Novel antibody–antibiotic conjugate eliminates intracellular S. aureus von Lehar, Sophie M., Pillow, Thomas, Xu, Min, Staben, Leanna, Kajihara, Kimberly K., Vandlen, Richard, DePalatis, Laura, Raab, Helga, Hazenbos, Wouter L., Hiroshi Morisaki, J., Kim, Janice, Park, Summer, Darwish, Martine, Lee, Byoung-Chul, Hernandez, Hilda, Loyet, Kelly M., Lupardus, Patrick, Fong, Rina, Yan, Donghong, Chalouni, Cecile, Luis, Elizabeth, Khalfin, Yana, Plise, Emile, Cheong, Jonathan, Lyssikatos, Joseph P., Strandh, Magnus, Koefoed, Klaus, Andersen, Peter S., Flygare, John A., Wah Tan, Man, Brown, Eric J., Mariathasan, Sanjeev

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Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer’s Disease von Patel, Snahel, Meilandt, William J, Erickson, Rebecca I, Chen, Jinhua, Deshmukh, Gauri, Estrada, Anthony A, Fuji, Reina N, Gibbons, Paul, Gustafson, Amy, Harris, Seth F, Imperio, Jose, Liu, Wendy, Liu, Xingrong, Liu, Yichin, Lyssikatos, Joseph P, Ma, Changyou, Yin, Jianping, Lewcock, Joseph W, Siu, Michael

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Discovery of Potent and Selective Pyrazolopyrimidine Janus Kinase 2 Inhibitors von Hanan, Emily J, van Abbema, Anne, Barrett, Kathy, Blair, Wade S, Blaney, Jeff, Chang, Christine, Eigenbrot, Charles, Flynn, Sean, Gibbons, Paul, Hurley, Christopher A, Kenny, Jane R, Kulagowski, Janusz, Lee, Leslie, Magnuson, Steven R, Morris, Claire, Murray, Jeremy, Pastor, Richard M, Rawson, Tom, Siu, Michael, Ultsch, Mark, Zhou, Aihe, Sampath, Deepak, Lyssikatos, Joseph P

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Discovery of Highly Potent, Selective, and Brain-Penetrant Aminopyrazole Leucine-Rich Repeat Kinase 2 (LRRK2) Small Molecule Inhibitors von Estrada, Anthony A, Chan, Bryan K, Baker-Glenn, Charles, Beresford, Alan, Burdick, Daniel J, Chambers, Mark, Chen, Huifen, Dominguez, Sara L, Dotson, Jennafer, Drummond, Jason, Flagella, Michael, Fuji, Reina, Gill, Andrew, Halladay, Jason, Harris, Seth F, Heffron, Timothy P, Kleinheinz, Tracy, Lee, Donna W, Pichon, Claire E. Le, Liu, Xingrong, Lyssikatos, Joseph P, Medhurst, Andrew D, Moffat, John G, Nash, Kevin, Scearce-Levie, Kimberly, Sheng, Zejuan, Shore, Daniel G, Wong, Susan, Zhang, Shuo, Zhang, Xiaolin, Zhu, Haitao, Sweeney, Zachary K

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Evaluation of PNU-159682 antibody drug conjugates (ADCs) von Holte, Dane, Lyssikatos, Joseph P., Valdiosera, Amanda M., Swinney, Zachary, Sisodiya, Vikram, Sandoval, Joseph, Lee, Christina, Aujay, Monette A., Tchelepi, Robert B., Hamdy, Omar M., Gu, Christine, Lin, Baiwei, Sarvaiya, Hetal, Pysz, Marybeth A., Laysang, Amy, Williams, Samuel, Jun Lee, Dong, Holda, Magda K., Purcell, James W., Gavrilyuk, Julia

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Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma von Wang, Xiaojing, Blackaby, Wesley, Allen, Vivienne, Chan, Grace Ka Yan, Chang, Jae H, Chiang, Po-Chang, Diène, Coura, Drummond, Jason, Do, Steven, Fan, Eric, Harstad, Eric B, Hodges, Alastair, Hu, Huiyong, Jia, Wei, Kofie, William, Kolesnikov, Aleksandr, Lyssikatos, Joseph P, Ly, Justin, Matteucci, Mizio, Moffat, John G, Munugalavadla, Veerendra, Murray, Jeremy, Nash, David, Noland, Cameron L, Del Rosario, Geoff, Ross, Leanne, Rouse, Craig, Sharpe, Andrew, Slaga, Dionysos, Sun, Minghua, Tsui, Vickie, Wallweber, Heidi, Yu, Shang-Fan, Ebens, Allen J

