1042983-66-3Relevant academic research and scientific papers
Structure-based optimization of aminopyridines as PKCθ inhibitors
Jimenez, Juan-Miguel,Davis, Christopher,Boyall, Dean,Fraysse, Damien,Knegtel, Ronald,Settimo, Luca,Young, Stephen,Bolton, Claire,Chiu, Peter,Curnock, Adam,Rasmussen, Richele,Tanner, Adam,Ager, Ian
, p. 4645 - 4649 (2012)
The identification of a novel series of PKCθ inhibitors and subsequent optimization using docking based on a crystal structure of PKCθ is described. SAR was rapidly generated around an amino pyridine-ketone hit; (6-aminopyridin-2-yl)(2-aminopyridin-3-yl)methanone 2 leading to compound 21 which significantly inhibits production of IL-2 in a mouse SEB-IL2 model.
