Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation
Lewis, Huw D, Liddle, John, Coote, Jim E, Atkinson, Stephen J, Barker, Michael D, Bax, Benjamin D, Bicker, Kevin L, Bingham, Ryan P, Campbell, Matthew, Chen, Yu Hua, Chung, Chun-wa, Craggs, Peter D, Davis, Rob P, Eberhard, Dirk, Joberty, Gerard, Lind, Kenneth E, Locke, Kelly, Maller, Claire, Martinod, Kimberly, Patten, Chris, Polyakova, Oxana, Rise, Cecil E, Rüdiger, Martin, Sheppard, Robert J, Slade, Daniel J, Thomas, Pamela, Thorpe, Jim, Yao, Gang, Drewes, Gerard, Wagner, Denisa D, Thompson, Paul R, Prinjha, Rab K, Wilson, David M
Published in Nature chemical biology (01.03.2015)
Published in Nature chemical biology (01.03.2015)
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A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response
Kruidenier, Laurens, Chung, Chun-wa, Cheng, Zhongjun, Liddle, John, Che, KaHing, Joberty, Gerard, Bantscheff, Marcus, Bountra, Chas, Bridges, Angela, Diallo, Hawa, Eberhard, Dirk, Hutchinson, Sue, Jones, Emma, Katso, Roy, Leveridge, Melanie, Mander, Palwinder K., Mosley, Julie, Ramirez-Molina, Cesar, Rowland, Paul, Schofield, Christopher J., Sheppard, Robert J., Smith, Julia E., Swales, Catherine, Tanner, Robert, Thomas, Pamela, Tumber, Anthony, Drewes, Gerard, Oppermann, Udo, Patel, Dinshaw J., Lee, Kevin, Wilson, David M.
Published in Nature (London) (16.08.2012)
Published in Nature (London) (16.08.2012)
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Biocatalysis in Drug Design: Engineered Reductive Aminases (RedAms) Are Used to Access Chiral Building Blocks with Multiple Stereocenters
Casamajo, Arnau Rué, Yu, Yuqi, Schnepel, Christian, Morrill, Charlotte, Barker, Rhys, Levy, Colin W., Finnigan, James, Spelling, Victor, Westerlund, Kristina, Petchey, Mark, Sheppard, Robert J., Lewis, Richard J., Falcioni, Francesco, Hayes, Martin A., Turner, Nicholas J.
Published in Journal of the American Chemical Society (11.10.2023)
Published in Journal of the American Chemical Society (11.10.2023)
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A Chemical Probe for the ATAD2 Bromodomain
Bamborough, Paul, Chung, Chun-wa, Demont, Emmanuel H., Furze, Rebecca C., Bannister, Andrew J., Che, Ka Hing, Diallo, Hawa, Douault, Clement, Grandi, Paola, Kouzarides, Tony, Michon, Anne-Marie, Mitchell, Darren J., Prinjha, Rab K., Rau, Christina, Robson, Samuel, Sheppard, Robert J., Upton, Richard, Watson, Robert J.
