Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Ashvin Mistry"'
Autor:
Richard Goodwin, Fiona Thomson, John W. Clark, Brad Sherborne, Lynn Watson, Angus R. Brown, Morag Grassie, Jack Pick, Angela Cowley, Olaf Nimz, J. Richard Morphy, Lorraine McIntosh, Niall M. Hamilton, Littlewood Peter Thomas Albert, Alasdair Smith, Koc-Kan Ho, Michael Speake, Alison Hillier, Ashvin Mistry, Michael Bosies, Simon James Anthony Grove, Mark Craighead, Theresa McIntyre, Michael Kiczun, Grant Emma Jane, Moira A. Elmore, Hannah Hampson, Mark Weston, Susan MacDonald, Susan Goutcher, Scott J. Lusher, Gayle Spinks, Zoran Rankovic, Michael Ohlmeyer, Helen Cameron, Alistair Firth, Steven G. Kultgen, Celia Kingsbury
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:137-140
High-throughput screening of 3.87 million compounds delivered a novel series of non-steroidal GR antagonists. Subsequent rounds of optimisation allowed progression from a non-selective ligand with a poor ADMET profile to an orally bioavailable, selec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d62da153327bd28fcc24657573e661d2
https://doi.org/10.1016/j.bmcl.2010.11.054
https://doi.org/10.1016/j.bmcl.2010.11.054
Autor:
Hortense Deronzier, Cecile Dorleans, John Waller, Laurent Saniere, Andre Fouquet, Fiona Elizabeth Andrews, Mark Baugh, J.C.M. Uitdehaag, George McGarry, Phil Jones, Ann Mitchell, Emma Kinghorn, Eric Nicolai, Wilson Caulfield, Zoran Rankovic, Dominique Potin, Mario van Zeeland, Wullie Arbuckle, Jennifer Kerr, Jiaqiang Cai, Mark Wheaton Anderson, Iain Martin, Maureen Dempster, Ashvin Mistry, François Chevallier, William Finlay, Clive Long, Robinson John E, Xavier Fradera, Paul Westwood, Iain Cumming
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6237-6241
Several structure-guided optimisation strategies were explored in order to improve the hERG selectivity profile of cathepsin K inhibitor 1 , whilst maintaining its otherwise excellent in vitro and in vivo profile. Ultimately, attenuation of c log P a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dbcfb747e700da9944dc50d293047fcc
https://doi.org/10.1016/j.bmcl.2010.08.101
https://doi.org/10.1016/j.bmcl.2010.08.101
Autor:
Eric Nicolai, Clive Long, Ann Mitchell, Maureen Dempster, William Hamilton, Jennifer Kerr, Cecile Dorleans, Iain Martin, Paul Scullion, Hortense Deronzier, John Bruin, Emma Hamilton, Zoran Rankovic, Andre Fouquet, John Robinson, John Waller, Laurent Saniere, Mark Baugh, Fiona Andrews, Jiaqiang Cai, Joost C.M. Uitdehaag, Wilson Caulfield, Dominique Potin, Ashvin Mistry, François Chevallier, Paul Westwood, Emma Kinghorn, George McGarry, Iain Cumming, Mario van Zeeland, X. Fradera
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1524-1527
Morphing structural features of HTS-derived chemotypes led to the discovery of novel 2-cyano-pyrimidine inhibitors of cathepsin K with good pharmacokinetic profiles, for example, compound 20 showed high catK potency (IC(50)=4nM), >580-fold selectivit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c3024221a3f1580ea5f971d2c310f2b7
https://doi.org/10.1016/j.bmcl.2010.01.100
https://doi.org/10.1016/j.bmcl.2010.01.100
Autor:
Sylviane Boucharens, Joost C.M. Uitdehaag, Jonathan Gillespie, Mario van Zeeland, Zoran Rankovic, Jiaqiang Cai, Maureen Dempster, Clive Long, Iain Cumming, Ann Mitchell, Emma Hamilton, Ashvin Mistry, Craig Jamieson, Angela King, X. Fradera
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(5)
A novel dioxo-triazine series of cathepsin K inhibitors was identified from HTS. A rapid exploratory programme led to the discovery of potent and selective cathepsin K inhibitors, typified by compound 24 which displayed IC(50) values of 17nM against
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::53fdab9708c58710341cb4f40df927f7
https://pubmed.ncbi.nlm.nih.gov/20153187
https://pubmed.ncbi.nlm.nih.gov/20153187
Autor:
Morag Ferguson, Jean E. Cottney, Darren Edwards, James Baker, Jim Cairns, Paul Westwood, Fiona Jeremiah, Jason Tierney, Andrea K. Houghton, Mark York, Richard Goodwin, Phillip M. Cowley, Glenn Walker, Ashvin Mistry, Morag Easson, Iain Cumming, Richard Morphy, Wilson Caulfield, Julia M. Adam, Takao Kiyoi, Elizabeth Margaret Moir
Publikováno v:
MedChemComm. 1:54
A novel CB1 receptor agonist lead series was identified using a high-throughput screening approach. The initial screen afforded a single confirmed hit with poor water solubility. Structural variations were explored with the aim of introducing water s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::50a9771d81118999bd825e636e929401
https://doi.org/10.1039/c0md00022a
https://doi.org/10.1039/c0md00022a