787591-39-3Relevant articles and documents
Investigation of the binding pocket of human hematopoietic prostaglandin (PG) D2 synthase (hH-PGDS): A tale of two waters
Trujillo, John I.,Kiefer, James R.,Huang, Wei,Day, Jacqueline E.,Moon, Joseph,Jerome, Gina M.,Bono, Christine P.,Kornmeier, Christine M.,Williams, Melanie L.,Kuhn, Cyrille,Rennie, Glen R.,Wynn, Thomas A.,Carron, Christopher P.,Thorarensen, Atli
scheme or table, p. 3795 - 3799 (2012/07/27)
The inhibition of hH-PGDS has been proposed as a potential target for the development of anti-allergic and anti-inflammatory drugs. Herein we describe our investigation of the binding pocket of this important enzyme and our observation that two water molecules bind to our inhibitors and the enzyme. A series of compounds were prepared to the probe the importance of the water molecules in determining the binding affinity of the inhibitors to the enzyme. The study provides insight into the binding requirements for the design of potent hH-PGDS inhibitors.
Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhbitors
-
Page 45-46, (2010/02/09)
The present invention relates to 8-amino-aryl-substituted imidazopyrazines which modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.