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Discovery of GNE-6893, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of HPK1 Tellis, John C.; Wei, BinQing; Siu, Michael; An, Le; Chan, Grace Kayan; Chen, Yong; Du, Xiangnan; Gazzard, Lewis; Hu, Baihua; Kiefer, James; Kakiuchi-Kiyota, Satoko; Lainchbury, Michael; Linehan, Jonathan L.; Luo, Xifeng; Malhotra, Sushant; Mendonca, Rohan; Pang, Jodie; Ran, Yinqing; Sethuraman, Vijay; Seward, Eileen; Sneeringer, Chris; Su, Dian; Wang, Weiru; Wu, Ping; Moffat, John G.; Heffron, Timothy P.; Choo, Edna F.; Chan, Bryan K. 分享 收藏
Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model Braun, Marie-Gabrielle; Ashkenazi, Avi; Beveridge, Ramsay E.; Castanedo, Georgette; Wallweber, Heidi Ackerly; Beresini, Maureen H.; Clark, Kevin R.; De Bruyn, Tom; Fu, Liqiang; Gibbons, Paul; Jiang, Fan; Kaufman, Susan; Kan, David; Kiefer, James R.; Leclerc, Jean-Philippe; Lemire, Alexandre; Ly, Cuong; Segal, Ehud; Sims, Jessica; Wang, Weiru; Wei, Wentao; Zhao, Liang; Schwarz, Jacob B.; Rudolph, Joachim 分享 收藏
Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα Hanan, Emily J.; Braun, Marie-Gabrielle; Heald, Robert A.; MacLeod, Calum; Chan, Connie; Clausen, Saundra; Edgar, Kyle A.; Eigenbrot, Charles; Elliott, Richard; Endres, Nicholas; Friedman, Lori S.; Gogol, Emily; Gu, Xiao-Hui; Thibodeau, Rebecca Hong; Jackson, Philip S.; Kiefer, James R.; Knight, Jamie D.; Nannini, Michelle; Narukulla, Raman; Pace, Amanda; Pang, Jodie; Purkey, Hans E.; Salphati, Laurent; Sampath, Deepak; Schmidt, Stephen; Sideris, Steve; Song, Kyung; Sujatha-Bhaskar, Swathi; Ultsch, Mark; Wallweber, Heidi; Xin, Jianfeng; Yeap, SiewKuen; Young, Amy; Zhong, Yu; Staben, Steven T. 分享 收藏
Correction to: Preclinical development of ZED8, an 89Zr immuno-PET reagent for monitoring tumor CD8 status in patients undergoing cancer immunotherapy Ogasawara, Annie; Kiefer, James R.; Gill, Herman; Chiang, Eugene; Sriraman, Shravan; Ferl, Gregory Z.; Ziai, James; Bohorquez, Sandra Sanabria; Guelman, Sebastian; Wang, Xiangdan; Yang, Jihong; Phan, Minh Michael; Nguyen, Van; Chung, Shan; Yu, Christine; Tinianow, Jeff; Waaijer, Stijn Jan Hein; De Crespigny, Alex; Marik, Jan; Boswell, C. Andrew; Zabka, Tanja; Staflin, Karin; Williams, Simon-Peter 分享 收藏
Development of an 18F-labeled anti-human CD8 VHH for same-day immunoPET imaging Sriraman, Shravan Kumar; Davies, Christopher W.; Gill, Herman; Kiefer, James R.; Yin, Jianping; Ogasawara, Annie; Urrutia, Alejandra; Javinal, Vincent; Lin, Zhonghua; Seshasayee, Dhaya; Abraham, Ryan; Haas, Phil; Koth, Christopher; Marik, Jan; Koerber, James T.; Williams, Simon Peter 分享 收藏
Preclinical development of ZED8, an 89Zr immuno-PET reagent for monitoring tumor CD8 status in patients undergoing cancer immunotherapy Ogasawara, Annie; Kiefer, James R.; Gill, Herman; Chiang, Eugene; Sriraman, Shravan; Ferl, Gregory Z.; Ziai, James; Bohorquez, Sandra Sanabria; Guelman, Sebastian; Wang, Xiangdan; Yang, Jihong; Phan, Minh Michael; Van Nguyen; Chung, Shan; Yu, Christine; Tinianow, Jeff; Waaijer, Stijn Jan Hein; De Crespigny, Alex; Marik, Jan; Boswell, C. Andrew; Zabka, Tanja; Staflin, Karin; Williams, Simon-Peter 分享 收藏
A BCMA/CD16A bispecific innate cell engager for the treatment of multiple myeloma Kakiuchi-Kiyota, Satoko; Ross, Thorsten; Wallweber, Heidi Ackerly; Kiefer, James R.; Schutten, Melissa M.; Adedeji, Adeyemi O.; Cai, Hao; Hendricks, Robert; Cohen, Sivan; Myneni, Srividya; Liu, Luna; Fullerton, Aaron; Corr, Nicholas; Yu, Lanlan; Nagata, Denise de Almeida; Zhong, Shelly; Leong, Steven R.; Li, Ji; Nakamura, Rin; Sumiyoshi, Teiko; Li, Jinze; Ovacik, Ayse Meric; Zheng, Bing; Dillon, Mike; Spiess, Christoph; Wingert, Susanne; Rajkovic, Erich; Ellwanger, Kristina; Reusch, Uwe; Polson, Andrew G. 分享 收藏
