Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia
Tron, Adriana E, Belmonte, Matthew A, Adam, Ammar, Aquila, Brian M, Boise, Lawrence H, Chiarparin, Elisabetta, Cidado, Justin, Embrey, Kevin J, Gangl, Eric, Gibbons, Francis D, Gregory, Gareth P, Hargreaves, David, Hendricks, J Adam, Johannes, Jeffrey W, Johnstone, Ricky W, Kazmirski, Steven L, Kettle, Jason G, Lamb, Michelle L, Matulis, Shannon M, Nooka, Ajay K, Packer, Martin J, Peng, Bo, Rawlins, Philip B, Robbins, Daniel W, Schuller, Alwin G, Su, Nancy, Yang, Wenzhan, Ye, Qing, Zheng, Xiaolan, Secrist, J Paul, Clark, Edwin A, Wilson, David M, Fawell, Stephen E, Hird, Alexander W
Published in Nature communications (17.12.2018)
Published in Nature communications (17.12.2018)
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Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain
Akçay, Gizem, Belmonte, Matthew A, Aquila, Brian, Chuaqui, Claudio, Hird, Alexander W, Lamb, Michelle L, Rawlins, Philip B, Su, Nancy, Tentarelli, Sharon, Grimster, Neil P, Su, Qibin
Published in Nature chemical biology (01.11.2016)
Published in Nature chemical biology (01.11.2016)
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AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia
Keeton, Erika K., McEachern, Kristen, Dillman, Keith S., Palakurthi, Sangeetha, Cao, Yichen, Grondine, Michael R., Kaur, Surinder, Wang, Suping, Chen, Yuching, Wu, Allan, Shen, Minhui, Gibbons, Francis D., Lamb, Michelle L., Zheng, Xiaolan, Stone, Richard M., DeAngelo, Daniel J., Platanias, Leonidas C., Dakin, Les A., Chen, Huawei, Lyne, Paul D., Huszar, Dennis
Published in Blood (06.02.2014)
Published in Blood (06.02.2014)
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Ensemble-Based Docking Using Biased Molecular Dynamics
Campbell, Arthur J, Lamb, Michelle L, Joseph-McCarthy, Diane
Published in Journal of chemical information and modeling (28.07.2014)
Published in Journal of chemical information and modeling (28.07.2014)
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Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies
Barlaam, Bernard, Casella, Robert, Cidado, Justin, Cook, Calum, De Savi, Chris, Dishington, Allan, Donald, Craig S, Drew, Lisa, Ferguson, Andrew D, Ferguson, Douglas, Glossop, Steve, Grebe, Tyler, Gu, Chungang, Hande, Sudhir, Hawkins, Janet, Hird, Alexander W, Holmes, Jane, Horstick, James, Jiang, Yun, Lamb, Michelle L, McGuire, Thomas M, Moore, Jane E, O’Connell, Nichole, Pike, Andy, Pike, Kurt G, Proia, Theresa, Roberts, Bryan, San Martin, Maryann, Sarkar, Ujjal, Shao, Wenlin, Stead, Darren, Sumner, Neil, Thakur, Kumar, Vasbinder, Melissa M, Varnes, Jeffrey G, Wang, Jianyan, Wang, Lei, Wu, Dedong, Wu, Liangwei, Yang, Bin, Yao, Tieguang
Published in Journal of medicinal chemistry (24.12.2020)
Published in Journal of medicinal chemistry (24.12.2020)
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Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl‑1 Inhibitor (AZD5991) and Other Synthetic Macrocycles
Balazs, Amber Y. S, Carbajo, Rodrigo J, Davies, Nichola L, Dong, Yu, Hird, Alexander W, Johannes, Jeffrey W, Lamb, Michelle L, McCoull, William, Raubo, Piotr, Robb, Graeme R, Packer, Martin J, Chiarparin, Elisabetta
Published in Journal of medicinal chemistry (14.11.2019)
Published in Journal of medicinal chemistry (14.11.2019)
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Targeting adenosine A 2A receptor antagonism for treatment of cancer
Congreve, Miles, Brown, Giles A, Borodovsky, Alexandra, Lamb, Michelle L
Published in Expert opinion on drug discovery (02.11.2018)
Published in Expert opinion on drug discovery (02.11.2018)
