Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton’s Tyrosine Kinase Inhibitor in Early Clinical Development von Crawford, James J, Johnson, Adam R, Misner, Dinah L, Belmont, Lisa D, Castanedo, Georgette, Choy, Regina, Coraggio, Melis, Dong, Liming, Eigenbrot, Charles, Erickson, Rebecca, Ghilardi, Nico, Hau, Jonathan, Katewa, Arna, Kohli, Pawan Bir, Lee, Wendy, Lubach, Joseph W, McKenzie, Brent S, Ortwine, Daniel F, Schutt, Leah, Tay, Suzanne, Wei, BinQing, Reif, Karin, Liu, Lichuan, Wong, Harvey, Young, Wendy B

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Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy von Dragovich, Peter S, Pillow, Thomas H, Blake, Robert A, Sadowsky, Jack D, Adaligil, Emel, Adhikari, Pragya, Chen, Jinhua, Corr, Nicholas, dela Cruz-Chuh, Josefa, Del Rosario, Geoffrey, Fullerton, Aaron, Hartman, Steven J, Jiang, Fan, Kaufman, Susan, Kleinheinz, Tracy, Kozak, Katherine R, Liu, Liling, Lu, Ying, Mulvihill, Melinda M, Murray, Jeremy M, O’Donohue, Aimee, Rowntree, Rebecca K, Sawyer, William S, Staben, Leanna R, Wai, John, Wang, Jian, Wei, BinQing, Wei, Wentao, Xu, Zijin, Yao, Hui, Yu, Shang-Fan, Zhang, Donglu, Zhang, Hongyan, Zhang, Shenhua, Zhao, Yongxin, Zhou, Hao, Zhu, Xiaoyu

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Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties von Dragovich, Peter S, Pillow, Thomas H, Blake, Robert A, Sadowsky, Jack D, Adaligil, Emel, Adhikari, Pragya, Bhakta, Sunil, Blaquiere, Nicole, Chen, Jinhua, dela Cruz-Chuh, Josefa, Gascoigne, Karen E, Hartman, Steven J, He, Mingtao, Kaufman, Susan, Kleinheinz, Tracy, Kozak, Katherine R, Liu, Liang, Liu, Liling, Liu, Qi, Lu, Ying, Meng, Fanwei, Mulvihill, Melinda M, O’Donohue, Aimee, Rowntree, Rebecca K, Staben, Leanna R, Staben, Steven T, Wai, John, Wang, Jian, Wei, BinQing, Wilson, Catherine, Xin, Jianfeng, Xu, Zijin, Yao, Hui, Zhang, Donglu, Zhang, Hongyan, Zhou, Hao, Zhu, Xiaoyu

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Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition von Boudreau, Aaron, Purkey, Hans E, Hitz, Anna, Robarge, Kirk, Peterson, David, Labadie, Sharada, Kwong, Mandy, Hong, Rebecca, Gao, Min, Del Nagro, Christopher, Pusapati, Raju, Ma, Shuguang, Salphati, Laurent, Pang, Jodie, Zhou, Aihe, Lai, Tommy, Li, Yingjie, Chen, Zhongguo, Wei, Binqing, Yen, Ivana, Sideris, Steve, McCleland, Mark, Firestein, Ron, Corson, Laura, Vanderbilt, Alex, Williams, Simon, Daemen, Anneleen, Belvin, Marcia, Eigenbrot, Charles, Jackson, Peter K, Malek, Shiva, Hatzivassiliou, Georgia, Sampath, Deepak, Evangelista, Marie, O'Brien, Thomas

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A Second Fatty Acid Amide Hydrolase with Variable Distribution among Placental Mammals von Wei, Binqing Q., Mikkelsen, Tarjei S., McKinney, Michele K., Lander, Eric S., Cravatt, Benjamin F.