Target 2035-update on the quest for a probe for every protein Mueller, Susanne; Ackloo, Suzanne; Al Chawaf, Arij; Al-Lazikani, Bissan; Antolin, Albert; Baell, Jonathan B.; Beck, Hartmut; Beedie, Shaunna; Betz, Ulrich A. K.; Bezerra, Gustavo Arruda; Brennan, Paul E.; Brown, David; Brown, Peter J.; Bullock, Alex N.; Carter, Adrian J.; Chaikuad, Apirat; Chaineau, Mathilde; Ciulli, Alessio; Collins, Ian; Dreher, Jan; Drewry, David; Edfeldt, Kristina; Edwards, Aled M.; Egner, Ursula; Frye, Stephen, V; Fuchs, Stephen M.; Hall, Matthew D.; Hartung, Ingo, V; Hillisch, Alexander; Hitchcock, Stephen H.; Homan, Evert; Kannan, Natarajan; Kiefer, James R.; Knapp, Stefan; Kostic, Milka; Kubicek, Stefan; Leach, Andrew R.; Lindemann, Sven; Marsden, Brian D.; Matsui, Hisanori; Meier, Jordan L.; Merk, Daniel; Michel, Maurice; Morgan, Maxwell R.; Mueller-Fahrnow, Anke; Owen, Dafydd R.; Perry, Benjamin G.; Rosenberg, Saul H.; Saikatendu, Kumar Singh; Schapira, Matthieu; Scholten, Cora; Sharma, Sujata; Simeonov, Anton; Sundstrom, Michael; Superti-Furga, Giulio; Todd, Matthew H.; Tredup, Claudia; Vedadi, Masoud; von Delft, Frank; Willson, Timothy M.; Winter, Georg E.; Workman, Paul; Arrowsmith, Cheryl H. 分享 收藏
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GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER plus Breast Cancer Liang, Jun; Zbieg, Jason R.; Blake, Robert A.; Chang, Jae H.; Daly, Stephen; DiPasquale, Antonio G.; Friedman, Lori S.; Gelzleichter, Thomas; Gill, Matthew; Giltnane, Jennifer M.; Goodacre, Simon; Guan, Jane; Hartman, Steven J.; Ingalla, Ellen Rei; Kategaya, Lorn; Kiefer, James R.; Kleinheinz, Tracy; Labadie, Sharada S.; Lai, Tommy; Li, Jun; Liao, Jiangpeng; Liu, Zhiguo; Mody, Vidhi; McLean, Neville; Metcalfe, Ciara; Nannini, Michelle A.; Oeh, Jason; O'Rourke, Martin G.; Ortwine, Daniel F.; Ran, Yingqing; Ray, Nicholas C.; Roussel, Fabien; Sambrone, Amy; Sampath, Deepak; Schutt, Leah K.; Vinogradova, Maia; Wai, John; Wang, Tao; Wertz, Ingrid E.; White, Jonathan R.; Yeap, Siew Kuen; Young, Amy; Zhang, Birong; Zheng, Xiaoping; Zhou, Wei; Zhong, Yu; Wang, Xiaojing 分享 收藏
Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity Crawford, James J.; Lee, Wendy; Johnson, Adam R.; Delatorre, Kelly J.; Chen, Jacob; Eigenbrot, Charles; Heidmann, Julia; Kakiuchi-Kiyota, Satoko; Katewa, Arna; Kiefer, James R.; Liu, Lichuan; Lubach, Joseph W.; Misner, Dinah; Purkey, Hans; Reif, Karin; Vogt, Jennifer; Wong, Harvey; Yu, Christine; Young, Wendy B. 分享 收藏
The kinase IRAK4 promotes endosomal TLR and immune complex signaling in B cells and plasmacytoid dendritic cells Corzo, Cesar A.; Varfolomeev, Eugene; Setiadi, A. Francesca; Francis, Ross; Klabunde, Sha; Senger, Kate; Sujatha-Bhaskar, Swathi; Drobnick, Joy; Do, Steven; Suto, Eric; Huang, Zhiyu; Eastham-Anderson, Jeffrey; Katewa, Arna; Pang, Jodie; Domeyer, Melanie; Dela Cruz, Christopher; Paler-Martinez, Andres; Lau, Vivian W. C.; Hadadianpour, Azadeh; Ramirez-Carrozi, Vladimir; Sun, Yonglian; Bao, Katherine; Xu, Daqi; Hunley, Emily; Brightbill, Hans D.; Warming, Soren; Roose-Girma, Merone; Wong, Alfred; Tam, Lucinda; Emson, Claire L.; Crawford, James J.; Young, Wendy B.; Pappu, Rajita; McKenzie, Brent S.; Asghari, Vida; Vucic, Domagoj; Hackney, Jason A.; Austin, Cary D.; Lee, Wyne P.; Lekkerkerker, Annemarie; Ghilardi, Nico; Bryan, Marian C.; Kiefer, James R.; Townsend, Michael J.; Zarrin, Ali A. 分享 收藏
