Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders
Bellenie, Benjamin R, Cheung, Kwai-Ming J, Varela, Ana, Pierrat, Olivier A, Collie, Gavin W, Box, Gary M, Bright, Michael D, Gowan, Sharon, Hayes, Angela, Rodrigues, Matthew J, Shetty, Kartika N, Carter, Michael, Davis, Owen A, Henley, Alan T, Innocenti, Paolo, Johnson, Louise D, Liu, Manjuan, de Klerk, Selby, Le Bihan, Yann-Vaï, Lloyd, Matthew G, McAndrew, P. Craig, Shehu, Erald, Talbot, Rachel, Woodward, Hannah L, Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M, Raynaud, Florence I, Rossanese, Olivia W, Hoelder, Swen
Published in Journal of medicinal chemistry (23.04.2020)
Published in Journal of medicinal chemistry (23.04.2020)
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Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors
Davis, Owen A., Cheung, Kwai-Ming J., Brennan, Alfie, Lloyd, Matthew G., Rodrigues, Matthew J., Pierrat, Olivier A., Collie, Gavin W., Le Bihan, Yann-Vaï, Huckvale, Rosemary, Harnden, Alice C., Varela, Ana, Bright, Michael D., Eve, Paul, Hayes, Angela, Henley, Alan T., Carter, Michael D., McAndrew, P. Craig, Talbot, Rachel, Burke, Rosemary, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Meniconi, Mirco, Bellenie, Benjamin R., Hoelder, Swen
Published in Journal of medicinal chemistry (23.06.2022)
Published in Journal of medicinal chemistry (23.06.2022)
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Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket
Lloyd, Matthew G, Huckvale, Rosemary, Cheung, Kwai-Ming J, Rodrigues, Matthew J, Collie, Gavin W, Pierrat, Olivier A, Gatti Iou, Mahad, Carter, Michael, Davis, Owen A, McAndrew, P. Craig, Gunnell, Emma, Le Bihan, Yann-Vaï, Talbot, Rachel, Henley, Alan T, Johnson, Louise D, Hayes, Angela, Bright, Michael D, Raynaud, Florence I, Meniconi, Mirco, Burke, Rosemary, van Montfort, Rob L. M, Rossanese, Olivia W, Bellenie, Benjamin R, Hoelder, Swen
Published in Journal of medicinal chemistry (09.12.2021)
Published in Journal of medicinal chemistry (09.12.2021)
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Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones
Harnden, Alice C., Davis, Owen A., Box, Gary M., Hayes, Angela, Johnson, Louise D., Henley, Alan T., de Haven Brandon, Alexis K., Valenti, Melanie, Cheung, Kwai-Ming J., Brennan, Alfie, Huckvale, Rosemary, Pierrat, Olivier A., Talbot, Rachel, Bright, Michael D., Akpinar, Hafize Aysin, Miller, Daniel S. J., Tarantino, Dalia, Gowan, Sharon, de Klerk, Selby, McAndrew, Peter Craig, Le Bihan, Yann-Vaï, Meniconi, Mirco, Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Bellenie, Benjamin R., Hoelder, Swen
Published in Journal of medicinal chemistry (27.04.2023)
Published in Journal of medicinal chemistry (27.04.2023)
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Journal Article
Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo
Huckvale, Rosemary, Harnden, Alice C., Cheung, Kwai-Ming J., Pierrat, Olivier A., Talbot, Rachel, Box, Gary M., Henley, Alan T., de Haven Brandon, Alexis K., Hallsworth, Albert E., Bright, Michael D., Akpinar, Hafize Aysin, Miller, Daniel S. J., Tarantino, Dalia, Gowan, Sharon, Hayes, Angela, Gunnell, Emma A., Brennan, Alfie, Davis, Owen A., Johnson, Louise D., de Klerk, Selby, McAndrew, Craig, Le Bihan, Yann-Vaï, Meniconi, Mirco, Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Bellenie, Benjamin R., Hoelder, Swen