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High-Throughput Cysteine Scanning To Identify Stable Antibody Conjugation Sites for Maleimide- and Disulfide-Based Linkers von Ohri, Rachana, Bhakta, Sunil, Fourie-O’Donohue, Aimee, dela Cruz-Chuh, Josefa, Tsai, Siao Ping, Cook, Ryan, Wei, Binqing, Ng, Carl, Wong, Athena W, Bos, Aaron B, Farahi, Farzam, Bhakta, Jiten, Pillow, Thomas H, Raab, Helga, Vandlen, Richard, Polakis, Paul, Liu, Yichin, Erickson, Hans, Junutula, Jagath R, Kozak, Katherine R

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Targeted drug delivery through the traceless release of tertiary and heteroaryl amines from antibody–drug conjugates von Staben, Leanna R., Koenig, Stefan G., Lehar, Sophie M., Vandlen, Richard, Zhang, Donglu, Chuh, Josefa, Yu, Shang-Fan, Ng, Carl, Guo, Jun, Liu, Yanzhou, Fourie-O'Donohue, Aimee, Go, MaryAnn, Linghu, Xin, Segraves, Nathaniel L., Wang, Tao, Chen, Jinhua, Wei, BinQing, Phillips, Gail D. Lewis, Xu, Keyang, Kozak, Katherine R., Mariathasan, Sanjeev, Flygare, John A., Pillow, Thomas H.

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The HER2-directed antibody-drug conjugate DHES0815A in advanced and/or metastatic breast cancer: preclinical characterization and phase 1 trial results von Lewis, Gail D., Li, Guangmin, Guo, Jun, Yu, Shang-Fan, Fields, Carter T., Lee, Genee, Zhang, Donglu, Dragovich, Peter S., Pillow, Thomas, Wei, BinQing, Sadowsky, Jack, Leipold, Douglas, Wilson, Tim, Kamath, Amrita, Mamounas, Michael, Lee, M. Violet, Saad, Ola, Choeurng, Voleak, Ungewickell, Alexander, Monemi, Sharareh, Crocker, Lisa, Kalinsky, Kevin, Modi, Shanu, Jung, Kyung Hae, Hamilton, Erika, LoRusso, Patricia, Krop, Ian, Schutten, Melissa M., Commerford, Renee, Sliwkowski, Mark X., Cho, Eunpi

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Soft Docking and Multiple Receptor Conformations in Virtual Screening von Ferrari, Anna Maria, Wei, Binqing Q, Costantino, Luca, Shoichet, Brian K

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Systematic Variation of Pyrrolobenzodiazepine (PBD)-Dimer Payload Physicochemical Properties Impacts Efficacy and Tolerability of the Corresponding Antibody–Drug Conjugates von Staben, Leanna R, Chen, Jinhua, Cruz-Chuh, Josefa dela, del Rosario, Geoff, Go, Mary Ann, Guo, Jun, Khojasteh, S. Cyrus, Kozak, Katherine R, Li, Guangmin, Ng, Carl, Lewis Phillips, Gail D, Pillow, Thomas H, Rowntree, Rebecca K, Wai, John, Wei, BinQing, Xu, Keyang, Xu, Zijin, Yu, Shang-Fan, Zhang, Donglu, Dragovich, Peter S

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Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase von Dragovich, Peter S., Fauber, Benjamin P., Corson, Laura B., Ding, Charles Z., Eigenbrot, Charles, Ge, HongXiu, Giannetti, Anthony M., Hunsaker, Thomas, Labadie, Sharada, Liu, Yichin, Malek, Shiva, Pan, Borlan, Peterson, David, Pitts, Keith, Purkey, Hans E., Sideris, Steve, Ultsch, Mark, VanderPorten, Erica, Wei, BinQing, Xu, Qing, Yen, Ivana, Yue, Qin, Zhang, Huihui, Zhang, Xuying

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Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase von Fauber, Benjamin P., Dragovich, Peter S., Chen, Jinhua, Corson, Laura B., Ding, Charles Z., Eigenbrot, Charles, Giannetti, Anthony M., Hunsaker, Thomas, Labadie, Sharada, Liu, Yichin, Liu, Yingchun, Malek, Shiva, Peterson, David, Pitts, Keith, Sideris, Steve, Ultsch, Mark, VanderPorten, Erica, Wang, Jing, Wei, BinQing, Yen, Ivana, Yue, Qin

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Testing a Flexible-receptor Docking Algorithm in a Model Binding Site von Wei, Binqing Q., Weaver, Larry H., Ferrari, Anna M., Matthews, Brian W., Shoichet, Brian K.

