Claude Barberis, Neil Moorcroft, Chris Arendt, Mikhail Levit, Sandra Moreno-Mazza, Joseph Batchelor, Ingrid Mechin, Tahir Majid
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Discovery of N-Substituted 7-Azaindoles as PIM1 Kinase Inhibitors – Part I
Sep 18, 2017
Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4- yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7
Jul 17, 2017
Nigel Alan Swain, Dave Batchelor, Serge Beaudoin, Bruce M. Bechle, Paul A Bradley, Alan D Brown, Bruce Brown, Ken J Butcher, Richard P Butt, Mark L Chapman, Stephen Denton, David Ellis, Sebastien Galan, Stephen M Gaulier, Ben S Greener, Marcel J. de Groot, Mel S Glossop, Ian K Gurrell, Jo Hannam, Matthew S Johnson, Zhixin Lin, Christopher J Markworth, Brian E Marron, David S Millan, Shoko Nakagawa, Andy Pike, David Printzenhoff, David J Rawson, Sarah J Ransley, Steven M Reister, Kosuke Sasaki, R Ian Storer, Paul Anthony Stupple, and Christopher W West
Ion-pulling simulations provide insights into the mechanisms of channel opening of the skeletal muscle ryanodine receptor
Jun 05, 2017
David D. Mowrey, Le Xu, Yingwu Mei, Daniel A. Pasek, Gerhard Meissner, and Nikolay V. Dokholyan
The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics
Apr 26, 2017
D. C. Pryde, N. A. Swain, P. A. Stupple, C. W. West, B. Marron, C. J. Markworth, D. Printzenhoff, Z. Lin, P. J. Cox, R. Suzuki, S. McMurray, G. J. Waldron, C. E. Payne, J. S. Warmus and M. L. Chapman
The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels
Aug 31, 2016
Jonathan W. Theile, Matthew D. Fuller, and Mark L. Chapman
Biophysical and Pharmacological Characterization of Nav1.9 Voltage Dependent Sodium Channels Stably Expressed in HEK-293 Cells
Aug 24, 2016
Zhixin Lin, Sonia Santos, Karen Padilla, David Printzenhoff, Neil A. Castle
Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release
Apr 06, 2016
Aristos J. Alexandrou, Adam R. Brown, Mark L. Chapman, Mark Estacion, Jamie Turner, Malgorzata A. Mis, Anna Wilbrey, Elizabeth C. Payne, Alex Gutteridge, Peter J. Cox, Rachel Doyle, David Printzenhoff, Zhixin Lin, Brian E. Marron, Christopher West, Nigel A. Swain, R. Ian Storer, Paul Stupple, Neil A. Castle, James A. Hounshell, Mirko Rivara, Andrew Randall, Sulayman D. Dib-Hajj, Douglas Krafte, Stephen G. Waxman, Manoj K. Patel, Richard P. Butt, Edward B. Stevens
APOL1 kidney disease risk variants cause cytotoxicity by depleting cellular potassium and inducing stress-activated protein kinases
Nov 21, 2015
Opeyemi A. Olabisi, Jia-Yue Zhang, Lynn VerPlank, Nathan Zahler, Salvatore DiBartolo III, John F. Heneghan, Johannes S. Schlöndorff, Jung Hee Suh, Paul Yan, Seth L. Alper, David J. Friedman, and Martin R. Pollak
Validation of ion channel targets
Nov 05, 2015
Aaron C Gerlach and Brett M Antonio
SAR156497, an Exquisitely Selective Inhibitor of Aurora Kinases
Aug 29, 2015
Jean-Christophe Carry, Franco̧is Clerc, Hervé Minoux, Laurent Schio, Jacques Mauger, Anil Nair, Eric Parmantier, Ronan LeMoigne, Cécile Delorme, Jean-Paul Nicolas, Alain Krick, Pierre-Yves Abećassis, Véronique Crocq-Stuerga, Stéphanie Pouzieux, Laure Delarbre, Sébastien Maignan, Thomas Bertrand, Kirsten Bjergarde, Nina Ma,Sylvette Lachaud, Houlfa Guizani, Reḿi Lebel, Gilles Doerflinger, Sylvie Monget, Sebastien Perron, Francis Gasse, Odile Angouillant-Boniface, Bruno Filoche-Romme,́ Michel Murer, Sylvie Gontier, CeĺinePrev́ost, Marie-Line Monteiro, Cećile Combeau