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
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N‑Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype
Wellaway, Christopher R, Bamborough, Paul, Bernard, Sharon G, Chung, Chun-wa, Craggs, Peter D, Cutler, Leanne, Demont, Emmanuel H, Evans, John P, Gordon, Laurie, Karamshi, Bhumika, Lewis, Antonia J, Lindon, Matthew J, Mitchell, Darren J, Rioja, Inmaculada, Soden, Peter E, Taylor, Simon, Watson, Robert J, Willis, Rob, Woolven, James M, Wyspiańska, Beata S, Kerr, William J, Prinjha, Rab K
Published in Journal of medicinal chemistry (10.09.2020)
Published in Journal of medicinal chemistry (10.09.2020)
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Journal Article
Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins
Preston, Alex, Atkinson, Stephen, Bamborough, Paul, Chung, Chun-wa, Craggs, Peter D, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Jones, Emma J, Lindon, Matthew, Michon, Anne-Marie, Mitchell, Darren J, Prinjha, Rab K, Rianjongdee, Francesco, Rioja, Inmaculada, Seal, Jonathan, Taylor, Simon, Wall, Ian, Watson, Robert J, Woolven, James, Demont, Emmanuel H
Published in Journal of medicinal chemistry (10.09.2020)
Published in Journal of medicinal chemistry (10.09.2020)
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Journal Article
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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Journal Article
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 ed.) (12.09.2016)
Published in Angewandte Chemie (International ed.) (12.09.2016)
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Journal Article
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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Journal Article
Identification of a Series of N‑Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins
Harrison, Lee A, Atkinson, Stephen J, Bassil, Anna, Chung, Chun-wa, Grandi, Paola, Gray, James R. J, Levernier, Etienne, Lewis, Antonia, Lugo, David, Messenger, Cassie, Michon, Anne-Marie, Mitchell, Darren J, Preston, Alex, Prinjha, Rab K, Rioja, Inmaculada, Seal, Jonathan T, Taylor, Simon, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Published in Journal of medicinal chemistry (12.08.2021)
Published in Journal of medicinal chemistry (12.08.2021)
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Journal Article
Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression
Jones, Katherine L., Beaumont, Dominic M., Bernard, Sharon G., Bit, Rino A., Campbell, Simon P., Chung, Chun-wa, Cutler, Leanne, Demont, Emmanuel H., Dennis, Kate, Gordon, Laurie, Gray, James R., Haase, Michael, Lewis, Antonia J., McCleary, Scott, Mitchell, Darren J., Moore, Susanne M., Parr, Nigel, Robb, Olivia J., Smithers, Nicholas, Soden, Peter E., Suckling, Colin J., Taylor, Simon, Walker, Ann L., Watson, Robert J., Prinjha, Rab K.
Published in Journal of medicinal chemistry (26.08.2021)
Published in Journal of medicinal chemistry (26.08.2021)
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Journal Article
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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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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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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Journal Article
Design and Characterization of 1,3-Dihydro‑2H‑benzo[d]azepin-2-ones as Rule-of‑5 Compliant Bivalent BET Inhibitors
Bamborough, Paul, Chung, Chun-wa, Goodwin, Nicole C., Mitchell, Darren J., Neipp, Christopher E., Phillipou, Alex, Preston, Alex, Prinjha, Rab K., Soden, Peter E., Watson, Robert J., Demont, Emmanuel H.
Published in ACS medicinal chemistry letters (14.09.2023)
Published in ACS medicinal chemistry letters (14.09.2023)
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Journal Article
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family
Preston, Alex, Atkinson, Stephen J, Bamborough, Paul, Chung, Chun-wa, Gordon, Laurie J, Grandi, Paola, Gray, James R. J, Harrison, Lee A, Lewis, Antonia J, Lugo, David, Messenger, Cassie, Michon, Anne-Marie, Mitchell, Darren J, Prinjha, Rab K, Rioja, Inmaculada, Seal, Jon, Taylor, Simon, Thesmar, Pierre, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Published in ACS medicinal chemistry letters (13.08.2020)
Published in ACS medicinal chemistry letters (13.08.2020)
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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
Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1
Westaway, Susan M., Thompson, Mervyn, Rami, Harshad K., Stemp, Geoffrey, Trouw, Leontine S., Mitchell, Darren J., Seal, Jon T., Medhurst, Stephen J., Lappin, Sarah C., Biggs, James, Wright, James, Arpino, Sandra, Jerman, Jeffrey C., Cryan, Jennifer E., Holland, Vicky, Winborn, Kim Y., Coleman, Tanya, Stevens, Alexander J., Davis, John B., Gunthorpe, Martin J.
