Compound, composition, and method of activating GIRK potassium channel and use of same for treating conditions of interest
The present invention provides small molecule activators of GIRK potassium channels and methods for use thereof.
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Page/Page column 31; 32; 33
(2015/07/07)
Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators
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.
Ramos-Hunter, Susan J.,Engers, Darren W.,Kaufmann, Kristian,Du, Yu,Lindsley, Craig W.,Weaver, C. David,Sulikowski, Gary A.
p. 5195 - 5198
(2013/09/12)
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