Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Michael David Barker"'
Autor:
Nicholas C. O. Tomkinson, Sophie M. Bertrand, Kenneth David Down, Brett Cosgrove, Michael David Barker
Physicochemical properties, such as solubility, are important when prioritising compounds for progression on a drug discovery project. There is limited literature around the systematic effects of core changes on thermodynamic solubility. This work de
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb089decaaa92b634c134279b6dc9737
https://strathprints.strath.ac.uk/76856/1/Cosgrove_etal_BMCL_2021_Investigating_the_effects_of_the_core_nitrogen_atom_configuration.pdf
https://strathprints.strath.ac.uk/76856/1/Cosgrove_etal_BMCL_2021_Investigating_the_effects_of_the_core_nitrogen_atom_configuration.pdf
Autor:
Michael David Barker, Emma J. Jones, Robert J. Watson, Huw D. Lewis, Cesar Ramirez-Molina, David Matthew Wilson, Marion C. Dickson, Robert P. Davis, Francis Louis Atkinson, Margarete Neu, Donald O. Somers, John Liddle
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:3458-3462
The discovery and lead optimisation of a novel series of SYK inhibitors is described. These were optimised for SYK potency and selectivity against Aurora B. Compounds were profiled in a human skin penetration study to identify a suitable candidate mo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ea0edda7c25304f4d66d8a85ae30e56a
https://doi.org/10.1016/j.bmcl.2018.09.022
https://doi.org/10.1016/j.bmcl.2018.09.022
Autor:
Alex Preston, Scott McCleary, Emma J. Jones, Huw D. Lewis, Michael David Barker, Robert J. Watson, Tracy Jane Shipley, Cesar Ramirez-Molina, Dave Lugo, Clement Douault, Robert P. Davis, David Matthew Wilson, Margarete Neu, Neil Stuart Garton, Edward Hooper-Greenhill, John Liddle, Don O. Somers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:4606-4612
The optimisation of the azanaphthyridine series of Spleen Tyrosine Kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over hERG activity. A go
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::60c70f363fa050d5a84cc13aacffd65e
https://doi.org/10.1016/j.bmcl.2016.08.070
https://doi.org/10.1016/j.bmcl.2016.08.070
Autor:
Rab K. Prinjha, Alex Preston, Inma Rioja, Roy Katso, Melanie Leveridge, Chun-wa Chung, Michael David Barker, Laurens Kruidenier, Gerard Joberty, Kevin Lee, Onkar M. P. Singh, Joanna Taylor, Matthew Campbell, Michelle Pemberton, Fiona Brown, Robert Eagle, Carl Haslam, David Matthew Wilson, Neil Stuart Garton, Tracy Jane Shipley, Colin J. Suckling, Philip G. Humphreys, Gerard Drewes, Laurie J. Gordon, Pamela Thomas, Jack A. Brown, Gail A. Seal, Thomas George Christopher Hayhow, Susan Marie Westaway
Publikováno v:
Journal of Medicinal Chemistry. 59:1370-1387
Following the discovery of cell penetrant pyridine-4-carboxylate inhibitors of the KDM4 (JMJD2) and KDM5 (JARID1) families of histone lysine demethylases (e.g., 1), further optimization led to the identification of non-carboxylate inhibitors derived
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1dd41f32203668dbba76c4b0b0fbc2e4
https://doi.org/10.1021/acs.jmedchem.5b01538
https://doi.org/10.1021/acs.jmedchem.5b01538
Autor:
Robert P. Davis, Kelly Locke, Rab K. Prinjha, Peter D. Craggs, Gang Yao, Chun-wa Chung, Kenneth E Lind, Oxana Polyakova, Jim E Coote, Daniel J. Slade, Jim Thorpe, John Liddle, David Matthew Wilson, Benjamin D. Bax, Denisa D. Wagner, Kimberly Martinod, Ryan P. Bingham, Yu Hua Chen, Kevin L. Bicker, Claire Maller, Matthew Campbell, Gerard Joberty, Huw D. Lewis, Dirk Eberhard, Martin Rüdiger, Gerard Drewes, Paul R. Thompson, Cecil E Rise, Robert J. Sheppard, Chris Patten, Stephen John Atkinson, Michael David Barker, Pamela Thomas
Publikováno v:
Nature chemical biology
PAD4 has been strongly implicated in the pathogenesis of autoimmune, cardiovascular and oncological diseases through clinical genetics and gene disruption in mice. New selective PAD4 inhibitors binding a calcium-deficient form of the PAD4 enzyme have
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::edf0de94c1b2987c42df9e5a113919ce
https://doi.org/10.1038/nchembio.1735
https://doi.org/10.1038/nchembio.1735
Autor:
