Publications by authors named "Gavin Whitlock"

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The Pandemic Response Box─Accelerating Drug Discovery Efforts after Disease Outbreaks.
Kirandeep Samby, Dominique Besson, Anirban Dutta, Buddhadev Patra, Angelique Doy, Gavin Whitlock

ACS Infect Dis· April 2022

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DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
Charles E Mowbray, Stéphanie Braillard, Paul A Glossop, Gavin A Whitlock, Robert T Jacobs

J Med Chem· November 2021

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Preclinical trial of a MAP4K4 inhibitor to reduce infarct size in the pig: does cardioprotection in human stem cell-derived myocytes predict success in large mammals?
Maaike Te Lintel Hekkert, Gary Newton, Kathryn Chapman, Rehan Aqil, Robert Downham, Gavin Whitlock

Basic Res Cardiol· May 2021

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Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
Peter Jones, R Ian Storer, Yogesh A Sabnis, Florian M Wakenhut, Gavin A Whitlock

J Med Chem· January 2017

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Quantitative Chemical Proteomic Profiling of Ubiquitin Specific Proteases in Intact Cancer Cells.
Jennifer A Ward, Lauren McLellan, Martin Stockley, Karl R Gibson, Gavin A Whitlock

ACS Chem Biol· December 2016

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Novel Amino-pyrazole Ureas with Potent In Vitro and In Vivo Antileishmanial Activity.
Charles E Mowbray, Stéphanie Braillard, William Speed, Paul A Glossop, Gavin A Whitlock

J Med Chem· December 2015

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Small-molecule anti-inflammatory drug compositions for the treatment of asthma: a patent review (2013 - 2014).
Paul Glossop, Gavin Whitlock, Karl Gibson

Expert Opin Ther Pat· July 2015

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Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors.
R Ian Storer, Paul E Brennan, Alan D Brown, Peter J Bungay, Kelly M Conlon, Gavin A Whitlock

J Med Chem· June 2014

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Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform.
Bimbisar Desai, Karen Dixon, Elizabeth Farrant, Qixing Feng, Karl R Gibson, Gavin Whitlock

J Med Chem· April 2013

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Identification of type-II inhibitors using kinase structures.
Frank Lovering, Joseph McDonald, Gavin A Whitlock, Paul A Glossop, Chris Phillips

Chem Biol Drug Des· November 2012

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Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.
Mark D Andrews, Paul V Fish, Julian Blagg, Tiffini K Brabham, Paul E Brennan, Gavin A Whitlock

Bioorg Med Chem Lett· May 2011

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Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.
M Jonathan Fray, Paul V Fish, Gillian A Allan, Gerwyn Bish, Nick Clarke, Gavin A Whitlock

Bioorg Med Chem Lett· June 2010

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Understanding CYP2D6 interactions.
Marcel J de Groot, Florian Wakenhut, Gavin Whitlock, Ruth Hyland

Drug Discov Today· October 2009

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Pharmacological properties of 2-((R-5-chloro-4-methoxymethylindan-1-yl)-1H-imidazole (PF-3774076), a novel and selective alpha1A-adrenergic partial agonist, in in vitro and in vivo models of urethral function.
Kelly Conlon, Clare Christy, Simon Westbrook, Gavin Whitlock, Lee Roberts

J Pharmacol Exp Ther· September 2009

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Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence.
Paul E Brennan, Gavin A Whitlock, Danny K H Ho, Kelly Conlon, Gordon McMurray

Bioorg Med Chem Lett· September 2009

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N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.
Florian Wakenhut, Gill A Allan, Paul V Fish, M Jonathan Fray, Anthony C Harrison, Gavin A Whitlock

Bioorg Med Chem Lett· September 2009

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Potent and selective alpha1A adrenoceptor partial agonists--novel imidazole frameworks.
Gavin A Whitlock, Paul E Brennan, Lee R Roberts, Alan Stobie

Bioorg Med Chem Lett· June 2009

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6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha1A adrenoceptor partial agonists.
Lee R Roberts, Paul V Fish, R Ian Storer, Gavin A Whitlock

Bioorg Med Chem Lett· June 2009

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4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: design, synthesis and structure-activity relationships.
Paul V Fish, Mark D Andrews, M Jonathan Fray, Alan Stobie, Florian Wakenhut, Gavin A Whitlock

Bioorg Med Chem Lett· May 2009

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Chloroquine-astemizole hybrids with potent in vitro and in vivo antiplasmodial activity.
Chitalu C Musonda, Gavin A Whitlock, Michael J Witty, Reto Brun, Marcel Kaiser

Bioorg Med Chem Lett· January 2009

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Synthesis and evaluation of 2-pyridyl pyrimidines with in vitro antiplasmodial and antileishmanial activity.
Chitalu C Musonda, Gavin A Whitlock, Michael J Witty, Reto Brun, Marcel Kaiser

Bioorg Med Chem Lett· January 2009

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Novel 2-imidazoles as potent, selective and CNS penetrant alpha1A adrenoceptor partial agonists.
Lee R Roberts, Justin Bryans, Kelly Conlon, Gordon McMurray, Alan Stobie, Gavin A Whitlock

Bioorg Med Chem Lett· December 2008

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Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity.
Paul V Fish, Nancy S Barta, David L F Gray, Thomas Ryckmans, Alan Stobie, Gavin A Whitlock

Bioorg Med Chem Lett· August 2008

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N-Benzyl-N-(pyrrolidin-3-yl)carboxamides as a new class of selective dual serotonin/noradrenaline reuptake inhibitors.
Florian Wakenhut, Paul V Fish, M Jonathan Fray, Ian Gurrell, James E Mills, Gavin A Whitlock

Bioorg Med Chem Lett· August 2008

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Pyridyl-phenyl ether monoamine reuptake inhibitors: Impact of lipophilicity on dual SNRI pharmacology and off-target promiscuity.
Gavin A Whitlock, Paul V Fish, M Jonathan Fray, Alan Stobie, Florian Wakenhut

Bioorg Med Chem Lett· May 2008

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