Publications by authors named "Robin A Fairhurst"

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A 'One-Shot' strategy for preparative chiral sub/supercritical fluid chromatography with chiroptical detection accelerates purification and enhances characterization for drug discovery.
John Reilly, Marie-Anne Lozach, Aldo Meishammer, Marcel Reck, Robin A Fairhurst

J Chromatogr A· March 2025

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Adventures with the β-adrenoceptor Receptor: A Career Long Interest in Agonising One of the Most Widely Studied GPCRs.
Robin A Fairhurst

Chimia (Aarau)· August 2024

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Exploring the kinetic selectivity of drugs targeting the β -adrenoceptor.
David A Sykes, Mireia Jiménez-Rosés, John Reilly, Robin A Fairhurst, Steven J Charlton

Pharmacol Res Perspect· August 2022

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Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.
Robin A Fairhurst, Pascal Furet, Patricia Imbach-Weese, Frédéric Stauffer, Heinrich Rueeger

J Med Chem· June 2022

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Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
Robin A Fairhurst, Thomas Knoepfel, Nicole Buschmann, Catherine Leblanc, Robert Mah

J Med Chem· November 2020

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Correction to "2-Formylpyridyl Ureas as Highly Selective Reversible-Covalent Inhibitors of Fibroblast Growth Factor Receptor 4".
Thomas Knoepfel, Pascal Furet, Robert Mah, Nicole Buschmann, Catherine Leblanc, Robin A Fairhurst

ACS Med Chem Lett· November 2020

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FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer.
Andreas Weiss, Flavia Adler, Alexandra Buhles, Christelle Stamm, Robin A Fairhurst

Mol Cancer Ther· December 2019

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Pharmacological Characterization of a Novel 5-Hydroxybenzothiazolone-Derived -Adrenoceptor Agonist with Functional Selectivity for Anabolic Effects on Skeletal Muscle Resulting in a Wider Cardiovascular Safety Window in Preclinical Studies.
Magdalena Koziczak-Holbro, Dean F Rigel, Bérengère Dumotier, David A Sykes, Jeffrey Tsao, Robin A Fairhurst

J Pharmacol Exp Ther· May 2019

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Bile Acid Sequestration by Cholestyramine Mitigates FGFR4 Inhibition-Induced ALT Elevation.
Heiko S Schadt, Armin Wolf, Joerg Andreas Mahl, Kuno Wuersch, Philippe Couttet, Robin A Fairhurst

Toxicol Sci· May 2018

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2-Formylpyridyl Ureas as Highly Selective Reversible-Covalent Inhibitors of Fibroblast Growth Factor Receptor 4.
Thomas Knoepfel, Pascal Furet, Robert Mah, Nicole Buschmann, Catherine Leblanc, Robin A Fairhurst

ACS Med Chem Lett· March 2018

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Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region.
Robin A Fairhurst, Thomas Knoepfel, Catherine Leblanc, Nicole Buschmann, Christoph Gaul

Medchemcomm· August 2017

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Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors.
Robin A Fairhurst, Giorgio Caravatti, Vito Guagnano, Reiner Aichholz, Joachim Blanz

Bioorg Med Chem Lett· October 2016

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Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.
Callum J Dickson, Viktor Hornak, Camilo Velez-Vega, Daniel J J McKay, John Reilly, Robin A Fairhurst

J Med Chem· June 2016

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Long Receptor Residence Time of C26 Contributes to Super Agonist Activity at the Human β2 Adrenoceptor.
Elizabeth M Rosethorne, Michelle E Bradley, Karolina Gherbi, David A Sykes, Afrah Sattikar, Robin A Fairhurst

Mol Pharmacol· April 2016

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Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Robin A Fairhurst, Thomas H Marsilje, Stefan Stutz, Andreas Boos, Michel Niklaus

Bioorg Med Chem Lett· April 2016

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Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity.
Marc Gerspacher, Robin A Fairhurst, Robert Mah, Esther Roehn-Carnemolla, Pascal Furet

Bioorg Med Chem Lett· September 2015

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Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.
Robin A Fairhurst, Marc Gerspacher, Patricia Imbach-Weese, Robert Mah, Giorgio Caravatti

Bioorg Med Chem Lett· September 2015

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Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.
Robin A Fairhurst, Patricia Imbach-Weese, Marc Gerspacher, Giorgio Caravatti, Pascal Furet

Bioorg Med Chem Lett· September 2015

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The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.
Nicola Arnold, David Beattie, Michelle Bradley, Andrew Brearley, Lyndon Brown, Robin A Fairhurst

Bioorg Med Chem Lett· September 2014

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Observed drug-receptor association rates are governed by membrane affinity: the importance of establishing "micro-pharmacokinetic/pharmacodynamic relationships" at the β2-adrenoceptor.
David A Sykes, Cheryl Parry, John Reilly, Penny Wright, Robin A Fairhurst

Mol Pharmacol· April 2014

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Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.
Pascal Furet, Vito Guagnano, Robin A Fairhurst, Patricia Imbach-Weese, Ian Bruce

Bioorg Med Chem Lett· July 2013

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An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol.
David Beattie, David Beer, Michelle E Bradley, Ian Bruce, Steven J Charlton, Robin A Fairhurst

Bioorg Med Chem Lett· October 2012

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A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.
David Beattie, Michelle Bradley, Andrew Brearley, Steven J Charlton, Bernard M Cuenoud, Robin A Fairhurst

Bioorg Med Chem Lett· September 2010

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Efficacy is a contributing factor to the clinical onset of bronchodilation of inhaled beta(2)-adrenoceptor agonists.
Elizabeth M Rosethorne, Robert J Turner, Robin A Fairhurst, Steven J Charlton

Naunyn Schmiedebergs Arch Pharmacol· September 2010

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The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.
François Baur, David Beattie, David Beer, David Bentley, Michelle Bradley, Robin A Fairhurst

J Med Chem· May 2010

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