Back to Search
Start Over
Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Sep2013, Vol. 23 Issue 18, p5195-5198. 4p. - Publication Year :
- 2013
-
Abstract
- 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. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 23
- Issue :
- 18
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 89885163
- Full Text :
- https://doi.org/10.1016/j.bmcl.2013.07.002