Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor
Perera, Timothy P S, Jovcheva, Eleonora, Mevellec, Laurence, Vialard, Jorge, De Lange, Desiree, Verhulst, Tinne, Paulussen, Caroline, Van De Ven, Kelly, King, Peter, Freyne, Eddy, Rees, David C, Squires, Matthew, Saxty, Gordon, Page, Martin, Murray, Christopher W, Gilissen, Ron, Ward, George, Thompson, Neil T, Newell, David R, Cheng, Na, Xie, Liang, Yang, Jennifer, Platero, Suso J, Karkera, Jayaprakash D, Moy, Christopher, Angibaud, Patrick, Laquerre, Sylvie, Lorenzi, Matthew V
Published in Molecular cancer therapeutics (01.06.2017)
Published in Molecular cancer therapeutics (01.06.2017)
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Identification of N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design
Wyatt, Paul G, Woodhead, Andrew J, Berdini, Valerio, Boulstridge, John A, Carr, Maria G, Cross, David M, Davis, Deborah J, Devine, Lindsay A, Early, Theresa R, Feltell, Ruth E, Lewis, E. Jonathan, McMenamin, Rachel L, Navarro, Eva F, O’Brien, Michael A, O’Reilly, Marc, Reule, Matthias, Saxty, Gordon, Seavers, Lisa C. A, Smith, Donna-Michelle, Squires, Matt S, Trewartha, Gary, Walker, Margaret T, Woolford, Alison J.-A
Published in Journal of medicinal chemistry (28.08.2008)
Published in Journal of medicinal chemistry (28.08.2008)
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Identification of Inhibitors of Protein Kinase B Using Fragment-Based Lead Discovery
Saxty, Gordon, Woodhead, Steven J, Berdini, Valerio, Davies, Thomas G, Verdonk, Marcel L, Wyatt, Paul G, Boyle, Robert G, Barford, David, Downham, Robert, Garrett, Michelle D, Carr, Robin A
Published in Journal of medicinal chemistry (17.05.2007)
Published in Journal of medicinal chemistry (17.05.2007)
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Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2‑Related Factor 2 (KEAP1:NRF2) Protein–Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery
Davies, Thomas G, Wixted, William E, Coyle, Joseph E, Griffiths-Jones, Charlotte, Hearn, Keisha, McMenamin, Rachel, Norton, David, Rich, Sharna J, Richardson, Caroline, Saxty, Gordon, Willems, Henriëtte M. G, Woolford, Alison J.-A, Cottom, Joshua E, Kou, Jen-Pyng, Yonchuk, John G, Feldser, Heidi G, Sanchez, Yolanda, Foley, Joseph P, Bolognese, Brian J, Logan, Gregory, Podolin, Patricia L, Yan, Hongxing, Callahan, James F, Heightman, Tom D, Kerns, Jeffrey K
Published in Journal of medicinal chemistry (28.04.2016)
Published in Journal of medicinal chemistry (28.04.2016)
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Structure–Activity and Structure–Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2‑Related Factor 2 (KEAP1/NRF2) Protein–Protein Interaction
Heightman, Tom D, Callahan, James F, Chiarparin, Elisabetta, Coyle, Joseph E, Griffiths-Jones, Charlotte, Lakdawala, Ami S, McMenamin, Rachel, Mortenson, Paul N, Norton, David, Peakman, Torren M, Rich, Sharna J, Richardson, Caroline, Rumsey, William L, Sanchez, Yolanda, Saxty, Gordon, Willems, Henriëtte M. G, Wolfe, Lawrence, Woolford, Alison J.-A, Wu, Zining, Yan, Hongxing, Kerns, Jeffrey K, Davies, Thomas G
Published in Journal of medicinal chemistry (09.05.2019)
Published in Journal of medicinal chemistry (09.05.2019)
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A Fragment-Derived Clinical Candidate for Antagonism of X‑Linked and Cellular Inhibitor of Apoptosis Proteins: 1‑(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl‑1H,2H,3H‑pyrrolo[3,2‑b]pyridin-1-yl)-2-[(2R,5R)‑5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660)
Johnson, Christopher N., Ahn, Jong Sook, Buck, Ildiko M., Chiarparin, Elisabetta, Day, James E. H., Hopkins, Anna, Howard, Steven, Lewis, Edward J., Martins, Vanessa, Millemaggi, Alessia, Munck, Joanne M., Page, Lee W., Peakman, Torren, Reader, Michael, Rich, Sharna J., Saxty, Gordon, Smyth, Tomoko, Thompson, Neil T., Ward, George A., Williams, Pamela A., Wilsher, Nicola E., Chessari, Gianni
Published in Journal of medicinal chemistry (23.08.2018)