Published in Journal of medicinal chemistry (23.06.2022)
Published in Journal of medicinal chemistry (23.06.2022)
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Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance
Gurden, Mark D, Westwood, Isaac M, Faisal, Amir, Naud, Sébastien, Cheung, Kwai-Ming J, McAndrew, Craig, Wood, Amy, Schmitt, Jessica, Boxall, Kathy, Mak, Grace, Workman, Paul, Burke, Rosemary, Hoelder, Swen, Blagg, Julian, Van Montfort, Rob L M, Linardopoulos, Spiros
Published in Cancer research (Chicago, Ill.) (15.08.2015)
Published in Cancer research (Chicago, Ill.) (15.08.2015)
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Design of Potent and Selective Hybrid Inhibitors of the Mitotic Kinase Nek2: Structure–Activity Relationship, Structural Biology, and Cellular Activity
Innocenti, Paolo, Cheung, Kwai-Ming J, Solanki, Savade, Mas-Droux, Corine, Rowan, Fiona, Yeoh, Sharon, Boxall, Kathy, Westlake, Maura, Pickard, Lisa, Hardy, Tara, Baxter, Joanne E, Aherne, G. Wynne, Bayliss, Richard, Fry, Andrew M, Hoelder, Swen
Published in Journal of medicinal chemistry (12.04.2012)
Published in Journal of medicinal chemistry (12.04.2012)
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Aminopyrazine Inhibitors Binding to an Unusual Inactive Conformation of the Mitotic Kinase Nek2: SAR and Structural Characterization
Whelligan, Daniel K, Solanki, Savade, Taylor, Dawn, Thomson, Douglas W, Cheung, Kwai-Ming J, Boxall, Kathy, Mas-Droux, Corine, Barillari, Caterina, Burns, Samantha, Grummitt, Charles G, Collins, Ian, van Montfort, Rob L. M, Aherne, G. Wynne, Bayliss, Richard, Hoelder, Swen
Published in Journal of medicinal chemistry (11.11.2010)
Published in Journal of medicinal chemistry (11.11.2010)
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Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues
Sharp, Swee Y, Prodromou, Chrisostomos, Boxall, Kathy, Powers, Marissa V, Holmes, Joanna L, Box, Gary, Matthews, Thomas P, Cheung, Kwai-Ming J, Kalusa, Andrew, James, Karen, Hayes, Angela, Hardcastle, Anthea, Dymock, Brian, Brough, Paul A, Barril, Xavier, Cansfield, Julie E, Wright, Lisa, Surgenor, Allan, Foloppe, Nicolas, Hubbard, Roderick E, Aherne, Wynne, Pearl, Laurence, Jones, Keith, McDonald, Edward, Raynaud, Florence, Eccles, Sue, Drysdale, Martin, Workman, Paul
Published in Molecular cancer therapeutics (01.04.2007)
Published in Molecular cancer therapeutics (01.04.2007)
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Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)‑5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737)
Osborne, James D, Matthews, Thomas P, McHardy, Tatiana, Proisy, Nicolas, Cheung, Kwai-Ming J, Lainchbury, Michael, Brown, Nathan, Walton, Michael I, Eve, Paul D, Boxall, Katherine J, Hayes, Angela, Henley, Alan T, Valenti, Melanie R, De Haven Brandon, Alexis K, Box, Gary, Jamin, Yann, Robinson, Simon P, Westwood, Isaac M, van Montfort, Rob L. M, Leonard, Philip M, Lamers, Marieke B. A. C, Reader, John C, Aherne, G. Wynne, Raynaud, Florence I, Eccles, Suzanne A, Garrett, Michelle D, Collins, Ian
Published in Journal of medicinal chemistry (09.06.2016)
Published in Journal of medicinal chemistry (09.06.2016)
