50419-85-7Relevant articles and documents
Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay
Knoepfel, Thomas,Nimsgern, Pierre,Jacquier, Sébastien,Bourrel, Marjorie,Vangrevelinghe, Eric,Glatthar, Ralf,Behnke, Dirk,Alper, Phil B.,Michellys, Pierre-Yves,Deane, Jonathan,Junt, Tobias,Zipfel, Géraldine,Limonta, Sarah,Hawtin, Stuart,Andre, Cedric,Boulay, Thomas,Loetscher, Pius,Faller, Michael,Blank, Jutta,Feifel, Roland,Betschart, Claudia
, p. 8276 - 8295 (2020/08/24)
Inappropriate activation of endosomal TLR7 and TLR8 occurs in several autoimmune diseases, in particular systemic lupus erythematosus (SLE). Herein, the development of a TLR8 antagonist competition assay and its application for hit generation of dual TLR7
Discovery, synthesis, and biological evaluation of thiazoloquin(az)olin(on)es as potent CD38 inhibitors
Haffner, Curt D.,Becherer, J. David,Boros, Eric E.,Cadilla, Rodolfo,Carpenter, Tiffany,Cowan, David,Deaton, David N.,Guo, Yu,Harrington, Wallace,Henke, Brad R.,Jeune, Michael R.,Kaldor, Istvan,Milliken, Naphtali,Petrov, Kim G.,Preugschat, Frank,Schulte, Christie,Shearer, Barry G.,Shearer, Todd,Smalley, Terrence L.,Stewart, Eugene L.,Stuart, J. Darren,Ulrich, John C.
, p. 3548 - 3571 (2015/05/05)
A series of thiazoloquin(az)olinones were synthesized and found to have potent inhibitory activity against CD38. Several of these compounds were also shown to have good pharmacokinetic properties and demonstrated the ability to elevate NAD levels in plasm
