Back Cover: Discovery of a Highly Selective PLD2 Inhibitor (ML395): A New Probe with Improved Physiochemical Properties and Broad-Spectrum Antiviral Activity against Influenza Strains (ChemMedChem 12/2014)

Further chemical optimization of the halopemide-derived family of dual phospholipaseD1/2 (PLD1/2) inhibitors afforded ML395 (VU0468809), a potent, >80-fold PLD2 selective allosteric inhibitor (cellular PLD1, IC50 >30000nM; cellular PLD2, IC50 =360nM). Moreover, ML395 possesses an attractive in...

Full description

Saved in:
Bibliographic Details
Published inChemMedChem Vol. 9; no. 12; p. 2820
Main Authors O'Reilly, Matthew C., Oguin III, Thomas H., Scott, Sarah A., Thomas, Paul G., Locuson, Charles W., Morrison, Ryan D., Daniels, J. Scott, Brown, H. Alex, Lindsley, Craig W.
Format Journal Article
LanguageEnglish
Published Weinheim WILEY-VCH Verlag 01.12.2014
Wiley Subscription Services, Inc
Subjects
antivirals
inhibitors
lipids
Pharmacology
phospholipase D
PLD2
Online AccessGet full text
ISSN1860-7179
1860-7187
DOI10.1002/cmdc.201490047

Cover

More Information
Summary:Further chemical optimization of the halopemide-derived family of dual phospholipaseD1/2 (PLD1/2) inhibitors afforded ML395 (VU0468809), a potent, >80-fold PLD2 selective allosteric inhibitor (cellular PLD1, IC50 >30000nM; cellular PLD2, IC50 =360nM). Moreover, ML395 possesses an attractive in vitro DMPK profile, improved physiochemical properties, ancillary pharmacology (Eurofins Panel) cleaner than any other reported PLD inhibitor, and has been found to possess interesting activity as an antiviral agent in cellular assays against a range of influenza strains (H1, H3, H5 and H7).
Bibliography:istex:8C1B70ADF93B4756E02D57F131A64983AE1E3B3B
ArticleID:CMDC201490047
ark:/67375/WNG-5R0GSWQ6-H
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 14
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.201490047