Published in Angewandte Chemie International Edition (12.09.2016)
Published in Angewandte Chemie International Edition (12.09.2016)
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Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors
Bamborough, Paul, Chung, Chun-wa, Furze, Rebecca C, Grandi, Paola, Michon, Anne-Marie, Sheppard, Robert J, Barnett, Heather, Diallo, Hawa, Dixon, David P, Douault, Clement, Jones, Emma J, Karamshi, Bhumika, Mitchell, Darren J, Prinjha, Rab K, Rau, Christina, Watson, Robert J, Werner, Thilo, Demont, Emmanuel H
Published in Journal of medicinal chemistry (13.08.2015)
Published in Journal of medicinal chemistry (13.08.2015)
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Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode
Lucas, Simon C. C, Atkinson, Stephen J, Bamborough, Paul, Barnett, Heather, Chung, Chun-wa, Gordon, Laurie, Mitchell, Darren J, Phillipou, Alexander, Prinjha, Rab K, Sheppard, Robert J, Tomkinson, Nicholas C. O, Watson, Robert J, Demont, Emmanuel H
Published in Journal of medicinal chemistry (28.05.2020)
Published in Journal of medicinal chemistry (28.05.2020)
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Route to Prolonged Residence Time at the Histamine H1 Receptor: Growing from Desloratadine to Rupatadine
Bosma, Reggie, Wang, Zhiyong, Kooistra, Albert J, Bushby, Nick, Kuhne, Sebastiaan, van den Bor, Jelle, Waring, Michael J, de Graaf, Chris, de Esch, Iwan J, Vischer, Henry F, Sheppard, Robert J, Wijtmans, Maikel, Leurs, Rob
Published in Journal of medicinal chemistry (25.07.2019)
Published in Journal of medicinal chemistry (25.07.2019)
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Journal Article
Route to Prolonged Residence Time at the Histamine H-1 Receptor: Growing from Desloratadine to Rupatadine
Bosma, Reggie, Wang, Zhiyong, Kooistra, Albert J., Bushby, Nick, Kuhne, Sebastiaan, van den Bor, Jelle, Waring, Michael J., de Graaf, Chris, de Esch, Iwan J., Vischer, Henry F., Sheppard, Robert J., Wijtmans, Maikel, Leurs, Rob
Published in Journal of medicinal chemistry (25.07.2019)
Published in Journal of medicinal chemistry (25.07.2019)
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Journal Article
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors
Demont, Emmanuel H., Chung, Chun-wa, Furze, Rebecca C., Grandi, Paola, Michon, Anne-Marie, Wellaway, Chris, Barrett, Nathalie, Bridges, Angela M., Craggs, Peter D., Diallo, Hawa, Dixon, David P., Douault, Clement, Emmons, Amanda J., Jones, Emma J., Karamshi, Bhumika V., Locke, Kelly, Mitchell, Darren J., Mouzon, Bernadette H., Prinjha, Rab K., Roberts, Andy D., Sheppard, Robert J., Watson, Robert J., Bamborough, Paul
Published in Journal of medicinal chemistry (23.07.2015)
Published in Journal of medicinal chemistry (23.07.2015)
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Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors
Bamborough, Paul, Chung, Chun-wa, Furze, Rebecca C, Grandi, Paola, Michon, Anne-Marie, Watson, Robert J, Mitchell, Darren J, Barnett, Heather, Prinjha, Rab K, Rau, Christina, Sheppard, Robert J, Werner, Thilo, Demont, Emmanuel H
Published in Journal of medicinal chemistry (27.09.2018)
Published in Journal of medicinal chemistry (27.09.2018)
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Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor
Bosma, Reggie, Stoddart, Leigh A., Georgi, Victoria, Bouzo-Lorenzo, Monica, Bushby, Nick, Inkoom, Loretta, Waring, Michael J., Briddon, Stephen J., Vischer, Henry F., Sheppard, Robert J., Fernández-Montalván, Amaury, Hill, Stephen J., Leurs, Rob
Published in Scientific reports (27.05.2019)
Published in Scientific reports (27.05.2019)
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Journal Article
A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification
Bamborough, Paul, Chung, Chun-wa, Demont, Emmanuel H, Bridges, Angela M, Craggs, Peter D, Dixon, David P, Francis, Peter, Furze, Rebecca C, Grandi, Paola, Jones, Emma J, Karamshi, Bhumika, Locke, Kelly, Lucas, Simon C. C, Michon, Anne-Marie, Mitchell, Darren J, Pogány, Peter, Prinjha, Rab K, Rau, Christina, Roa, Ana Maria, Roberts, Andrew D, Sheppard, Robert J, Watson, Robert J
Published in Journal of medicinal chemistry (22.08.2019)
Published in Journal of medicinal chemistry (22.08.2019)
