Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases von Caldwell, Richard D, Qiu, Hui, Askew, Ben C, Bender, Andrew T, Brugger, Nadia, Camps, Montserrat, Dhanabal, Mohanraj, Dutt, Vikram, Eichhorn, Thomas, Gardberg, Anna S, Goutopoulos, Andreas, Grenningloh, Roland, Head, Jared, Healey, Brian, Hodous, Brian L, Huck, Bayard R, Johnson, Theresa L, Jones, Christopher, Jones, Reinaldo C, Mochalkin, Igor, Morandi, Federica, Nguyen, Ngan, Meyring, Michael, Potnick, Justin R, Santos, Dusica Cvetinovic, Schmidt, Ralf, Sherer, Brian, Shutes, Adam, Urbahns, Klaus, Follis, Ariele Viacava, Wegener, Ansgar A, Zimmerli, Simone C, Liu-Bujalski, Lesley

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Abstract 2337: Recapitulating and targeting hypoxia-induced tumor metabolism using zebrafish tumor-derived xenografts-models von Rodriguez, Gabriela Vazquez, Ali, Zaheer, Vildevall, Malin, Erkstam, Anna, Goutopoulos, Andreas, Fahlgren, Anna, Jensen, Lasse D.

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Evidence for Follicle-stimulating Hormone Receptor as a Functional Trimer von Jiang, Xuliang, Fischer, David, Chen, Xiaoyan, McKenna, Sean D., Liu, Heli, Sriraman, Venkataraman, Yu, Henry N., Goutopoulos, Andreas, Arkinstall, Steve, He, Xiaolin

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Phase 1 first-in-human trial of MTB-9655, the first oral inhibitor of ACSS2, in patients with advanced solid tumors von Perets, Ruth, Geva, Ravit, McKean, Meredith, Goutopoulos, Andreas, Erez, Omri, Phadnis, Monica, Youssoufian, Hagop, Schwartz, Brian E., Kansra, Vikram, Fattaey, Ali

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Abstract LB-295: Discovery of potent selective oral ACSS2 inhibitors for the treatment of acetate avid tumors von Goutopoulos, Andreas, Erez, Omri, Nakache, Philippe, Alchanati, Iris, Hay-Koren, Avital, Paz, Dikla, Kovalerchik, Dimitri, Oppenheimer, Hannah, Gottlieb, Eyal, Botti, Simone, Mor, Inbal, Pastukh, Nina

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Identification of Clinical Candidate M2698, a Dual p70S6K and Akt Inhibitor, for Treatment of PAM Pathway-Altered Cancers von DeSelm, Lizbeth, Huck, Bayard, Lan, Ruoxi, Neagu, Constantin, Potnick, Justin, Xiao, Yufang, Chen, Xiaoling, Jones, Reinaldo, Richardson, Thomas E, Heasley, Brian H, Haxell, Thomas, Moore, Joseph, Tian, Hui, Georgi, Katrin, Rohdich, Felix, Sutton, Amanda, Johnson, Theresa, Mochalkin, Igor, Jackson, Jennifer, Lin, Jing, Crowley, Lindsey, Machl, Andreas, Clark, Anderson, Wilker, Erik, Sherer, Brian, Goutopoulos, Andreas

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Discovery of potent and selective reversible Bruton’s tyrosine kinase inhibitors von Qiu, Hui, Ali, Zahid, Bender, Andrew, Caldwell, Richard, Chen, Yi-Ying, Fang, Zhizhou, Gardberg, Anna, Glaser, Nina, Goettsche, Anja, Goutopoulos, Andreas, Grenningloh, Roland, Hanschke, Bettina, Head, Jared, Johnson, Theresa, Jones, Christopher, Jones, Reinaldo, Kulkarni, Shashank, Maurer, Christine, Morandi, Federica, Neagu, Constantin, Poetzsch, Sven, Potnick, Justin, Schmidt, Ralf, Roe, Katherine, Viacava Follis, Ariele, Wing, Carolyn, Zhu, Xiaohua, Sherer, Brian

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Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit von Qiu, Hui, Liu-Bujalski, Lesley, Caldwell, Richard D, Follis, Ariele Viacava, Gardberg, Anna, Goutopoulos, Andreas, Grenningloh, Roland, Head, Jared, Johnson, Theresa, Jones, Reinaldo, Mochalkin, Igor, Morandi, Federica, Neagu, Constantin, Sherer, Brian

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A phase 1 study of TPST-1120 as a single agent and in combination with nivolumab in subjects with advanced solid tumors von Yarchoan, Mark, Powderly, John D., Bastos, Bruno R., Karasic, Thomas Benjamin, Crysler, Oxana V., Munster, Pamela N., McKean, Meredith, Emens, Leisha A., Saenger, Yvonne M., Ged, Yasser, Stagg, Robert, Goutopoulos, Andreas, Moon, Anne, Jenkins, Yonchu, Prasit, Peppi, Dubensky, Thomas Walter, Whiting, Sam H., Ulahannan, Susanna Varkey

