Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors
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
Published in Journal of medicinal chemistry (27.09.2012)
Published in Journal of medicinal chemistry (27.09.2012)
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Discovery of pyrrolopyrimidine inhibitors of Akt
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.
Published in Bioorganic & medicinal chemistry letters (01.10.2010)
Published in Bioorganic & medicinal chemistry letters (01.10.2010)
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Journal Article
Discovery and SAR of spirochromane Akt inhibitors
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.
Published in Bioorganic & medicinal chemistry letters (15.04.2011)
Published in Bioorganic & medicinal chemistry letters (15.04.2011)
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Journal Article
RET Solvent Front Mutations Mediate Acquired Resistance to Selective RET Inhibition in RET-Driven Malignancies
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
Published in Journal of thoracic oncology (01.04.2020)
Published in Journal of thoracic oncology (01.04.2020)
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Journal Article
Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors
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.
Published in Bioorganic & medicinal chemistry letters (01.12.2010)
Published in Bioorganic & medicinal chemistry letters (01.12.2010)
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Journal Article
A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors
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
Published in Cancer discovery (01.09.2017)
Published in Cancer discovery (01.09.2017)
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Computation of Brain−Blood Partitioning of Organic Solutes via Free Energy Calculations
Lombardo, Franco, Blake, James F, Curatolo, William J
Published in Journal of medicinal chemistry (22.11.1996)
Published in Journal of medicinal chemistry (22.11.1996)
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Journal Article
Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity
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
Published in ACS medicinal chemistry letters (13.12.2018)
Published in ACS medicinal chemistry letters (13.12.2018)
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Journal Article
Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS G12D Inhibitor
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
Published in Journal of medicinal chemistry (24.02.2022)
Published in Journal of medicinal chemistry (24.02.2022)
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Journal Article
Use of QSPR Modeling to Characterize In Vitro Binding of Drugs to a Gut-Restricted Polymer
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
Published in Pharmaceutical research (01.04.2018)
Published in Pharmaceutical research (01.04.2018)
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Journal Article
Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor
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
Published in Journal of medicinal chemistry (24.02.2022)
Published in Journal of medicinal chemistry (24.02.2022)
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Journal Article
Discovery of 5‑Azaquinoxaline Derivatives as Potent and Orally Bioavailable Allosteric SHP2 Inhibitors
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.
Published in ACS medicinal chemistry letters (14.12.2023)
Published in ACS medicinal chemistry letters (14.12.2023)
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Journal Article
Discovery of Highly Potent, Selective, and Efficacious Small Molecule Inhibitors of ERK1/2
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
Published in Journal of medicinal chemistry (26.02.2015)
Published in Journal of medicinal chemistry (26.02.2015)
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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 Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development
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
Published in Journal of medicinal chemistry (23.06.2016)
Published in Journal of medicinal chemistry (23.06.2016)
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Journal Article
Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2
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.
Published in Bioorganic & medicinal chemistry letters (15.06.2014)
Published in Bioorganic & medicinal chemistry letters (15.06.2014)
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Journal Article
Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer
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
Published in Journal of medicinal chemistry (09.07.2020)
Published in Journal of medicinal chemistry (09.07.2020)
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Journal Article
Identification of the Clinical Development Candidate MRTX849 , a Covalent KRAS G12C Inhibitor for the Treatment of Cancer
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
Published in Journal of medicinal chemistry (09.07.2020)
Published in Journal of medicinal chemistry (09.07.2020)
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Journal Article
Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors
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
Published in Bioorganic & medicinal chemistry letters (01.05.2007)
Published in Bioorganic & medicinal chemistry letters (01.05.2007)
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