883045-67-8Relevant academic research and scientific papers
Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators
Ramos-Hunter, Susan J.,Engers, Darren W.,Kaufmann, Kristian,Du, Yu,Lindsley, Craig W.,Weaver, C. David,Sulikowski, Gary A.
, p. 5195 - 5198 (2013)
This Letter describes a novel series of GIRK activators identified through an HTS campaign. The HTS lead was a potent and efficacious dual GIRK1/2 and GIRK1/4 activator. Further chemical optimization through both iterative parallel synthesis and fragment library efforts identified dual GIRK1/2 and GIRK1/4 activators as well as the first examples of selective GIRK1/4 activators. Importantly, these compounds were inactive on GIRK2 and other non-GIRK1 containing GIRK channels, and SAR proved shallow.