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The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors
Cheung, Kwai-Ming J., Matthews, Thomas P., James, Karen, Rowlands, Martin G., Boxall, Katherine J., Sharp, Swee Y., Maloney, Alison, Roe, S. Mark, Prodromou, Chrisostomos, Pearl, Laurence H., Aherne, G. Wynne, McDonald, Edward, Workman, Paul
Published in Bioorganic & medicinal chemistry letters (15.07.2005)
Published in Bioorganic & medicinal chemistry letters (15.07.2005)
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Structure-Based Design of Orally Bioavailable 1H‑Pyrrolo[3,2‑c]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)
Naud, Sébastien, Westwood, Isaac M, Faisal, Amir, Sheldrake, Peter, Bavetsias, Vassilios, Atrash, Butrus, Cheung, Kwai-Ming J, Liu, Manjuan, Hayes, Angela, Schmitt, Jessica, Wood, Amy, Choi, Vanessa, Boxall, Kathy, Mak, Grace, Gurden, Mark, Valenti, Melanie, de Haven Brandon, Alexis, Henley, Alan, Baker, Ross, McAndrew, Craig, Matijssen, Berry, Burke, Rosemary, Hoelder, Swen, Eccles, Suzanne A, Raynaud, Florence I, Linardopoulos, Spiros, van Montfort, Rob L. M, Blagg, Julian
Published in Journal of medicinal chemistry (27.12.2013)
Published in Journal of medicinal chemistry (27.12.2013)
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In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors
SHARP, Swee Y, BOXALL, Kathy, PATTERSON, Lisa, MATTHEWS, Thomas P, CHEUNG, Kwai-Ming J, BALL, Karen, HAYES, Angela, RAYNAUD, Florence, MARAIS, Richard, PEARL, Laurence, ECCLES, Sue, AHERNE, Wynne, ROWLANDS, Martin, MCDONALD, Edward, WORKMAN, Paul, PRODROMOU, Chrisostomos, ROE, S. Mark, MALONEY, Alison, POWERS, Marissa, CLARKE, Paul A, BOX, Gary, SANDERSON, Sharon
Published in Cancer research (Chicago, Ill.) (01.03.2007)
Published in Cancer research (Chicago, Ill.) (01.03.2007)
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Identification of Inhibitors of Checkpoint Kinase 1 through Template Screening
Matthews, Thomas P, Klair, Suki, Burns, Samantha, Boxall, Kathy, Cherry, Michael, Fisher, Martin, Westwood, Isaac M, Walton, Michael I, McHardy, Tatiana, Cheung, Kwai-Ming J, Van Montfort, Rob, Williams, David, Aherne, G. Wynne, Garrett, Michelle D, Reader, John, Collins, Ian
Published in Journal of medicinal chemistry (13.08.2009)
Published in Journal of medicinal chemistry (13.08.2009)
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Journal Article
Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing
Reader, John C, Matthews, Thomas P, Klair, Suki, Cheung, Kwai-Ming J, Scanlon, Jane, Proisy, Nicolas, Addison, Glynn, Ellard, John, Piton, Nelly, Taylor, Suzanne, Cherry, Michael, Fisher, Martin, Boxall, Kathy, Burns, Samantha, Walton, Michael I, Westwood, Isaac M, Hayes, Angela, Eve, Paul, Valenti, Melanie, de Haven Brandon, Alexis, Box, Gary, van Montfort, Rob L. M, Williams, David H, Aherne, G. Wynne, Raynaud, Florence I, Eccles, Suzanne A, Garrett, Michelle D, Collins, Ian
Published in Journal of medicinal chemistry (22.12.2011)
Published in Journal of medicinal chemistry (22.12.2011)
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A RIPK1-specific PROTAC degrader achieves potent antitumor activity by enhancing immunogenic cell death
