Discovery of I‑BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition
Theodoulou, Natalie H, Bamborough, Paul, Bannister, Andrew J, Becher, Isabelle, Bit, Rino A, Che, Ka Hing, Chung, Chun-wa, Dittmann, Antje, Drewes, Gerard, Drewry, David H, Gordon, Laurie, Grandi, Paola, Leveridge, Melanie, Lindon, Matthew, Michon, Anne-Marie, Molnar, Judit, Robson, Samuel C, Tomkinson, Nicholas C. O, Kouzarides, Tony, Prinjha, Rab K, Humphreys, Philip G
Published in Journal of medicinal chemistry (25.02.2016)
Published in Journal of medicinal chemistry (25.02.2016)
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BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability
Jennings, Laura E., Schiedel, Matthias, Hewings, David S., Picaud, Sarah, Laurin, Corentine M.C., Bruno, Paul A., Bluck, Joseph P., Scorah, Amy R., See, Larissa, Reynolds, Jessica K., Moroglu, Mustafa, Mistry, Ishna N., Hicks, Amy, Guzanov, Pavel, Clayton, James, Evans, Charles N.G., Stazi, Giulia, Biggin, Philip C., Mapp, Anna K., Hammond, Ester M., Humphreys, Philip G., Filippakopoulos, Panagis, Conway, Stuart J.
Published in Bioorganic & medicinal chemistry (15.07.2018)
Published in Bioorganic & medicinal chemistry (15.07.2018)
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Lithiation-Induced Migrations from Nitrogen to Carbon in Terminal Aziridines
Hodgson, David M., Humphreys, Philip G., Xu, Zhaoqing, Ward, John G.
Published in Angewandte Chemie (International ed.) (01.01.2007)
Published in Angewandte Chemie (International ed.) (01.01.2007)
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Widening the usefulness of epoxides and aziridines in synthesis
Hodgson, David M., Humphreys, Philip G., Hughes, Steven P.
Published in Pure and applied chemistry (01.02.2007)
Published in Pure and applied chemistry (01.02.2007)
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Clinical progress and pharmacology of small molecule bromodomain inhibitors
Theodoulou, Natalie H, Tomkinson, Nicholas CO, Prinjha, Rab K, Humphreys, Philip G
Published in Current opinion in chemical biology (01.08.2016)
Published in Current opinion in chemical biology (01.08.2016)
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Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach
Bassi, Zuni I, Fillmore, Martin C, Miah, Afjal H, Chapman, Trevor D, Maller, Claire, Roberts, Emma J, Davis, Lauren C, Lewis, Darcy E, Galwey, Nicholas W, Waddington, Kirsty E, Parravicini, Valentino, Macmillan-Jones, Abigail L, Gongora, Celine, Humphreys, Philip G, Churcher, Ian, Prinjha, Rab K, Tough, David F
Published in ACS chemical biology (19.10.2018)
Published in ACS chemical biology (19.10.2018)
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Advancements in the Development of non‐BET Bromodomain Chemical Probes
Clegg, Michael A., Tomkinson, Nicholas C. O., Prinjha, Rab K., Humphreys, Philip G.
Published in ChemMedChem (19.02.2019)
Published in ChemMedChem (19.02.2019)
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Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe
Humphreys, Philip G, Bamborough, Paul, Chung, Chun-wa, Craggs, Peter D, Gordon, Laurie, Grandi, Paola, Hayhow, Thomas G, Hussain, Jameed, Jones, Katherine L, Lindon, Matthew, Michon, Anne-Marie, Renaux, Jessica F, Suckling, Colin J, Tough, David F, Prinjha, Rab K
Published in Journal of medicinal chemistry (26.01.2017)
Published in Journal of medicinal chemistry (26.01.2017)
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Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains
Clegg, Michael A., Bamborough, Paul, Chung, Chun-wa, Craggs, Peter D., Gordon, Laurie, Grandi, Paola, Leveridge, Melanie, Lindon, Matthew, Liwicki, Gemma M., Michon, Anne-Marie, Molnar, Judit, Rioja, Inmaculada, Soden, Peter E., Theodoulou, Natalie H., Werner, Thilo, Tomkinson, Nicholas C. O., Prinjha, Rab K., Humphreys, Philip G.
