1034297-69-2Relevant articles and documents
Identification of indole inhibitors of human hematopoietic prostaglandin D2 synthase (hH-PGDS)
Edfeldt, Fredrik,Even?s, Johan,Lepist?, Matti,Ward, Alison,Petersen, Jens,Wissler, Lisa,Rohman, Mattias,Sivars, Ulf,Svensson, Karin,Perry, Matthew,Feierberg, Isabella,Zhou, Xiao-Hong,Hansson, Thomas,Narjes, Frank
, p. 2496 - 2500 (2015)
Abstract Human H-PGDS has shown promise as a potential target for anti-allergic and anti-inflammatory drugs. Here we describe the discovery of a novel class of indole inhibitors, identified through focused screening of 42,000 compounds and evaluated using a series of hit validation assays that included fluorescence polarization binding, 1D NMR, ITC and chromogenic enzymatic assays. Compounds with low nanomolar potency, favorable physico-chemical properties and inhibitory activity in human mast cells have been identified. In addition, our studies suggest that the active site of hH-PGDS can accommodate larger structural diversity than previously thought, such as the introduction of polar groups in the inner part of the binding pocket.
PYRIDINE BENZAMIDES AND PYRAZINE BENZAMIDES USED AS PKD INHIBITORS
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Page/Page column 88, (2008/12/06)
The present invention pertains generally to the field of therapeutic compounds,. arid more specifically to certain pyridine benzamide and pyrazine benzamide compounds (I) (referred to herein as PDBA and PZBA compounds) which, inter alia, inhibit protein kinase D (PKD) (e.g., PKD1, PKD2, PKD3). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PKD, and in the treatment of diseases and conditions that are mediated by PKD1 that are ameliorated by the inhibition of PKD, etc., including proliferative conditions such as cancer, etc.