Mannion, Jonathan, Gifford, Valentina, Bellenie, Benjamin, Fernando, Winnie, Ramos Garcia, Laura, Wilson, Rebecca, John, Sidonie Wicky, Udainiya, Savita, Patin, Emmanuel C., Tiu, Crescens, Smith, Angel, Goicoechea, Maria, Craxton, Andrew, Moraes de Vasconcelos, Nathalia, Guppy, Naomi, Cheung, Kwai-Ming J., Cundy, Nicholas J., Pierrat, Olivier, Brennan, Alfie, Roumeliotis, Theodoros I., Benstead-Hume, Graeme, Alexander, John, Muirhead, Gareth, Layzell, Scott, Lyu, Wenxin, Roulstone, Victoria, Allen, Mark, Baldock, Holly, Legrand, Arnaud, Gabel, Florian, Serrano-Aparicio, Natalia, Starling, Chris, Guo, Hongyan, Upton, Jason, Gyrd-Hansen, Mads, MacFarlane, Marion, Seddon, Benedict, Raynaud, Florence, Roxanis, Ioannis, Harrington, Kevin, Haider, Syed, Choudhary, Jyoti S., Hoelder, Swen, Tenev, Tencho, Meier, Pascal
Published in Immunity (Cambridge, Mass.) (09.07.2024)
Published in Immunity (Cambridge, Mass.) (09.07.2024)
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NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis
Eccles, Suzanne A, Massey, Andy, Raynaud, Florence I, Sharp, Swee Y, Box, Gary, Valenti, Melanie, Patterson, Lisa, de Haven Brandon, Alexis, Gowan, Sharon, Boxall, Frances, Aherne, Wynne, Rowlands, Martin, Hayes, Angela, Martins, Vanessa, Urban, Frederique, Boxall, Kathy, Prodromou, Chrisostomos, Pearl, Laurence, James, Karen, Matthews, Thomas P, Cheung, Kwai-Ming, Kalusa, Andrew, Jones, Keith, McDonald, Edward, Barril, Xavier, Brough, Paul A, Cansfield, Julie E, Dymock, Brian, Drysdale, Martin J, Finch, Harry, Howes, Rob, Hubbard, Roderick E, Surgenor, Alan, Webb, Paul, Wood, Mike, Wright, Lisa, Workman, Paul
Published in Cancer research (Chicago, Ill.) (15.04.2008)
Published in Cancer research (Chicago, Ill.) (15.04.2008)
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Journal Article
Structure-Based Design of Orally Bioavailable 1 H -Pyrrolo[3,2- c ]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)
Naud, Sébastien, Westwood, Isaac M., Faisal, Amir, Sheldrake, Peter, Bavetsias, Vassilios, Atrash, Butrus, Cheung, Kwai-Ming J., Liu, Manjuan, Hayes, Angela, Schmitt, Jessica, Wood, Amy, Choi, Vanessa, Boxall, Kathy, Mak, Grace, Gurden, Mark, Valenti, Melanie, de Haven Brandon, Alexis, Henley, Alan, Baker, Ross, McAndrew, Craig, Matijssen, Berry, Burke, Rosemary, Hoelder, Swen, Eccles, Suzanne A., Raynaud, Florence I., Linardopoulos, Spiros, van Montfort, Rob L. M., Blagg, Julian
Published in Journal of medicinal chemistry (27.12.2013)
Published in Journal of medicinal chemistry (27.12.2013)
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Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4‑d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N 2‑(2-Ethoxy-4-(4-methyl‑4H‑1,2,4-triazol-3-yl)phenyl)-6-methyl‑N 8‑neopentylpyrido[3,4‑d]pyrimidine-2,8-diamine (BOS172722)
Woodward, Hannah L, Innocenti, Paolo, Cheung, Kwai-Ming J, Hayes, Angela, Roberts, Jennie, Henley, Alan T, Faisal, Amir, Mak, Grace Wing-Yan, Box, Gary, Westwood, Isaac M, Cronin, Nora, Carter, Michael, Valenti, Melanie, De Haven Brandon, Alexis, O’Fee, Lisa, Saville, Harry, Schmitt, Jessica, Burke, Rosemary, Broccatelli, Fabio, van Montfort, Rob L. M, Raynaud, Florence I, Eccles, Suzanne A, Linardopoulos, Spiros, Blagg, Julian, Hoelder, Swen
Published in Journal of medicinal chemistry (27.09.2018)
Published in Journal of medicinal chemistry (27.09.2018)
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