Publications

PAPERS

The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors

By Deaton, David N.; Do, Young; Holt, Jason; Jeune, Michael R.; Fritz Kramer, H.; 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.; Darren Stuart, J.; 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; E. D. Smith, Ian; Somers, Don O.; Sneddon, Helen F.; Uddin, Sorif; Cleasby, Anne; Mortenson, Paul N.; Richardson, Caroline; Saxty, Gordon

From Bioorganic & Medicinal Chemistry (2019), Ahead of Print.

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)

By 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

From Journal of Medicinal Chemistry (2018), 61(16), 7314-7329. |  Language: English, Database: CAPLUS

Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor

By 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.

From Molecular Cancer Therapeutics (2017), 16(6), 1010-1020.  |  Language: English, Database: CAPLUS

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

By 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;  et al

From Journal of Medicinal Chemistry (2016), 59(8), 3991-4006.  |  Language: English, Database: CAPLUS

Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors

By 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;  et al

From ACS Medicinal Chemistry Letters (2015), 6(7), 798-803.  |  Language: English, Database: CAPLUS

Identification of orally bioavailable small-molecule inhibitors of hematopoietic prostaglandin D2 synthase using X-ray fragment based drug discovery

By Saxty, Gordon; Norton, David; Affleck, Karen; Clapham, Dave; Cleasby, Anne; Coyle, Joe; Day, Philip; Frederickson, Martyn; Hancock, Ashley; Hobbs, Heather;  et al

From MedChemComm (2014), 5(2), 134-141.  |  Language: English, Database: CAPLUS

Potent, Selective Inhibitors of Fibroblast Growth Factor Receptor Define Fibroblast Growth Factor Dependence in Preclinical Cancer Models

By Squires, Matthew; Ward, George; Saxty, Gordon; Berdini, Valerio; Cleasby, Anne; King, Peter; Angibaud, Patrick; Perera, Tim; Fazal, Lynsey; Ross, Douglas;  et al

From Molecular Cancer Therapeutics (2011), 10(9), 1542-1552.  |  Language: English, Database: CAPLUS

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

By 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.;  et al

From Journal of Medicinal Chemistry (2008), 51(16), 4986-4999.  |  Language: English, Database: CAPLUS

Identification of Inhibitors of Protein Kinase B Using Fragment-Based Lead Discovery

By 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.;  et al

From Journal of Medicinal Chemistry (2007), 50(10), 2293-2296.  |  Language: English, Database: CAPLUS

BOOKS

Chapter 18: FBDD Applications to Kinase Drug Hunting (pages 425–446)

Gordon Saxty

Editor(s): Daniel A. Erlanson, Wolfgang Jahnke. Published Online: 8 JAN 2016

DOI: 10.1002/9783527683604

Current Trends in Macrocyclic Drug Discovery and beyond-Ro5

By Alihodzic Sulejman; Bukvic Mirjana; Elenkov Ivaylo J; Hutinec Antun; KostrunSanja; Pesic Dijana; Saxty Gordon*; Tomaskovic Linda; ZiherDinko

From Progress in medicinal chemistry (2018), 57(1), 113-233.

Current Trends in Macrocyclic Drug Discovery and beyond-Ro5

Gordon Saxty

Editor(s): Daniel A. Erlanson, Wolfgang Jahnke. Published Online: 8 JAN 2016

From Fragment-based Drug Discovery Lessons and Outlook CAPLUS