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Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf von Sutherlin, Daniel P., Baker, Stewart, Bisconte, Angelina, Blaney, Paul M., Brown, Anthony, Chan, Bryan K., Chantry, David, Castanedo, Georgette, DePledge, Paul, Goldsmith, Paul, Goldstein, David M., Hancox, Timothy, Kaur, Jasmit, Knowles, David, Kondru, Rama, Lesnick, John, Lucas, Matthew C., Lewis, Cristina, Murray, Jeremy, Nadin, Alan J., Nonomiya, Jim, Pang, Jodie, Pegg, Neil, Price, Steve, Reif, Karin, Safina, Brian S., Salphati, Laurent, Staben, Steven, Seward, Eileen M., Shuttleworth, Stephen, Sohal, Sukhjit, Sweeney, Zachary K., Ultsch, Mark, Waszkowycz, Bohdan, Wei, Binqing

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A Model Binding Site for Testing Scoring Functions in Molecular Docking von Wei, Binqing Q., Baase, Walter A., Weaver, Larry H., Matthews, Brian W., Shoichet, Brian K.

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A streamlined platform for high-content functional proteomics of primary human specimens von Jessani, Nadim, Niessen, Sherry, Wei, BinQing Q, Nicolau, Monica, Humphrey, Mark, Ji, Youngran, Han, Wonshik, Noh, Dong-Young, Yates, John R, Jeffrey, Stefanie S, Cravatt, Benjamin F

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Structure-based Inhibitor Discovery against Adenylyl Cyclase Toxins from Pathogenic Bacteria That Cause Anthrax and Whooping Cough von Soelaiman, Sandriyana, Wei, Binqing Q., Bergson, Pamela, Lee, Young-Sam, Shen, Yuequan, Mrksich, Milan, Shoichet, Brian K., Tang, Wei-Jen

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Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα) von Dragovich, Peter S., Adhikari, Pragya, Blake, Robert A., Blaquiere, Nicole, Chen, Jinhua, Cheng, Yun-Xing, den Besten, Willem, Han, Jinping, Hartman, Steven J., He, Jintang, He, Mingtao, Rei Ingalla, Ellen, Kamath, Amrita V., Kleinheinz, Tracy, Lai, Tommy, Leipold, Douglas D., Li, Chun Sing, Liu, Qi, Lu, Jiawei, Lu, Ying, Meng, Fanwei, Meng, Lingyao, Ng, Carl, Peng, Kaishan, Lewis Phillips, Gail, Pillow, Thomas H., Rowntree, Rebecca K., Sadowsky, Jack D., Sampath, Deepak, Staben, Leanna, Staben, Steven T., Wai, John, Wan, Kunpeng, Wang, Xinxin, Wei, BinQing, Wertz, Ingrid E., Xin, Jianfeng, Xu, Keyang, Yao, Hui, Zang, Richard, Zhang, Donglu, Zhou, Hao, Zhao, Yongxin

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Discovery of a Potent, Selective, and Orally Available Class I Phosphatidylinositol 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor (GDC-0980) for the Treatme... von Sutherlin, Daniel P, Bao, Linda, Berry, Megan, Castanedo, Georgette, Chuckowree, Irina, Dotson, Jenna, Folks, Adrian, Friedman, Lori, Goldsmith, Richard, Gunzner, Janet, Heffron, Timothy, Lesnick, John, Lewis, Cristina, Mathieu, Simon, Murray, Jeremy, Nonomiya, Jim, Pang, Jodie, Pegg, Niel, Prior, Wei Wei, Rouge, Lionel, Salphati, Laurent, Sampath, Deepak, Tian, Qingping, Tsui, Vickie, Wan, Nan Chi, Wang, Shumei, Wei, BinQing, Wiesmann, Christian, Wu, Ping, Zhu, Bing-Yan, Olivero, Alan

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Discovery of 2‑{3-[2-(1-Isopropyl-3-methyl‑1H‑1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2‑d][1,4]oxazepin-9-yl]‑1H‑pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β‑Sparing... von Ndubaku, Chudi O, Heffron, Timothy P, Staben, Steven T, Baumgardner, Matthew, Blaquiere, Nicole, Bradley, Erin, Bull, Richard, Do, Steven, Dotson, Jennafer, Dudley, Danette, Edgar, Kyle A, Friedman, Lori S, Goldsmith, Richard, Heald, Robert A, Kolesnikov, Aleksandr, Lee, Leslie, Lewis, Cristina, Nannini, Michelle, Nonomiya, Jim, Pang, Jodie, Price, Steve, Prior, Wei Wei, Salphati, Laurent, Sideris, Steve, Wallin, Jeffery J, Wang, Lan, Wei, BinQing, Sampath, Deepak, Olivero, Alan G

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