Potent and selective bivalent inhibitors of BET bromodomains
Waring, Michael J, Chen, Huawei, Rabow, Alfred A, Walker, Graeme, Bobby, Romel, Boiko, Scott, Bradbury, Rob H, Callis, Rowena, Clark, Edwin, Dale, Ian, Daniels, Danette L, Dulak, Austin, Flavell, Liz, Holdgate, Geoff, Jowitt, Thomas A, Kikhney, Alexey, McAlister, Mark, Méndez, Jacqui, Ogg, Derek, Patel, Joe, Petteruti, Philip, Robb, Graeme R, Robers, Matthew B, Saif, Sakina, Stratton, Natalie, Svergun, Dmitri I, Wang, Wenxian, Whittaker, David, Wilson, David M, Yao, Yi
Published in Nature chemical biology (01.12.2016)
Published in Nature chemical biology (01.12.2016)
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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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Pyrimidinone Nicotinamide Mimetics as Selective Tankyrase and Wnt Pathway Inhibitors Suitable for in Vivo Pharmacology
Johannes, Jeffrey W, Almeida, Lynsie, Barlaam, Bernard, Boriack-Sjodin, P. Ann, Casella, Robert, Croft, Rosemary A, Dishington, Allan P, Gingipalli, Lakshmaiah, Gu, Chungang, Hawkins, Janet L, Holmes, Jane L, Howard, Tina, Huang, Jian, Ioannidis, Stephanos, Kazmirski, Steven, Lamb, Michelle L, McGuire, Thomas M, Moore, Jane E, Ogg, Derek, Patel, Anil, Pike, Kurt G, Pontz, Timothy, Robb, Graeme R, Su, Nancy, Wang, Haiyun, Wu, Xiaoyun, Zhang, Hai-Jun, Zhang, Yue, Zheng, Xiaolan, Wang, Tao
Published in ACS medicinal chemistry letters (12.03.2015)
Published in ACS medicinal chemistry letters (12.03.2015)
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The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold
Bonn, Peter, Brink, D. Mikael, Fägerhag, Jonas, Jurva, Ulrik, Robb, Graeme R., Schnecke, Volker, Svensson Henriksson, Anette, Waring, Michael J., Westerlund, Christer
Published in Bioorganic & medicinal chemistry letters (15.12.2012)
Published in Bioorganic & medicinal chemistry letters (15.12.2012)
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Automated Adaptive Absolute Binding Free Energy Calculations
Clark, Finlay, Robb, Graeme R., Cole, Daniel J., Michel, Julien
Published in Journal of chemical theory and computation (10.09.2024)
Published in Journal of chemical theory and computation (10.09.2024)
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Matched molecular pairs as a medicinal chemistry tool
Griffen, Ed, Leach, Andrew G, Robb, Graeme R, Warner, Daniel J
Published in Journal of medicinal chemistry (24.11.2011)
Published in Journal of medicinal chemistry (24.11.2011)
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Development of a Novel B‑Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6
McCoull, William, Cheung, Tony, Anderson, Erica, Barton, Peter, Burgess, Jonathan, Byth, Kate, Cao, Qing, Castaldi, M. Paola, Chen, Huawei, Chiarparin, Elisabetta, Carbajo, Rodrigo J, Code, Erin, Cowan, Suzanna, Davey, Paul R, Ferguson, Andrew D, Fillery, Shaun, Fuller, Nathan O, Gao, Ning, Hargreaves, David, Howard, Martin R, Hu, Jun, Kawatkar, Aarti, Kemmitt, Paul D, Leo, Elisabetta, Molina, Daniel M, O’Connell, Nichole, Petteruti, Philip, Rasmusson, Timothy, Raubo, Piotr, Rawlins, Philip B, Ricchiuto, Piero, Robb, Graeme R, Schenone, Monica, Waring, Michael J, Zinda, Michael, Fawell, Stephen, Wilson, David M