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Corrigendum to “Discovery of 4-aminopyrimidine analogs as highly potent dual P70S6K/Akt inhibitors” [Bioorgan. Med. Chem. Lett. 50 (2021) 128352] von Xiao, Yufang, Huck, Bayard R., Lan, Ruoxi, DeSelm, Lizbeth, Chen, Xiaoling, Qiu, Hui, Neagu, Constantin, Johnson, Theresa, Mochalkin, Igor, Gardberg, Anna, Jiang, Xuliang, Tian, Hui, Dutt, Vikram, Santos, Dusica, Head, Jared, Jackson, Jennifer, Syed, Sakeena, Lin, Jing, Wilker, Erik, Ma, Jianguo, Clark, Anderson, Machl, Andreas, Bankston, Donald, Jones, Christopher C.V., Goutopoulos, Andreas, Sherer, Brian

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Discovery of 4-aminopyrimidine analogs as highly potent dual P70S6K/Akt inhibitors von Xiao, Yufang, Huck, Bayard R., Lan, Ruoxi, DeSelm, Lizbeth, Chen, Xiaoling, Qiu, Hui, Neagu, Constantin, Johnson, Theresa, Mochalkin, Igor, Gardberg, Anna, Jiang, Xuliang, Tian, Hui, Dutt, Vikram, Santos, Dusica, Head, Jared, Jackson, Jennifer, Syed, Sakeena, Lin, Jing, Wilker, Erik, Ma, Jianguo, Clark, Anderson, Machl, Andreas, Bankston, Donald, Jones, Christopher C.V., Goutopoulos, Andreas, Sherer, Brian

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Synthesis and SAR development of quinoline analogs as novel P2X7 receptor antagonists von Xiao, Yufang, Karra, Srinivasa, Goutopoulos, Andreas, Morse, Noune Tahmassian, Zhang, Susan, Dhanabal, Mohanraj, Tian, Hui, Seenisamy, Jeyaprakashnarayanan, Jayadevan, Jayashankaran, Caldwell, Richard, Potnick, Justin, Bleich, Matthew, Chekler, Eugene, Sherer, Brian, Sriraman, Venkataraman

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Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk von Caldwell, Richard, Liu-Bujalski, Lesley, Qiu, Hui, Mochalkin, Igor, Jones, Reinaldo, Neagu, Constantin, Goutopoulos, Andreas, Grenningloh, Roland, Johnson, Theresa, Sherer, Brian, Gardberg, Anna, Follis, Ariele Viacava, Morandi, Federica, Head, Jared

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Discovery of Covalent Bruton's Tyrosine Kinase Inhibitors with Decreased CYP2C8 Inhibitory Activity von Qiu, Hui, Ali, Zahid, Bowlan, Julian, Caldwell, Richard, Gardberg, Anna, Glaser, Nina, Goutopoulos, Andreas, Head, Jared, Johnson, Theresa, Maurer, Christine, Georgi, Katrin, Grenningloh, Roland, Fang, Zhizhou, Morandi, Federica, Rohdich, Felix, Schmidt, Ralf, Follis, Ariele Viacava, Sherer, Brian

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From cannabis to cannabinergics: new therapeutic opportunities von Goutopoulos, Andreas, Makriyannis, Alexandros

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Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti‐myeloma activity in vitro and in vivo von Kim, Kihyun, Kong, Sun‐Young, Fulciniti, Mariateresa, Li, Xianfeng, Song, Weihua, Nahar, Sabikun, Burger, Peter, Rumizen, Mathew J., Podar, Klaus, Chauhan, Dharminder, Hideshima, Teru, Munshi, Nikhil C., Richardson, Paul, Clark, Ann, Ogden, Janet, Goutopoulos, Andreas, Rastelli, Luca, Anderson, Kenneth C., Tai, Yu‐Tzu

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Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors von Qiu, Hui, Liu-Bujalski, Lesley, Caldwell, Richard D., Viacava Follis, Ariele, Gardberg, Anna, Goutopoulos, Andreas, Grenningloh, Roland, Head, Jared, Johnson, Theresa, Jones, Christopher C.V., Jones, Reinaldo, Mochalkin, Igor, Morandi, Federica, Neagu, Constantin, Potnick, Justin, Sherer, Brian

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Abstract 1397: A phenotypic-based drug discovery approach against tumors with MTAP loss von Goutopoulos, Andreas, Amanati, Iris, Hay-Koren, Avital, Fattaey, Ali, Nakache, Philippe, Kovalerchik, Dimitri, Paz, Dikla, Botti, Simone, Oppenheimer, Hanna, Erez, Omri, Fainer, Irit

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Abstract 2326: Preclinical characterization of MTB-9655, a first-in-class, clinical stage ACSS2 inhibitor von Goutopoulos, Andreas, Amanati, Iris, Fattaey, Ali, Hay-Koren, Avital, Nakache, Philippe, Erez, Omri, Kovalerchik, Dimitri, Paz, Dikla, Botti, Simone, Oppenheimer, Hannah, Fainer, Irit

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Discovery of Affinity‐Based Probes for Btk Occupancy Assays von Qiu, Hui, Caldwell, Richard, Liu‐Bujalski, Lesley, Goutopoulos, Andreas, Jones, Reinaldo, Potnick, Justin, Sherer, Brian, Bender, Andrew, Grenningloh, Roland, Xu, Daigen, Gardberg, Anna, Mochalkin, Igor, Johnson, Theresa, Viacava Follis, Ariele, Head, Jared, Morandi, Federica

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