X-ray Crystal Structure of the Novel Enhanced-Affinity Glucocorticoid Agonist Fluticasone Furoate in the Glucocorticoid Receptor−Ligand Binding Domain
Biggadike, Keith, Bledsoe, Randy K, Hassell, Anne M, Kirk, Barrie E, McLay, Iain M, Shewchuk, Lisa M, Stewart, Eugene L
Published in Journal of medicinal chemistry (26.06.2008)
Published in Journal of medicinal chemistry (26.06.2008)
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Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor
Biggadike, Keith, Bledsoe, Randy K, Coe, Diane M, Cooper, Tony W.J, House, David, Iannone, Marie A, Macdonald, Simon J.F, Madauss, Kevin P, McLay, Iain M, Shipley, Tracy J, Taylor, Simon J, Tran, Thuy B, Uings, Iain J, Weller, Victoria, Williams, Shawn P
Published in Proceedings of the National Academy of Sciences - PNAS (27.10.2009)
Published in Proceedings of the National Academy of Sciences - PNAS (27.10.2009)
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Synthesis and Structure−Activity Relationships of Long-acting β2 Adrenergic Receptor Agonists Incorporating Metabolic Inactivation: An Antedrug Approach
Procopiou, Panayiotis A, Barrett, Victoria J, Bevan, Nicola J, Biggadike, Keith, Box, Philip C, Butchers, Peter R, Coe, Diane M, Conroy, Richard, Emmons, Amanda, Ford, Alison J, Holmes, Duncan S, Horsley, Helen, Kerr, Fern, Li-Kwai-Cheung, Anne-Marie, Looker, Brian E, Mann, Inderjit S, McLay, Iain M, Morrison, Valerie S, Mutch, Peter J, Smith, Claire E, Tomlin, Paula
Published in Journal of medicinal chemistry (10.06.2010)
Published in Journal of medicinal chemistry (10.06.2010)
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Dissociated Nonsteroidal Glucocorticoid Receptor Modulators; Discovery of the Agonist Trigger in a Tetrahydronaphthalene−Benzoxazine Series
Barker, Mike, Clackers, Margaret, Copley, Royston, Demaine, Derek A, Humphreys, Davina, Inglis, Graham G. A, Johnston, Michael J, Jones, Haydn T, Haase, Michael V, House, David, Loiseau, Richard, Nisbet, Lesley, Pacquet, Francois, Skone, Philip A, Shanahan, Stephen E, Tape, Dan, Vinader, Victoria M, Washington, Melanie, Uings, Iain, Upton, Richard, McLay, Iain M, Macdonald, Simon J. F
Published in Journal of medicinal chemistry (13.07.2006)
Published in Journal of medicinal chemistry (13.07.2006)
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Synthesis and Structure−Activity Relationships of Long-acting β2 Adrenergic Receptor Agonists Incorporating Arylsulfonamide Groups
Procopiou, Panayiotis A, Barrett, Victoria J, Bevan, Nicola J, Biggadike, Keith, Butchers, Peter R, Coe, Diane M, Conroy, Richard, Edney, Dean D, Field, Rita N, Ford, Alison J, Guntrip, Stephen B, Looker, Brian E, McLay, Iain M, Monteith, Michael J, Morrison, Valerie S, Mutch, Peter J, Richards, Stephen A, Sasse, Rosemary, Smith, Claire E
Published in Journal of medicinal chemistry (23.04.2009)
Published in Journal of medicinal chemistry (23.04.2009)
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Nonsteroidal Glucocorticoid Agonists: Tetrahydronaphthalenes with Alternative Steroidal A-Ring Mimetics Possessing Dissociated (Transrepression/Transactivation) Efficacy Selectivity
Biggadike, Keith, Boudjelal, Mohamed, Clackers, Margaret, Coe, Diane M, Demaine, Derek A, Hardy, George W, Humphreys, Davina, Inglis, Graham G. A, Johnston, Michael J, Jones, Haydn T, House, David, Loiseau, Richard, Needham, Deborah, Skone, Philip A, Uings, Iain, Veitch, Gemma, Weingarten, Gordon G, McLay, Iain M, Macdonald, Simon J. F
Published in Journal of medicinal chemistry (27.12.2007)
Published in Journal of medicinal chemistry (27.12.2007)
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Analysis of Neighborhood Behavior in Lead Optimization and Array Design
Papadatos, George, Cooper, Anthony W. J, Kadirkamanathan, Visakan, Macdonald, Simon J. F, McLay, Iain M, Pickett, Stephen D, Pritchard, John M, Willett, Peter, Gillet, Valerie J
Published in Journal of Chemical Information and Modeling (23.02.2009)
Published in Journal of Chemical Information and Modeling (23.02.2009)