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER plus Breast Cancer Liang, Jun; Blake, Robert; Chang, Jae; Friedman, Lori S.; Goodacre, Simon; Hartman, Steven; Ingalla, Ellen Rei; Kiefer, James R.; Kleinheinz, Tracy; Labadie, Sharada; Li, Jun; Lai, Kwong Wah; Liao, Jiangpeng; Mody, Vidhi; McLean, Neville; Metcalfe, Ciara; Nannini, Michelle; Ortwine, Daniel; Ran, Yingqing; Ray, Nick; Roussel, Fabien; Sambrone, Amy; Sampath, Deepak; Vinogradova, Maia; Wai, John; Wang, Tao; Yeap, Kuen; Young, Amy; Zbieg, Jason; Zhang, Birong; Zheng, Xiaoping; Zhong, Yu; Wang, Xiaojing 分享 收藏
Discovery of Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity 发现具有强大体内活性的强效苯并内酰胺IRAK4抑制剂 Rajapaksa, Naomi S.; Gobbi, Alberto; Drobnick, Joy; Do, Steven; Kolesnikov, Aleksandr; Liang, Jun; Chen, Yongsheng; Sujatha-Bhaskar, Swathi; Huang, Zhiyu; Brightbill, Hans; Francis, Ross; Yu, Christine; Choo, Edna F.; DeMent, Kevin; Ran, Yingqing; An, Le; Emson, Claire; Maher, Jonathan; Wai, John; McKenzie, Brent S.; Lupardus, Patrick J.; Zarrin, Ali A.; Kiefer, James R.; Bryan, Marian C. 分享 收藏
Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors Bryan, Marian C.; Drobnick, Joy; Gobbi, Alberto; Kolesnikov, Aleksandr; Chen, Yongsheng; Rajapaksa, Naomi; Ndubaku, Chudi; Feng, Jianwen; Chang, Willy; Francis, Ross; Yu, Christine; Choo, Edna F.; DeMent, Kevin; Ran, Yingqing; An, Le; Emson, Claire; Huang, Zhiyu; Sujatha-Bhaskar, Swathi; Brightbill, Hans; DiPasquale, Antonio; Maher, Jonathan; Wai, John; McKenzie, Brent S.; Lupardus, Patrick J.; Zarrin, Ali A.; Kiefer, James R. 分享 收藏
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Water molecules in protein-ligand interfaces. Evaluation of software tools and SAR comparison Nittinger, Eva; Gibbons, Paul; Eigenbrot, Charles; Davies, Doug R.; Maurer, Brigitte; Yu, Christine L.; Kiefer, James R.; Kuglstatter, Andreas; Murray, Jeremy; Ortwine, Daniel F.; Tang, Yong; Tsui, Vickie 分享 收藏
Discovery of 3-Cyano-N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-5-yObenzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor Related Orphan Receptor C2 Inverse Agonist Schnute, Mark E.; Wennerstal, Mattias; Alley, Jennifer; Bengtsson, Martin; Blinn, James R.; Bolten, Charles W.; Braden, Timothy; Bonn, Tomas; Carlsson, Bo; Caspers, Nicole; Chen, Ming; Choi, Chulho; Collis, Leon P.; Crouse, Kimberly; Farnegardh, Mathias; Fennell, Kimberly F.; Fish, Susan; Flick, Andrew C.; Goos-Nilsson, Annika; Gullberg, Hjalmar; Harris, Peter K.; Heasley, Steven E.; Hegen, Martin; Hromockyj, Alexander E.; Hu, Xiao; Husman, Bolette; Janosik, Tomasz; Jones, Peter; Kaila, Neelu; Kallin, Elisabet; Kauppi, Bjorn; Kiefer, James R.; Knafels, John; Koehler, Konrad; Kruger, Lars; Kurumbail, Ravi G.; Kyne, Robert E., Jr.; Li, Wei; Lofstedt, Joakim; Long, Scott A.; Menard, Carol A.; Mente, Scot; Messing, Dean; Meyers, Marvin J.; Napierata, Lee; Noteberg, Daniel; Nuhant, Philippe; Pelc, Matthew J.; Prinsen, Michael J.; Rhonnstad, Patrik; Backstrom-Rydin, Eva; Sandberg, Johnny; Sandstrom, Maria; Shah, Falgun; Sjoberg, Maria; Sundell, Aron; Taylor, Alexandria P.; Thorarensen, Atli; Trujillo, John I.; Trzupek, John D.; Unwalla, Ray; Vajdos, Felix F.; Weinberg, Robin A.; Wood, David C.; Xing, Li; Zamaratski, Edouard; Zapf, Christoph W.; Zhao, Yajuan; Wilhelmsson, Anna; Berstein, Gabriel 分享 收藏
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