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Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3‑Amino-4-pyridine Carboxylate Derivatives
Westaway, Susan M, Preston, Alex G. S, Barker, Michael D, Brown, Fiona, Brown, Jack A, Campbell, Matthew, Chung, Chun-wa, Diallo, Hawa, Douault, Clement, Drewes, Gerard, Eagle, Robert, Gordon, Laurie, Haslam, Carl, Hayhow, Thomas G, Humphreys, Philip G, Joberty, Gerard, Katso, Roy, Kruidenier, Laurens, Leveridge, Melanie, Liddle, John, Mosley, Julie, Muelbaier, Marcel, Randle, Rebecca, Rioja, Inma, Rueger, Anne, Seal, Gail A, Sheppard, Robert J, Singh, Onkar, Taylor, Joanna, Thomas, Pamela, Thomson, Douglas, Wilson, David M, Lee, Kevin, Prinjha, Rab K
Published in Journal of medicinal chemistry (25.02.2016)
Published in Journal of medicinal chemistry (25.02.2016)
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Journal Article
Structure-Activity Relationships of the Sustained Effects of Adenosine A2A Receptor Agonists Driven by Slow Dissociation Kinetics
Hothersall, J Daniel, Guo, Dong, Sarda, Sunil, Sheppard, Robert J, Chen, Hongming, Keur, Wesley, Waring, Michael J, IJzerman, Adriaan P, Hill, Stephen J, Dale, Ian L, Rawlins, Philip B
Published in Molecular pharmacology (01.01.2017)
Published in Molecular pharmacology (01.01.2017)
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Journal Article
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain
Demont, Emmanuel H, Bamborough, Paul, Chung, Chun-wa, Craggs, Peter D, Fallon, David, Gordon, Laurie J, Grandi, Paola, Hobbs, Clare I, Hussain, Jameed, Jones, Emma J, Le Gall, Armelle, Michon, Anne-Marie, Mitchell, Darren J, Prinjha, Rab K, Roberts, Andy D, Sheppard, Robert J, Watson, Robert J
Published in ACS medicinal chemistry letters (13.11.2014)
Published in ACS medicinal chemistry letters (13.11.2014)
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Journal Article
Structure–Affinity Relationships and Structure–Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists
Xia, Lizi, de Vries, Henk, Lenselink, Eelke B., Louvel, Julien, Waring, Michael J., Cheng, Leifeng, Pahlén, Sara, Petersson, Maria J., Schell, Peter, Olsson, Roine I., Heitman, Laura H., Sheppard, Robert J., IJzerman, Adriaan P.
Published in Journal of medicinal chemistry (14.12.2017)
Published in Journal of medicinal chemistry (14.12.2017)
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Journal Article
Interrogating the Druggability of the 2‑Oxoglutarate-Dependent Dioxygenase Target Class by Chemical Proteomics
Joberty, Gérard, Boesche, Markus, Brown, Jack A, Eberhard, Dirk, Garton, Neil S, Humphreys, Philip G, Mathieson, Toby, Muelbaier, Marcel, Ramsden, Nigel G, Reader, Valérie, Rueger, Anne, Sheppard, Robert J, Westaway, Susan M, Bantscheff, Marcus, Lee, Kevin, Wilson, David M, Prinjha, Rab K, Drewes, Gerard
Published in ACS chemical biology (15.07.2016)
Published in ACS chemical biology (15.07.2016)
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Journal Article
GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain
Bamborough, Paul, Barnett, Heather A, Becher, Isabelle, Bird, Mark J, Chung, Chun-wa, Craggs, Peter D, Demont, Emmanuel H, Diallo, Hawa, Fallon, David J, Gordon, Laurie J, Grandi, Paola, Hobbs, Clare I, Hooper-Greenhill, Edward, Jones, Emma J, Law, Robert P, Le Gall, Armelle, Lugo, David, Michon, Anne-Marie, Mitchell, Darren J, Prinjha, Rab K, Sheppard, Robert J, Watson, Allan J. B, Watson, Robert J
Published in ACS medicinal chemistry letters (09.06.2016)
Published in ACS medicinal chemistry letters (09.06.2016)
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Journal Article
Kruidenier et al. reply
Kruidenier, Laurens, Chung, Chun-wa, Cheng, Zhongjun, Liddle, John, Che, KaHing, Joberty, Gerard, Bantscheff, Marcus, Bountra, Chas, Bridges, Angela, Diallo, Hawa, Eberhard, Dirk, Hutchinson, Sue, Jones, Emma, Katso, Roy, Leveridge, Melanie, Mander, Palwinder K., Mosley, Julie, Ramirez-Molina, Cesar, Rowland, Paul, Schofield, Christopher J., Sheppard, Robert J., Smith, Julia E., Swales, Catherine, Tanner, Robert, Thomas, Pamela, Tumber, Anthony, Drewes, Gerard, Oppermann, Udo, Patel, Dinshaw J., Lee, Kevin, Wilson, David M.
Published in Nature (London) (02.10.2014)
Published in Nature (London) (02.10.2014)
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