Published in Journal of medicinal chemistry (11.06.2020)
Published in Journal of medicinal chemistry (11.06.2020)
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Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N‑Terminal Bromodomain Chemical Probe
Bradley, Erin, Fusani, Lucia, Chung, Chun-wa, Craggs, Peter D., Demont, Emmanuel H., Humphreys, Philip G., Mitchell, Darren J., Phillipou, Alex, Rioja, Inmaculada, Shah, Rishi R., Wellaway, Christopher R., Prinjha, Rab K., Palmer, David S., Kerr, William J., Reid, Marc, Wall, Ian D., Cookson, Rosa
Published in Journal of medicinal chemistry (14.12.2023)
Published in Journal of medicinal chemistry (14.12.2023)
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Alkene Syn- and Anti-Oxyamination with Malonoyl Peroxides
Curle, Jonathan M, Perieteanu, Marina C, Humphreys, Philip G, Kennedy, Alan R, Tomkinson, Nicholas C. O
Published in Organic letters (21.02.2020)
Published in Organic letters (21.02.2020)
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Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening
Wellaway, Christopher R, Amans, Dominique, Bamborough, Paul, Barnett, Heather, Bit, Rino A, Brown, Jack A, Carlson, Neil R, Chung, Chun-wa, Cooper, Anthony W. J, Craggs, Peter D, Davis, Robert P, Dean, Tony W, Evans, John P, Gordon, Laurie, Harada, Isobel L, Hirst, David J, Humphreys, Philip G, Jones, Katherine L, Lewis, Antonia J, Lindon, Matthew J, Lugo, Dave, Mahmood, Mahnoor, McCleary, Scott, Medeiros, Patricia, Mitchell, Darren J, O’Sullivan, Michael, Le Gall, Armelle, Patel, Vipulkumar K, Patten, Chris, Poole, Darren L, Shah, Rishi R, Smith, Jane E, Stafford, Kayleigh A. J, Thomas, Pamela J, Vimal, Mythily, Wall, Ian D, Watson, Robert J, Wellaway, Natalie, Yao, Gang, Prinjha, Rab K
Published in Journal of medicinal chemistry (23.01.2020)
Published in Journal of medicinal chemistry (23.01.2020)
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Design, Synthesis, and Characterization of I‑BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate
Humphreys, Philip G, Atkinson, Stephen J, Bamborough, Paul, Bit, Rino A, Chung, Chun-wa, Craggs, Peter D, Cutler, Leanne, Davis, Rob, Ferrie, Alan, Gong, GangLi, Gordon, Laurie J, Gray, Matthew, Harrison, Lee A, Hayhow, Thomas G, Haynes, Andrea, Henley, Nick, Hirst, David J, Holyer, Ian D, Lindon, Matthew J, Lovatt, Cerys, Lugo, David, McCleary, Scott, Molnar, Judit, Osmani, Qendresa, Patten, Chris, Preston, Alex, Rioja, Inmaculada, Seal, Jonathan T, Smithers, Nicholas, Sun, Fenglai, Tang, Dalin, Taylor, Simon, Theodoulou, Natalie H, Thomas, Clare, Watson, Robert J, Wellaway, Christopher R, Zhu, Linrong, Tomkinson, Nicholas C. O, Prinjha, Rab K
Published in Journal of medicinal chemistry (10.02.2022)
Published in Journal of medicinal chemistry (10.02.2022)
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Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4‑d]pyrimidin-4(3H)‑one Derivatives
Westaway, Susan M, Preston, Alex G. S, Barker, Michael D, Brown, Fiona, Brown, Jack A, Campbell, Matthew, Chung, Chun-wa, Drewes, Gerard, Eagle, Robert, Garton, Neil, Gordon, Laurie, Haslam, Carl, Hayhow, Thomas G, Humphreys, Philip G, Joberty, Gerard, Katso, Roy, Kruidenier, Laurens, Leveridge, Melanie, Pemberton, Michelle, Rioja, Inma, Seal, Gail A, Shipley, Tracy, Singh, Onkar, Suckling, Colin J, Taylor, Joanna, Thomas, Pamela, 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
Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I‑BET432
Humphreys, Philip G., Anderson, Niall A., Bamborough, Paul, Baxter, Andrew, Chung, Chun-wa, Cookson, Rosa, Craggs, Peter D., Dalton, Toryn, Fournier, Julie C. L., Gordon, Laurie J., Gray, Heather F., Gray, Matthew W., Gregory, Richard, Hirst, David J., Jamieson, Craig, Jones, Katherine L., Kessedjian, Hripsimee, Lugo, David, McGonagle, Grant, Patel, Vipulkumar K., Patten, Christopher, Poole, Darren L., Prinjha, Rab K., Ramirez-Molina, Cesar, Rioja, Inmaculada, Seal, Gail, Stafford, Kayleigh A. J., Shah, Rishi R., Tape, Daniel, Theodoulou, Natalie H., Tomlinson, Laura, Ukuser, Sabri, Wall, Ian D., Wellaway, Natalie, White, Gemma
Published in Journal of medicinal chemistry (24.11.2022)
Published in Journal of medicinal chemistry (24.11.2022)
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Journal Article
Structure- and Property-Based Optimization of Efficient Pan-Bromodomain and Extra Terminal Inhibitors to Identify Oral and Intravenous Candidate I‑BET787
Hirst, David J., Bamborough, Paul, Al-Mahdi, Niam, Angell, Davina C., Barnett, Heather A., Baxter, Andrew, Bit, Rino A., Brown, Jack A., Chung, Chun-wa, Craggs, Peter D., Davis, Robert P., Demont, Emmanuel H., Ferrie, Alan, Gordon, Laurie J., Harada, Isobel, Ho, Tim C. T., Holyer, Ian D., Hooper-Greenhill, Edward, Jones, Katherine L., Lindon, Matthew J., Lovatt, Cerys, Lugo, David, Maller, Claire, McGonagle, Grant, Messenger, Cassie, Mitchell, Darren J., Pascoe, David D., Patel, Vipulkumar K., Patten, Christopher, Poole, Darren L., Shah, Rishi R., Rioja, Inmaculada, Stafford, Kayleigh A. J., Tape, Daniel, Taylor, Simon, Theodoulou, Natalie H., Tomlinson, Laura, Wall, Ian D., Wellaway, Christopher R., White, Gemma, Prinjha, Rab K., Humphreys, Philip G.
Published in Journal of medicinal chemistry (27.06.2024)
Published in Journal of medicinal chemistry (27.06.2024)
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Progress in the Development of non-BET Bromodomain Chemical Probes
Theodoulou, Natalie H., Tomkinson, Nicholas C. O., Prinjha, Rab K., Humphreys, Philip G.
Published in ChemMedChem (04.03.2016)
Published in ChemMedChem (04.03.2016)
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