1166854-99-4Relevant academic research and scientific papers
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase
Grey, Ron,Pierce, Albert C.,Bemis, Guy W.,Jacobs, Marc D.,Moody, Cameron Stuver,Jajoo, Rahul,Mohal, Narinder,Green, Jeremy
scheme or table, p. 3019 - 3022 (2010/01/16)
A series of substituted 3-aryl-6-amino-triazolo[4,3-b]pyridazines were identified as highly selective inhibitors of Pim-1 kinase. Initial exploration identified compound 24 as a potent, selective inhibitor, limited in its utility by poor solubility and permeability. Understanding the unusual ATP-binding site of the Pim kinases and X-ray crystallographic data on compound 24 led to design improvements in this class of inhibitor. This resulted in compound 29, a selective, soluble and permeable inhibitor of Pim-1.
