PubMed 23916258

Referenced in Channelpedia wiki pages of: none

Automatically associated channels: Kir2.1 , Kir2.2 , Kir3.1 , Kir3.2 , Kv4.1

Title: Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators.

Authors: Susan J Ramos-Hunter, Darren W Engers, Kristian Kaufmann, Yu Du, Craig W Lindsley, C David Weaver, Gary A Sulikowski

Journal, date & volume: Bioorg. Med. Chem. Lett., 2013 Sep 15 , 23, 5195-8

PubMed link:

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.