Journal article
Lead Optimization of Positive Allosteric KV7.2/3 Channel Modulators toward Improved Balance of Lipophilicity and Aqueous Solubility
Abstract
The voltage-gated potassium channel KV7.2/3 is gaining attention for its association with several medical indications. While recently reported, potent compounds aimed to fill the therapeutic gap left by market-withdrawn activators, key physicochemical parameters did not meet the requirements of potential drug candidates. Targeting the membrane-located channel requires subtly balancing lipophilicity, activity, and aqueous solubility. This …
Authors
Lemke J; Mengers N; Schmidt L; Schulig L; König S; Rosendahl P; Bartz F-M; Garscha U; Bednarski PJ; Link A
Journal
Journal of Medicinal Chemistry, Vol. 68, No. 8, pp. 8377–8399
Publisher
American Chemical Society (ACS)
Publication Date
April 24, 2025
DOI
10.1021/acs.jmedchem.4c03112
ISSN
0022-2623