Dolores, Dudley, Danette A, Gaudino, John J, Gould, Stephen E, Grina, Jonas, Hunsaker, Thomas, Liu, Lichuan, Martinson, Matthew, Moreno, David, Mueller, Lars, Orr, Christine, Pacheco, Patricia, Qin, Ann, Rasor, Kevin, Ren, Li, Robarge, Kirk, Shahidi-Latham, Sheerin, Stults, Jeffrey, Sullivan, Francis, Wang, Weiru, Yin, Jianping, Zhou, Aihe, Belvin, Marcia, Merchant, Mark, Moffat, John, Schwarz, Jacob B

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Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2 von Blake, James F., Gaudino, John J., De Meese, Jason, Mohr, Peter, Chicarelli, Mark, Tian, Hongqi, Garrey, Rustam, Thomas, Allen, Siedem, Christopher S., Welch, Michael B., Kolakowski, Gabrielle, Kaus, Robert, Burkard, Michael, Martinson, Matthew, Chen, Huifen, Dean, Brian, Dudley, Danette A., Gould, Stephen E., Pacheco, Patricia, Shahidi-Latham, Sheerin, Wang, Weiru, West, Kristina, Yin, Jianping, Moffat, John, Schwarz, Jacob B.

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Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors von Eary, C. Todd, Jones, Zachary S., Groneberg, Robert D., Burgess, Laurence E., Mareska, David A., Drew, Mark D., Blake, James F., Laird, Ellen R., Balachari, Devan, O’Sullivan, Michael, Allen, Andrew, Marsh, Vivienne

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