Published in ACS chemical biology (16.11.2018)
Published in ACS chemical biology (16.11.2018)
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Discovery of Pyrazolo[1,5‑a]pyrimidine B‑Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors
McCoull, William, Abrams, Roman D, Anderson, Erica, Blades, Kevin, Barton, Peter, Box, Matthew, Burgess, Jonathan, Byth, Kate, Cao, Qing, Chuaqui, Claudio, Carbajo, Rodrigo J, Cheung, Tony, Code, Erin, Ferguson, Andrew D, Fillery, Shaun, Fuller, Nathan O, Gangl, Eric, Gao, Ning, Grist, Matthew, Hargreaves, David, Howard, Martin R, Hu, Jun, Kemmitt, Paul D, Nelson, Jennifer E, O’Connell, Nichole, Prince, D. Bryan, Raubo, Piotr, Rawlins, Philip B, Robb, Graeme R, Shi, Junjie, Waring, Michael J, Whittaker, David, Wylot, Marta, Zhu, Xiahui
Published in Journal of medicinal chemistry (25.05.2017)
Published in Journal of medicinal chemistry (25.05.2017)
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Development of a Series of Pyrrolopyridone MAT2A Inhibitors
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Published in Journal of medicinal chemistry (28.03.2024)
Published in Journal of medicinal chemistry (28.03.2024)
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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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Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood–Brain Barrier: The Discovery of AZD1390
Pike, Kurt G., Hunt, Thomas A., Barlaam, Bernard, Benstead, David, Cadogan, Elaine, Chen, Kan, Cook, Calum R., Colclough, Nicola, Deng, Chao, Durant, Stephen T., Eatherton, Andrew, Goldberg, Kristin, Johnström, Peter, Liu, Libin, Liu, Zhaoqun, Nissink, J. Willem M., Pang, Chengling, Pass, Martin, Robb, Graeme R., Roberts, Caroline, Schou, Magnus, Steward, Oliver, Sykes, Andy, Yan, Yumei, Zhai, Baochang, Zheng, Li
Published in Journal of medicinal chemistry (22.02.2024)
Published in Journal of medicinal chemistry (22.02.2024)
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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 and In Vivo Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity
Smith, James M., Barlaam, Bernard, Beattie, David, Bradshaw, Lauren, Chan, Ho Man, Chiarparin, Elisabetta, Collingwood, Olga, Cooke, Sophie L., Cronin, Anna, Cumming, Iain, Dean, Emma, Debreczeni, Judit É., del Barco Barrantes, Iván, Diene, Coura, Gianni, Davide, Guerot, Carine, Guo, Xiaoxiao, Guven, Sinem, Hayhow, Thomas G., Hong, Ted, Kemmitt, Paul D., Lamont, Gillian M., Lamont, Scott, Lynch, James T., McWilliams, Lisa, Moore, Shaun, Raubo, Piotr, Robb, Graeme R., Robinson, James, Scott, James S., Srinivasan, Bharath, Steward, Oliver, Stubbs, Christopher J., Syson, Karl, Tan, Lixiang, Turner, Oliver, Underwood, Elizabeth, Urosevic, Jelena, Vazquez-Chantada, Mercedes, Whittaker, Amy L., Wilson, David M., Winter-Holt, Jon J.
