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Bioorg Med Chem Lett. 2013 Sep 15;23(18):5195-8. doi: 10.1016/j.bmcl.2013.07.002. Epub 2013 Jul 18.

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

Author information

1
Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA.

Abstract

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.

KEYWORDS:

Activators; GIRK; K(ir)3.x; Thallium flux

PMID:
23916258
PMCID:
PMC4066871
DOI:
10.1016/j.bmcl.2013.07.002
[Indexed for MEDLINE]
Free PMC Article

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