Published in Journal of medicinal chemistry (23.08.2018)
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Journal Article
A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660)
Johnson, Christopher N, Ahn, Jong Sook, Buck, Ildiko M, Chiarparin, Elisabetta, Day, James E H, Hopkins, Anna, Howard, Steven, Lewis, Edward J, Martins, Vanessa, Millemaggi, Alessia, Munck, Joanne M, Page, Lee W, Peakman, Torren, Reader, Michael, Rich, Sharna J, Saxty, Gordon, Smyth, Tomoko, Thompson, Neil T, Ward, George A, Williams, Pamela A, Wilsher, Nicola E, Chessari, Gianni
Published in Journal of medicinal chemistry (23.08.2018)
Published in Journal of medicinal chemistry (23.08.2018)
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A knowledge-based, structural-aided discovery of a novel class of 2-phe-nylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors
Schulte, Christie A., Deaton, David N., Diaz, Elsie, Do, Young, Gampe, Robert T., Guss, Jeffrey H., Hancock, Ashley P., Hobbs, Heather, Hodgson, Simon T., Holt, Jason, Jeune, Michael R., Kahler, Kirsten M., Kramer, H. Fritz, Le, Joelle, Mortenson, Paul N., Musetti, Caterina, Nolte, Robert T., Orband-Miller, Lisa A., Peckham, Gregory E., Petrov, Kim G., Pietrak, Beth L., Poole, Chuck, Price, Daniel J., Saxty, Gordon, Shillings, Anthony, Smalley, Terrence L., Somers, Don O., Stewart, Eugene L., Stuart, J. Darren, Thomson, Stephen A.
Published in Bioorganic & medicinal chemistry letters (01.09.2021)
Published in Bioorganic & medicinal chemistry letters (01.09.2021)
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Macrolide Inspired Macrocycles as Modulators of the IL-17A/IL-17RA Interaction
Koštrun, Sanja, Fajdetić, Andrea, Pešić, Dijana, Brajša, Karmen, Bencetić Mihaljević, Vlatka, Jelić, Dubravko, Petrinić Grba, Adriana, Elenkov, Ivaylo, Rupčić, Renata, Kapić, Samra, Ozimec Landek, Ivana, Butković, Kristina, Grgičević, Ana, Žiher, Dinko, Čikoš, Ana, Padovan, Jasna, Saxty, Gordon, Dack, Kevin, Bladh, Haakan, Skak-Nielsen, Tine, Feldbaek Nielsen, Simon, Lambert, Maja, Stahlhut, Martin
Published in Journal of medicinal chemistry (24.06.2021)
Published in Journal of medicinal chemistry (24.06.2021)
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Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode
Southall, Stacey M., Banerjee, Joydeep, Brown, Jason, Butkovic, Kristina, Cansfield, Andrew D., Cansfield, Julie E., Congreve, Miles S., Cseke, Gabriella, Deflorian, Francesca, Hunjadi, Martina Petrovic, Hutinec, Antun, Inturi, Trinadh Kumar, Rupcic, Renata, Saxty, Gordon, Watson, Stephen P.
Published in ACS medicinal chemistry letters (10.11.2022)
Published in ACS medicinal chemistry letters (10.11.2022)
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Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein–Ligand Complexes
Cansfield, Andrew D, Ator, Mark A, Banerjee, Joydeep, Bestwick, Michael, Bortolato, Andrea, Brown, Giles A, Brown, Jason, Butkovic, Kristina, Cansfield, Julie E, Christopher, John A, Congreve, Miles, Cseke, Gabriella, Deflorian, Francesca, Dugan, Benjamin, Hunjadi, Martina Petrovic, Hutinec, Antun, Inturi, Trinadh Kumar, Landek, Goran, Mason, Jonathan, O’Brien, Alistair, Ott, Gregory R, Rupcic, Renata, Saxty, Gordon, Southall, Stacey M, Zadravec, Rahela, Watson, Stephen P
Published in ACS chemical neuroscience (16.03.2022)
Published in ACS chemical neuroscience (16.03.2022)
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A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors
Schulte, Christie A., Deaton, David N., Diaz, Elsie, Do, Young, Gampe, Robert T., Guss, Jeffrey H., Hancock, Ashley P., Hobbs, Heather, Hodgson, Simon T., Holt, Jason, Jeune, Michael R., Kahler, Kirsten M., Kramer, H. Fritz, Le, Joelle, Mortenson, Paul N., Musetti, Caterina, Nolte, Robert T., Orband-Miller, Lisa A., Peckham, Gregory E., Petrov, Kim G., Pietrak, Beth L., Poole, Chuck, Price, Daniel J., Saxty, Gordon, Shillings, Anthony, Smalley, Terrence L., Somers, Don O., Stewart, Eugene L., Stuart, J. Darren, Thomson, Stephen A.