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Discovery and Mechanistic Study of a Small Molecule Inhibitor for Motor Protein KIFC1
Wu, Jiaquan, Mikule, Keith, Wang, Wenxian, Su, Nancy, Petteruti, Philip, Gharahdaghi, Farzin, Code, Erin, Zhu, Xiahui, Jacques, Kelly, Lai, Zhongwu, Yang, Bin, Lamb, Michelle L, Chuaqui, Claudio, Keen, Nicholas, Chen, Huawei
Published in ACS chemical biology (18.10.2013)
Published in ACS chemical biology (18.10.2013)
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Journal Article
Structure-Based Optimization of a Series of Covalent, Cell Active Bfl‑1 Inhibitors
Lucas, Simon C. C., Blackwell, J. Henry, Börjesson, Ulf, Hargreaves, David, Milbradt, Alexander G., Bostock, Mark J., Ahmed, Samiyah, Beaumont, Kevin, Cheung, Tony, Demanze, Sylvain, Gohlke, Andrea, Guerot, Carine, Haider, Afreen, Kantae, Vasudev, Kauffman, Gregory W., Kinzel, Olaf, Kupcova, Lea, Lainchbury, Michael D., Lamb, Michelle L., Leon, Leonardo, Palisse, Adeline, Sacchetto, Claudia, Storer, R. Ian, Su, Nancy, Thomson, Clare, Vales, John, Chen, Yunhua, Hu, Xiaolong
Published in Journal of medicinal chemistry (26.09.2024)
Published in Journal of medicinal chemistry (26.09.2024)
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Accelerated Discovery of Carbamate Cbl‑b Inhibitors Using Generative AI Models and Structure-Based Drug Design
Quinn, Taylor R., Giblin, Kathryn A., Thomson, Clare, Boerth, Jeffrey A., Bommakanti, Gayathri, Braybrooke, Erin, Chan, Christina, Chinn, Alex J., Code, Erin, Cui, Caifeng, Fan, Yukai, Grimster, Neil P., Kohara, Keishi, Lamb, Michelle L., Ma, Lina, Mfuh, Adelphe M., Robb, Graeme R., Robbins, Kevin J., Schimpl, Marianne, Tang, Haoran, Ware, Jamie, Wrigley, Gail L., Xue, Lin, Zhang, Yun, Zhu, Huimin, Hughes, Samantha J.
Published in Journal of medicinal chemistry (22.08.2024)
Published in Journal of medicinal chemistry (22.08.2024)
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Design of a Lead-Like Cysteine-Targeting Covalent Library and the Identification of Hits to Cys55 of Bfl-1
Lucas, Simon C. C., Milbradt, Alexander G., Blackwell, J. Henry, Bonomo, Silvia, Brierley, Andrew, Cassar, Doyle J., Freeman, Jared, Hadfield, Thomas E., Morrill, Lucas A., Riemens, Rick, Sarda, Sunil, Schiesser, Stefan, Wiktelius, Daniel, Ahmed, Samiyah, Bostock, Mark J., Börjesson, Ulf, De Fusco, Claudia, Guerot, Carine, Hargreaves, David, Hewitt, Sarah, Lamb, Michelle L., Su, Nancy, Whatling, Ryan, Wheeler, Matthew, Kettle, Jason G.
Published in Journal of medicinal chemistry (11.07.2024)
Published in Journal of medicinal chemistry (11.07.2024)
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Discovery and Optimization of the First ATP Competitive Type-III c‑MET Inhibitor
Michaelides, Iacovos N., Collie, Gavin W., Börjesson, Ulf, Vasalou, Christina, Alkhatib, Omar, Barlind, Louise, Cheung, Tony, Dale, Ian L., Embrey, Kevin J., Hennessy, Edward J., Khurana, Puneet, Koh, Cheryl M., Lamb, Michelle L., Liu, Jianming, Moss, Thomas A., O’Neill, Daniel J., Phillips, Christopher, Shaw, Joseph, Snijder, Arjan, Storer, R. Ian, Stubbs, Christopher J., Han, Fujin, Li, Chengzhi, Qiao, Jingchuan, Sun, Dong-Qing, Wang, Jingwen, Wang, Peng, Yang, Wenzhen
Published in Journal of medicinal chemistry (13.07.2023)
Published in Journal of medicinal chemistry (13.07.2023)
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Journal Article
Discovery of a Series of 7‑Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement
Barlaam, Bernard, De Savi, Chris, Dishington, Allan, Drew, Lisa, Ferguson, Andrew D, Ferguson, Douglas, Gu, Chungang, Hande, Sudhir, Hassall, Lorraine, Hawkins, Janet, Hird, Alexander W, Holmes, Jane, Lamb, Michelle L, Lister, Andrew S, McGuire, Thomas M, Moore, Jane E, O’Connell, Nichole, Patel, Anil, Pike, Kurt G, Sarkar, Ujjal, Shao, Wenlin, Stead, Darren, Varnes, Jeffrey G, Vasbinder, Melissa M, Wang, Lei, Wu, Liangwei, Xue, Lin, Yang, Bin, Yao, Tieguang
Published in Journal of medicinal chemistry (28.10.2021)
Published in Journal of medicinal chemistry (28.10.2021)
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Journal Article
Deconvoluting Kinase Inhibitor Induced Cardiotoxicity
Lamore, Sarah D, Ahlberg, Ernst, Boyer, Scott, Lamb, Michelle L, Hortigon-Vinagre, Maria P, Rodriguez, Victor, Smith, Godfrey L, Sagemark, Johanna, Carlsson, Lars, Bates, Stephanie M, Choy, Allison L, Stålring, Jonna, Scott, Clay W, Peters, Matthew F
Published in Toxicological sciences (01.07.2017)
Published in Toxicological sciences (01.07.2017)
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Pharmacological Inhibition of PARP6 Triggers Multipolar Spindle Formation and Elicits Therapeutic Effects in Breast Cancer
Wang, Zebin, Grosskurth, Shaun E, Cheung, Tony, Petteruti, Philip, Zhang, Jingwen, Wang, Xin, Wang, Wenxian, Gharahdaghi, Farzin, Wu, Jiaquan, Su, Nancy, Howard, Ryan T, Mayo, Michele, Widzowski, Dan, Scott, David A, Johannes, Jeffrey W, Lamb, Michelle L, Lawson, Deborah, Dry, Jonathan R, Lyne, Paul D, Tate, Edward W, Zinda, Michael, Mikule, Keith, Fawell, Stephen E, Reimer, Corinne, Chen, Huawei
Published in Cancer research (Chicago, Ill.) (01.12.2018)
Published in Cancer research (Chicago, Ill.) (01.12.2018)
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Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases
Dakin, Les A., Block, Michael H., Chen, Huawei, Code, Erin, Dowling, James E., Feng, Xiaomei, Ferguson, Andrew D., Green, Isabelle, Hird, Alexander W., Howard, Tina, Keeton, Erika K., Lamb, Michelle L., Lyne, Paul D., Pollard, Hannah, Read, Jon, Wu, Allan J., Zhang, Tao, Zheng, Xiaolan
Published in Bioorganic & medicinal chemistry letters (15.07.2012)
Published in Bioorganic & medicinal chemistry letters (15.07.2012)
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Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl‑b Inhibitors
Mfuh, Adelphe M., Boerth, Jeffrey A., Bommakanti, Gayathri, Chan, Christina, Chinn, Alex J., Code, Erin, Fricke, Patrick J., Giblin, Kathryn A., Gohlke, Andrea, Hansel, Catherine, Hariparsad, Niresh, Hughes, Samantha J., Jin, Meizhong, Kantae, Vasudev, Kavanagh, Stefan L., Lamb, Michelle L., Lane, Jordan, Moore, Rachel, Puri, Taranee, Quinn, Taylor R., Reddy, Iswarya, Robb, Graeme R., Robbins, Kevin J., Gancedo Rodrigo, Miguel, Schimpl, Marianne, Singh, Baljinder, Singh, Meha, Tang, Haoran, Thomson, Clare, Walsh, Jarrod J., Ware, Jamie, Watson, Iain D. G., Ye, Min-Wei, Wrigley, Gail L., Zhang, Andrew X., Zhang, Yun, Grimster, Neil P.
Published in Journal of medicinal chemistry (25.01.2024)
Published in Journal of medicinal chemistry (25.01.2024)
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Discovery of 5-Chloro-N 2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N 4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a Novel Inhibitor of the Jak/Stat Pathway
Ioannidis, Stephanos, Lamb, Michelle L, Wang, Tao, Almeida, Lynsie, Block, Michael H, Davies, Audrey M, Peng, Bo, Su, Mei, Zhang, Hai-Jun, Hoffmann, Ethan, Rivard, Caroline, Green, Isabelle, Howard, Tina, Pollard, Hannah, Read, Jon, Alimzhanov, Marat, Bebernitz, Geraldine, Bell, Kirsten, Ye, Minwei, Huszar, Dennis, Zinda, Michael
Published in Journal of medicinal chemistry (13.01.2011)
Published in Journal of medicinal chemistry (13.01.2011)
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