Published in Bioorganic & medicinal chemistry (15.10.2008)
Published in Bioorganic & medicinal chemistry (15.10.2008)
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Journal Article
Discovery of N-(3-Fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the First Small Molecule Motilin Receptor Agonist Clinical Candidate
Westaway, Susan M, Brown, Samantha L, Fell, Stephen C. M, Johnson, Christopher N, MacPherson, David T, Mitchell, Darren J, Myatt, James W, Stanway, Steven J, Seal, Jon T, Stemp, Geoffrey, Thompson, Mervyn, Lawless, Kirk, McKay, Fiona, Muir, Alison I, Barford, Jonathan M, Cluff, Chermaine, Mahmood, Sadhia R, Matthews, Kim L, Mohamed, Shiyam, Smith, Beverley, Stevens, Alexander J, Bolton, Victoria J, Jarvie, Emma M, Sanger, Gareth J
Published in Journal of medicinal chemistry (26.02.2009)
Published in Journal of medicinal chemistry (26.02.2009)
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Journal Article
Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists
AHMED, Mahmood, BRIGGS, Michael A, JOHNSON, Christopher N, MEDHURST, Andrew D, MITCHELL, Darren J, MOSS, Stephen F, POWLES, Jenifer, SEAL, Jon T, STEAN, Tania O, STEMP, Geoffrey, THOMPSON, Mervyn, TRAIL, Brenda, BROMIDGE, Steven M, UPTON, Neil, WINBORN, Kim, WITTY, David R, BUCK, Tania, CAMPBELL, Lorraine, DEEKS, Nigel J, GARNER, Ashley, GORDON, Laurie, HAMPRECHT, Dieter W, HOLLAND, Vicky
Published in Bioorganic & medicinal chemistry letters (01.11.2005)
Published in Bioorganic & medicinal chemistry letters (01.11.2005)
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Journal Article
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 (12.09.2016)
Published in Angewandte Chemie (12.09.2016)
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Journal Article
The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor
Westaway, Susan M., Brown, Samantha L., Conway, Elizabeth, Heightman, Tom D., Johnson, Christopher N., Lapsley, Kate, Macdonald, Gregor J., MacPherson, David T., Mitchell, Darren J., Myatt, James W., Seal, Jon T., Stanway, Steven J., Stemp, Geoffrey, Thompson, Mervyn, Celestini, Paolo, Colombo, Andrea, Consonni, Alessandra, Gagliardi, Stefania, Riccaboni, Mauro, Ronzoni, Silvano, Briggs, Michael A., Matthews, Kim L., Stevens, Alexander J., Bolton, Victoria J., Boyfield, Izzy, Jarvie, Emma M., Stratton, Sharon C., Sanger, Gareth J.
Published in Bioorganic & medicinal chemistry (15.12.2008)
Published in Bioorganic & medicinal chemistry (15.12.2008)
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Journal Article
Definition of the heterocyclic pharmacophore of bacterial methionyl tRNA synthetase inhibitors: potent antibacterially active non-quinolone analogues
Jarvest, Richard L, Armstrong, Sula A, Berge, John M, Brown, Pamela, Elder, John S, Brown, Murray J, Copley, Royston C.B, Forrest, Andrew K, Hamprecht, Dieter W, O'Hanlon, Peter J, Mitchell, Darren J, Rittenhouse, Stephen, Witty, David R
Published in Bioorganic & medicinal chemistry letters (02.08.2004)
Published in Bioorganic & medicinal chemistry letters (02.08.2004)
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