Published in Bioorganic & medicinal chemistry letters (01.09.2021)
Published in Bioorganic & medicinal chemistry letters (01.09.2021)
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The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors
Deaton, David N., Do, Young, Holt, Jason, Jeune, Michael R., Kramer, H. Fritz, Larkin, Andrew L., Orband-Miller, Lisa A., Peckham, Gregory E., Poole, Chuck, Price, Daniel J., Schaller, Lee T., Shen, Ying, Shewchuk, Lisa M., Stewart, Eugene L., Stuart, J. Darren, Thomson, Stephen A., Ward, Paris, Wilson, Joseph W., Xu, Tianshun, Guss, Jeffrey H., Musetti, Caterina, Rendina, Alan R., Affleck, Karen, Anders, David, Hancock, Ashley P., Hobbs, Heather, Hodgson, Simon T., Hutchinson, Jonathan, Leveridge, Melanie V., Nicholls, Harry, Smith, Ian E.D., Somers, Don O., Sneddon, Helen F., Uddin, Sorif, Cleasby, Anne, Mortenson, Paul N., Richardson, Caroline, Saxty, Gordon
Published in Bioorganic & medicinal chemistry (15.04.2019)
Published in Bioorganic & medicinal chemistry (15.04.2019)
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Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors
Murray, Christopher W, Berdini, Valerio, Buck, Ildiko M, Carr, Maria E, Cleasby, Anne, Coyle, Joseph E, Curry, Jayne E, Day, James E. H, Day, Phillip J, Hearn, Keisha, Iqbal, Aman, Lee, Lydia Y. W, Martins, Vanessa, Mortenson, Paul N, Munck, Joanne M, Page, Lee W, Patel, Sahil, Roomans, Susan, Smith, Kirsten, Tamanini, Emiliano, Saxty, Gordon
Published in ACS medicinal chemistry letters (09.07.2015)
Published in ACS medicinal chemistry letters (09.07.2015)
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Abstract 3640: Discovery of quinazolinones as fibroblast growth factor receptor (FGFR1-4) kinase inhibitors
Querolle, Olivier, Angibaud, Patrick, Colombel, Hélène, Caron, Virginie, Pilatte, Isabelle, Poncelet, Virginie, Esser, Norbert, Gilissen, Ron, King, Peter, Meerpoel, Lieven, Verhulst, Tinne, Wroblowski, Berthold, Vialard, Jorge, Murray, Chris W., Rees, David C., Reningovolo, Anita, Saxty, Gordon
Published in Cancer research (Chicago, Ill.) (01.08.2015)
Published in Cancer research (Chicago, Ill.) (01.08.2015)
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Abstract 3641: Identification of naphthyridines as potent inhibitors of fibroblast growth factor receptor kinase family
Angibaud, Patrick R., Obringer, Michel, Marin, Julien, Jeanty, Matthieu, Esser, Norbert, Gilissen, Ron, King, Peter, Meerpoel, Lieven, Querolle, Olivier, Rees, David C., Roux, Bruno, Saxty, Gordon, Verhulst, Tinne, Wroblowski, Berthold, Murray, Christopher C., Vialard, Jorge
Published in Cancer research (Chicago, Ill.) (01.08.2015)
Published in Cancer research (Chicago, Ill.) (01.08.2015)
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Journal Article
Abstract 1738: JNJ-42756493 is an inhibitor of FGFR-1, 2, 3 and 4 with nanomolar affinity for targeted therapy
Perera, Timothy, Jovcheva, Eleanora, Vialard, Jorge, Verhulst, Tinne, Esser, Norbert, Wroblowski, Berthold, Gilissen, Ron, Freyne, Eddy, King, Peter, Platero, Suso, Querolle, Olivier, Mevellec, Laurence, Murray, Christopher, Fazal, Lynsey, Saxty, Gordon, Ward, George, Squires, Matthew, Thompson, Neil, Newell, David, Angibaud, Patrick
Published in Cancer research (Chicago, Ill.) (01.10.2014)
Published in Cancer research (Chicago, Ill.) (01.10.2014)
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ASK1 저해성 피롤로피리미딘 및 피롤로피리딘 유도체
GIBSON KARL RICHARD, AMANTINI DAVID, VUJASINOVIC INES, SAXTY GORDON, POLJAK TANJA, ZIHER DINKO, WITTY DAVID, MESIC MILAN
Year of Publication 16.03.2020
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Year of Publication 16.03.2020
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BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY
ILDIKO MARIA BUCK, GIANNI CHESSARI, CHRISTOPHER NORBERT JOHNSON, SAXTY GORDON, NICOLA ELISABETH WILSHER, TAMANINI EMILIANO, JAMES EDWARD HARVEY DAY, CHARLOTTE MARY GRIFFITHS-JONES, STEVEN HOWARD
Year of Publication 12.11.2020
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Year of Publication 12.11.2020
Patent