Published in Journal of medicinal chemistry (22.08.2024)
Published in Journal of medicinal chemistry (22.08.2024)
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Correction to “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 (11.03.2021)
Published in Journal of medicinal chemistry (11.03.2021)
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Identification and optimisation of a pyrimidopyridone series of IRAK4 inhibitors
Cumming, Iain A., Degorce, Sébastien L., Aagaard, Anna, Braybrooke, Erin L., Davies, Nichola L., Diène, Coura R., Eatherton, Andrew J., Felstead, Hannah R., Groombridge, Sam D., Lenz, Eva M., Li, Yunxia, Nai, Youfeng, Pearson, Stuart, Robb, Graeme R., Scott, James S., Steward, Oliver R., Wu, Chengyan, Xue, Yafeng, Zhang, Lanping, Zhang, Yanxiu
Published in Bioorganic & medicinal chemistry (01.06.2022)
Published in Bioorganic & medicinal chemistry (01.06.2022)
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Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRASG12C with Demonstrable CNS Penetration
Kettle, Jason G., Bagal, Sharan K., Barratt, Derek, Bodnarchuk, Michael S., Boyd, Scott, Braybrooke, Erin, Breed, Jason, Cassar, Doyle J., Cosulich, Sabina, Davies, Michael, Davies, Nichola L., Deng, Chao, Eatherton, Andrew, Evans, Laura, Feron, Lyman J., Fillery, Shaun, Gleave, Emma S., Goldberg, Frederick W., Cortés González, Miguel A., Guerot, Carine, Haider, Afreen, Harlfinger, Stephanie, Howells, Rachel, Jackson, Anne, Johnström, Peter, Kemmitt, Paul D., Koers, Alex, Kondrashov, Mikhail, Lamont, Gillian M., Lamont, Scott, Lewis, Hilary J., Liu, Libin, Mylrea, Megan, Nash, Samuel, Niedbala, Michael J., Peter, Alison, Phillips, Christopher, Pike, Kurt, Raubo, Piotr, Robb, Graeme R., Ross, Sarah, Sanders, Matthew G., Schou, Magnus, Simpson, Iain, Steward, Oliver
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 AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRAS G12C with Demonstrable CNS Penetration
Kettle, Jason G, Bagal, Sharan K, Barratt, Derek, Bodnarchuk, Michael S, Boyd, Scott, Braybrooke, Erin, Breed, Jason, Cassar, Doyle J, Cosulich, Sabina, Davies, Michael, Davies, Nichola L, Deng, Chao, Eatherton, Andrew, Evans, Laura, Feron, Lyman J, Fillery, Shaun, Gleave, Emma S, Goldberg, Frederick W, Cortés González, Miguel A, Guerot, Carine, Haider, Afreen, Harlfinger, Stephanie, Howells, Rachel, Jackson, Anne, Johnström, Peter, Kemmitt, Paul D, Koers, Alex, Kondrashov, Mikhail, Lamont, Gillian M, Lamont, Scott, Lewis, Hilary J, Liu, Libin, Mylrea, Megan, Nash, Samuel, Niedbala, Michael J, Peter, Alison, Phillips, Christopher, Pike, Kurt, Raubo, Piotr, Robb, Graeme R, Ross, Sarah, Sanders, Matthew G, Schou, Magnus, Simpson, Iain, Steward, Oliver
Published in Journal of medicinal chemistry (13.07.2023)
Published in Journal of medicinal chemistry (13.07.2023)
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Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors
Degorce, Sébastien L., Aagaard, Anna, Anjum, Rana, Cumming, Iain A., Diène, Coura R., Fallan, Charlene, Johnson, Tony, Leuchowius, Karl-Johan, Orton, Alexandra L., Pearson, Stuart, Robb, Graeme R., Rosen, Alan, Scarfe, Graeme B., Scott, James S., Smith, James M., Steward, Oliver R., Terstiege, Ina, Tucker, Michael J., Turner, Paul, Wilkinson, Stephen D., Wrigley, Gail L., Xue, Yafeng
Published in Bioorganic & medicinal chemistry (01.12.2020)
Published in Bioorganic & medicinal chemistry (01.12.2020)
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Journal Article
Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4
Degorce, Sébastien L., Anjum, Rana, Dillman, Keith S., Drew, Lisa, Groombridge, Sam D., Halsall, Christopher T., Lenz, Eva M., Lindsay, Nicola A., Mayo, Michele F., Pink, Jennifer H., Robb, Graeme R., Scott, James S., Stokes, Stephen, Xue, Yafeng
Published in Bioorganic & medicinal chemistry (15.02.2018)
Published in Bioorganic & medicinal chemistry (15.02.2018)
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