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Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling von Zak, Mark, Hanan, Emily J., Lupardus, Patrick, Brown, David G., Robinson, Colin, Siu, Michael, Lyssikatos, Joseph P., Romero, F. Anthony, Zhao, Guiling, Kellar, Terry, Mendonca, Rohan, Ray, Nicholas C., Goodacre, Simon C., Crackett, Peter H., McLean, Neville, Hurley, Christopher A., Yuen, Po-wai, Cheng, Yun-Xing, Liu, Xiongcai, Liimatta, Marya, Kohli, Pawan Bir, Nonomiya, Jim, Salmon, Gary, Buckley, Gerry, Lloyd, Julia, Gibbons, Paul, Ghilardi, Nico, Kenny, Jane R., Johnson, Adam

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Discovery of Dual Leucine Zipper Kinase (DLK, MAP3K12) Inhibitors with Activity in Neurodegeneration Models von Patel, Snahel, Cohen, Frederick, Dean, Brian J., De La Torre, Kelly, Deshmukh, Gauri, Estrada, Anthony A., Ghosh, Arundhati Sengupta, Gibbons, Paul, Gustafson, Amy, Huestis, Malcolm P., Le Pichon, Claire E., Lin, Han, Liu, Wendy, Liu, Xingrong, Liu, Yichin, Ly, Cuong Q., Lyssikatos, Joseph P., Ma, Changyou, Scearce-Levie, Kimberly, Shin, Young G., Solanoy, Hilda, Stark, Kimberly L., Wang, Jian, Wang, Bei, Zhao, Xianrui, Lewcock, Joseph W., Siu, Michael

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2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors von Siu, Michael, Pastor, Richard, Liu, Wendy, Barrett, Kathy, Berry, Megan, Blair, Wade S., Chang, Christine, Chen, Jacob Z., Eigenbrot, Charles, Ghilardi, Nico, Gibbons, Paul, He, Haiying, Hurley, Christopher A., Kenny, Jane R., Cyrus Khojasteh, S., Le, Hoa, Lee, Leslie, Lyssikatos, Joseph P., Magnuson, Steve, Pulk, Rebecca, Tsui, Vickie, Ultsch, Mark, Xiao, Yisong, Zhu, Bing-yan, Sampath, Deepak

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Discovery of a Potent (4R,5S)‑4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modelin... von Chen, Huifen, Volgraf, Matthew, Do, Steven, Kolesnikov, Aleksandr, Shore, Daniel G, Verma, Vishal A, Villemure, Elisia, Wang, Lan, Chen, Yong, Hu, Baihua, Lu, Ai-Jun, Wu, Guosheng, Xu, Xiaofeng, Yuen, Po-wai, Zhang, Yamin, Erickson, Shawn D, Dahl, Martin, Brotherton-Pleiss, Christine, Tay, Suzanne, Ly, Justin Q, Murray, Lesley J, Chen, Jun, Amm, Desiree, Lange, Wienke, Hackos, David H, Reese, Rebecca M, Shields, Shannon D, Lyssikatos, Joseph P, Safina, Brian S, Estrada, Anthony A

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A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors von Lee, Wendy, Ortwine, Daniel F., Bergeron, Philippe, Lau, Kevin, Lin, Lichuan, Malek, Shiva, Nonomiya, Jim, Pei, Zhonghua, Robarge, Kirk D., Schmidt, Stephen, Sideris, Steve, Lyssikatos, Joseph P.

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Lead Optimization of a 4‑Aminopyridine Benzamide Scaffold To Identify Potent, Selective, and Orally Bioavailable TYK2 Inhibitors von Liang, Jun, van Abbema, Anne, Balazs, Mercedesz, Barrett, Kathy, Berezhkovsky, Leo, Blair, Wade, Chang, Christine, Delarosa, Donnie, DeVoss, Jason, Driscoll, Jim, Eigenbrot, Charles, Ghilardi, Nico, Gibbons, Paul, Halladay, Jason, Johnson, Adam, Kohli, Pawan Bir, Lai, Yingjie, Liu, Yanzhou, Lyssikatos, Joseph, Mantik, Priscilla, Menghrajani, Kapil, Murray, Jeremy, Peng, Ivan, Sambrone, Amy, Shia, Steven, Shin, Young, Smith, Jan, Sohn, Sue, Tsui, Vickie, Ultsch, Mark, Wu, Lawren C, Xiao, Yisong, Yang, Wenqian, Young, Judy, Zhang, Birong, Zhu, Bing-yan, Magnuson, Steven

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Spirocyclic β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: From Hit to Lowering of Cerebrospinal Fluid (CSF) Amyloid β in a Higher Species von Hunt, Kevin W, Cook, Adam W, Watts, Ryan J, Clark, Christopher T, Vigers, Guy, Smith, Darin, Metcalf, Andrew T, Gunawardana, Indrani W, Burkard, Michael, Cox, April A, Geck Do, Mary K, Dutcher, Darrin, Thomas, Allen A, Rana, Sumeet, Kallan, Nicholas C, DeLisle, Robert K, Rizzi, James P, Regal, Kelly, Sammond, Douglas, Groneberg, Robert, Siu, Michael, Purkey, Hans, Lyssikatos, Joseph P, Marlow, Allison, Liu, Xingrong, Tang, Tony P

