Publications by authors named "Philip A MacFaul"

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Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.
Bernard Barlaam, Elaine Cadogan, Andrew Campbell, Nicola Colclough, Allan Dishington, Philip A MacFaul

ACS Med Chem Lett· August 2018

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The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one).
Kurt G Pike, Bernard Barlaam, Elaine Cadogan, Andrew Campbell, Yingxue Chen, Philip A MacFaul

J Med Chem· May 2018

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Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.
James S Scott, Andrew Bailey, Robert D M Davies, Sébastien L Degorce, Philip A MacFaul

ACS Med Chem Lett· January 2016

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Aortic Binding of AZD5248: Mechanistic Insight and Reactivity Assays To Support Lead Optimzation.
Ryan A Bragg, Simon Brocklehurst, Frida Gustafsson, James Goodman, Kevin Hickling, Philip A MacFaul

Chem Res Toxicol· October 2015

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Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.
James S Scott, Suzanne S Bowker, Katy J Brocklehurst, Hayley S Brown, David S Clarke, Philip A MacFaul

J Med Chem· November 2014

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Conformational restriction in a series of GPR119 agonists: differences in pharmacology between mouse and human.
James S Scott, Katy J Brocklehurst, Hayley S Brown, David S Clarke, Helen Coe, Philip A MacFaul

Bioorg Med Chem Lett· June 2013

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Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.
James J Crawford, Peter W Kenny, Jonathan Bowyer, Calum R Cook, Jonathan E Finlayson, Philip A Macfaul

J Med Chem· October 2012

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Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.
Alexander G Dossetter, Jonathan Bowyer, Calum R Cook, James J Crawford, Jonathan E Finlayson, Philip A MacFaul

Bioorg Med Chem Lett· September 2012

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(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.
Alexander G Dossetter, Howard Beeley, Jonathan Bowyer, Calum R Cook, James J Crawford, Philip A MacFaul

J Med Chem· July 2012

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Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation.
James S Scott, Alan M Birch, Katy J Brocklehurst, Anders Broo, Hayley S Brown, Philip A Macfaul

J Med Chem· June 2012

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Selective non zinc binding inhibitors of MMP13.
Chris De Savi, Andrew D Morley, Attilla Ting, Ian Nash, Kostas Karabelas, Philip A Macfaul

Bioorg Med Chem Lett· July 2011

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A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.
David Buttar, Nicola Colclough, Stefan Gerhardt, Philip A MacFaul, Scott D Phillips

Bioorg Med Chem· November 2010

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Novel inhibitors of the alphavbeta3 integrin--lead identification strategy.
David Elliot, Eleanor Henshaw, Philip A MacFaul, Andrew D Morley, Peter Newham

Bioorg Med Chem Lett· August 2009

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5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.
Andrew D Morley, Peter W Kenny, Brenda Burton, Robert A Heald, Philip A Macfaul

Bioorg Med Chem Lett· March 2009

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A simple in vitro assay for assessing the reactivity of nitrile containing compounds.
Philip A MacFaul, Andrew D Morley, James J Crawford

Bioorg Med Chem Lett· February 2009

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Measurement of N-H Bond Strengths in Aromatic Amines by Photoacoustic Calorimetry(1).
Philip A. MacFaul, D. D. M. Wayner, K. U. Ingold

J Org Chem· May 1997

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