Laurens Kruidenier, Rebecca Randle, Hawa Diallo, Inma Rioja, Clement Douault, Anne Rueger, Chun-wa Chung, Thomas George Christopher Hayhow, Rab K. Prinjha, Alex Preston, Roy Katso, Matthew Campbell, Michael David Barker, J. Mosley, Kevin Lee, Joanna Taylor, Marcel Muelbaier, Douglas W. Thomson, Gail A. Seal, Jack A. Brown, Susan Marie Westaway, Onkar M. P. Singh, Gerard Joberty, Philip G. Humphreys, Melanie Leveridge, Laurie J. Gordon, Pamela Thomas, Carl Haslam, Fiona Brown, John Liddle, Gerard Drewes, Robert Eagle, Robert J. Sheppard, David Matthew Wilson
Publikováno v:
Journal of medicinal chemistry. 59(4)
Optimization of KDM6B (JMJD3) HTS hit 12 led to the identification of 3-((furan-2-ylmethyl)amino)pyridine-4-carboxylic acid 34 and 3-(((3-methylthiophen-2-yl)methyl)amino)pyridine-4-carboxylic acid 39 that are inhibitors of the KDM4 (JMJD2) family of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::169f1f983c8269e73c78cea4fff0100e
https://pubmed.ncbi.nlm.nih.gov/26771107
https://pubmed.ncbi.nlm.nih.gov/26771107
Autor:
Heather Hobbs, Rick P. C. Cousins, Caroline Whitworth, Ruth R. Osborn, Cesar Ramirez-Molina, Giorgia Vicentini, Chris Ioannou, Chun-wa Chung, Jeremy John Payne, Michelle L. Heathcote, Michael David Barker, Sebastien Andre Campos, Paul Faulder, Mary A. Morse, William L. Rumsey, John Liddle, Daniel Terence Tape, John Martin Pritchard, Rick Williamson, Duncan S. Holmes, Paul Bamborough
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5222-5226
The lead optimization of a series of potent azaindole IKK2 inhibitors is described. Optimization of the human whole blood activity and selectivity over IKK1 in parallel led to the discovery of 16, a potent and selective IKK2 inhibitor showing good ef
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::66c01094b7cd1f9f02ade498d99ac86e
https://doi.org/10.1016/j.bmcl.2012.06.065
https://doi.org/10.1016/j.bmcl.2012.06.065
Autor:
Philip Alan Skone, Donald O. Somers, Marion C. Dickson, Nick Smithers, Ann Louise Walker, Thomas George Christopher Hayhow, Stuart G. Leach, Karen Leavens, Clement Douault, Emma J. Jones, Dorothy Elwes, Robert J. Watson, Margarete Neu, Robert P. Davis, Matthew Gray, Neil Stuart Garton, Clare I. Hobbs, Alex Preston, Michael David Barker, Vipulkumar Kantibhai Patel, Cesar Ramirez-Molina, Paul S. Carter, Scott McCleary, Gordon G. Weingarten, Huw D. Lewis, Francis Louis Atkinson, John Liddle, Tracy Jane Shipley, Neil R. Curtis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6188-6194
The lead optimisation of the diaminopyrimidine carboxamide series of spleen tyrosine kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over l
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58fce9afb90ca4e724d4726df2268b6f
https://doi.org/10.1016/j.bmcl.2011.07.082
https://doi.org/10.1016/j.bmcl.2011.07.082
Autor:
John Dawson, Michael David Barker, Stuart Holman, Joanne O. Wiseman, Margarete Neu, Lisa E. Ranshaw, Fiona S. Lucas, Duncan S. Holmes, Michael Kranz, Christopher J. Delves, Beth J. Clarke, Woodrow Michael David, Tony W. Dean, Don O. Somers, Steven B. Guntrip, Stuart P. Ballantine, Yemisi E. Solanke, Mika K. Lindvaal, Sharon Lisa Gough, Brian Evans, Ward Peter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1380-1385
Crystallography driven optimisation of a lead derived from similarity searching of the GSK compound collection resulted in the discovery of quinoline-3-carboxamides as highly potent and selective inhibitors of phosphodiesterase 4B. This series has be
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c7d1b7e1eca93eb6425d855b2b8ac1a8
https://doi.org/10.1016/j.bmcl.2009.01.045
https://doi.org/10.1016/j.bmcl.2009.01.045
Autor:
Jeremy John Payne, Geoff W. Mellor, Smith Kathryn Jane, Richard A. Williamson, Sebastien Andre Campos, Geoffrey J. Cutler, Caroline Whitworth, Mary A. Morse, Michael David Barker, Heather Hobbs, Rick P. C. Cousins, Duncan S. Holmes, Daniel Terence Tape, Paul Bamborough, John Martin Pritchard, John Liddle, Chris Ioannou
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(9)
The synthesis and SAR of a novel series of IKK2 inhibitors are described. Modification around the hinge binding region of the 7-azaindole led to a series of potent and selective inhibitors with good cellular activity.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bac9d3089c47e68ac4f0cac67941fe59
https://pubmed.ncbi.nlm.nih.gov/19349179
https://pubmed.ncbi.nlm.nih.gov/19349179