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Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors von Hu, Huiyong, Wang, Xiaojing, Chan, Grace Ka Yan, Chang, Jae H., Do, Steven, Drummond, Jake, Ebens, Allen, Lee, Wendy, Ly, Justin, Lyssikatos, Joseph P., Murray, Jeremy, Moffat, John G., Chao, Qi, Tsui, Vickie, Wallweber, Heidi, Kolesnikov, Aleksandr

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Design of Selective PAK1 Inhibitor G‑5555: Improving Properties by Employing an Unorthodox Low‑pK a Polar Moiety von Ndubaku, Chudi O, Crawford, James J, Drobnick, Joy, Aliagas, Ignacio, Campbell, David, Dong, Ping, Dornan, Laura M, Duron, Sergio, Epler, Jennifer, Gazzard, Lewis, Heise, Christopher E, Hoeflich, Klaus P, Jakubiak, Diana, La, Hank, Lee, Wendy, Lin, Baiwei, Lyssikatos, Joseph P, Maksimoska, Jasna, Marmorstein, Ronen, Murray, Lesley J, O’Brien, Thomas, Oh, Angela, Ramaswamy, Sreemathy, Wang, Weiru, Zhao, Xianrui, Zhong, Yu, Blackwood, Elizabeth, Rudolph, Joachim

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Germinal‐center kinase‐like kinase co‐crystal structure reveals a swapped activation loop and C‐terminal extension von Marcotte, Douglas, Rushe, Mia, M. Arduini, Robert, Lukacs, Christine, Atkins, Kateri, Sun, Xin, Little, Kevin, Cullivan, Michael, Paramasivam, Murugan, Patterson, Thomas A., Hesson, Thomas, D. McKee, Timothy, May‐Dracka, Tricia L., Xin, Zhili, Bertolotti‐Ciarlet, Andrea, Bhisetti, Govinda R., Lyssikatos, Joseph P., Silvian, Laura F.

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Discovery of Highly Potent, Selective, and Brain-Penetrable Leucine-Rich Repeat Kinase 2 (LRRK2) Small Molecule Inhibitors von Estrada, Anthony A, Liu, Xingrong, Baker-Glenn, Charles, Beresford, Alan, Burdick, Daniel J, Chambers, Mark, Chan, Bryan K, Chen, Huifen, Ding, Xiao, DiPasquale, Antonio G, Dominguez, Sara L, Dotson, Jennafer, Drummond, Jason, Flagella, Michael, Flynn, Sean, Fuji, Reina, Gill, Andrew, Gunzner-Toste, Janet, Harris, Seth F, Heffron, Timothy P, Kleinheinz, Tracy, Lee, Donna W, Le Pichon, Claire E, Lyssikatos, Joseph P, Medhurst, Andrew D, Moffat, John G, Mukund, Susmith, Nash, Kevin, Scearce-Levie, Kimberly, Sheng, Zejuan, Shore, Daniel G, Tran, Thuy, Trivedi, Naimisha, Wang, Shumei, Zhang, Shuo, Zhang, Xiaolin, Zhao, Guiling, Zhu, Haitao, Sweeney, Zachary K

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Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451 von ROBERTS, W. Gregory, WHALEN, Pamela M, ATHERTON, James A, RALSTON, Sherry, SZEWC, Ruby, KATH, John C, JING LIN, SODERSTROM, Cathy, TKALCEVIC, George, COHEN, Bruce D, POLLACK, Vince, BARTH, Wayne, SODERSTROM, Erik, HUNGERFORD, Will, UNG, Ethan, MORASKI, Garrett, LYSSIKATOS, Joseph P, WANG, Huifen-F, COOPER, Beth, BAKER, Deborah A, SAVAGE, Douglas, DALVIE, Deepak

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Discovery of 7‑Tetrahydropyran-2-yl Chromans: β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors That Reduce Amyloid β‑Protein (Aβ) in the Central Nervous System... von Thomas, Allen A, Hunt, Kevin W, Volgraf, Matthew, Watts, Ryan J, Liu, Xingrong, Vigers, Guy, Smith, Darin, Sammond, Douglas, Tang, Tony P, Rhodes, Susan P, Metcalf, Andrew T, Brown, Karin D, Otten, Jennifer N, Burkard, Michael, Cox, April A, Do, Mary K. Geck, Dutcher, Darrin, Rana, Sumeet, DeLisle, Robert K, Regal, Kelly, Wright, Albion D, Groneberg, Robert, Scearce-Levie, Kimberly, Siu, Michael, Purkey, Hans E, Lyssikatos, Joseph P, Gunawardana, Indrani W

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α-Aryl pyrrolidine sulfonamides as TRPA1 antagonists von Verma, Vishal A., Shore, Daniel G.M., Chen, Huifen, Chen, Jun, Do, Steven, Hackos, David H., Kolesnikov, Aleks, Lyssikatos, Joseph P., Tay, Suzanne, Wang, Lan, Estrada, Anthony A.

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