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An Algorithm-Directed Two-Component Library Synthesized Via Solid-Phase Methodology Yielding Potent and Orally Bioavailable p38 MAP Kinase Inhibitors
McKenna, Jeffrey M, Halley, Frank, Souness, John E, McLay, Iain M, Pickett, Stephen D, Collis, Alan J, Page, Kenneth, Ahmed, Imtiaz
Published in Journal of medicinal chemistry (23.05.2002)
Published in Journal of medicinal chemistry (23.05.2002)
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Drug Rings Database with Web Interface. A Tool for Identifying Alternative Chemical Rings in Lead Discovery Programs
Lewell, Xiao Qing, Jones, Andrew C, Bruce, Craig L, Harper, Gavin, Jones, Matthew M, Mclay, Iain M, Bradshaw, John
Published in Journal of medicinal chemistry (17.07.2003)
Published in Journal of medicinal chemistry (17.07.2003)
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The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs
Watson, Nigel S., Adams, Carl, Belton, David, Brown, David, Burns-Kurtis, Cynthia L., Chaudry, Laiq, Chan, Chuen, Convery, Máire A., Davies, David E., Exall, Anne M., Harling, John D., Irvine, Stephanie, Irving, Wendy R., Kleanthous, Savvas, McLay, Iain M., Pateman, Anthony J., Patikis, Angela N., Roethke, Theresa J., Senger, Stefan, Stelman, Gary J., Toomey, John R., West, Robert I., Whittaker, Caroline, Zhou, Ping, Young, Robert J.
Published in Bioorganic & medicinal chemistry letters (15.03.2011)
Published in Bioorganic & medicinal chemistry letters (15.03.2011)
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Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity
Diallo, Hawa, Angell, Davina C., Barnett, Heather A., Biggadike, Keith, Coe, Diane M., Cooper, Tony W.J., Craven, Andy, Gray, James R., House, David, Jack, Torquil I., Keeling, Steve P., Macdonald, Simon J.F., McLay, Iain M., Oliver, Samuel, Taylor, Simon J., Uings, Iain J., Wellaway, Natalie
Published in Bioorganic & medicinal chemistry letters (15.02.2011)
Published in Bioorganic & medicinal chemistry letters (15.02.2011)
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Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists
Barnett, Heather A., Coe, Diane M., Cooper, Tony W.J., Jack, Torquil I., Jones, Haydn T., Macdonald, Simon J.F., McLay, Iain M., Rayner, Natalie, Sasse, Rosemary Z., Shipley, Tracy J., Skone, Phil A., Somers, Graham I., Taylor, Simon, Uings, Iain J., Woolven, James M., Weingarten, Gordon G.
Published in Bioorganic & medicinal chemistry letters (2009)
Published in Bioorganic & medicinal chemistry letters (2009)
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Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists
Biggadike, Keith, Caivano, Matilde, Clackers, Margaret, Coe, Diane M., Hardy, George W., Humphreys, Davina, Jones, Haydn T., House, David, Miles-Williams, Annette, Skone, Philip A., Uings, Iain, Weller, Vicki, McLay, Iain M., Macdonald, Simon J.F.
Published in Bioorganic & medicinal chemistry letters (15.08.2009)
Published in Bioorganic & medicinal chemistry letters (15.08.2009)
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Design and Synthesis of New Nonsteroidal Glucocorticoid Modulators through Application of an “Agreement Docking” Method
Barker, Mike, Clackers, Margaret, Demaine, Derek A, Humphreys, Davina, Johnston, Michael J, Jones, Haydn T, Pacquet, Francois, Pritchard, John M, Salter, Mark, Shanahan, Stephen E, Skone, Philip A, Vinader, Victoria M, Uings, Iain, McLay, Iain M, Macdonald, Simon J. F
Published in Journal of medicinal chemistry (14.07.2005)
Published in Journal of medicinal chemistry (14.07.2005)
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Non-steroidal glucocorticoid agonists—The discovery of aryl pyrazoles as A-ring mimetics
Clackers, Margaret, Coe, Diane M., Demaine, Derek A., Hardy, George W., Humphreys, Davina, Inglis, Graham G.A., Johnston, Michael J., Jones, Haydn T., House, David, Loiseau, Richard, Minick, Doug J., Skone, Philip A., Uings, Iain, McLay, Iain M., Macdonald, Simon J.F.
Published in Bioorganic & medicinal chemistry letters (01.09.2007)
Published in Bioorganic & medicinal chemistry letters (01.09.2007)
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