Lead Optimization of Positive Allosteric K<sub>V</sub>7.2/3 Channel Modulators toward Improved Balance of Lipophilicity and Aqueous Solubility

Lead Optimization of Positive Allosteric K<sub>V</sub>7.2/3 Channel Modulators toward Improved Balance of Lipophilicity and Aqueous Solubility

The voltage-gated potassium channel K<sub>V</sub>7.2/3 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 While recently reported, potent compounds aimed to fill the therapeutic gap left by market-withdrawn activators, key physicochemical parameters did not meet t...

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Bibliographic Details
Main Author: Jana Lemke (14554065) (author)
Other Authors: Nadine Mengers (21020570) (author), Louis Schmidt (8921705) (author), Lukas Schulig (6905666) (author), Stefanie König (1647862) (author), Pascal Rosendahl (21020573) (author), Frieda-Marie Bartz (12153469) (author), Ulrike Garscha (1811065) (author), Patrick J. Bednarski (1524088) (author), Andreas Link (613755) (author)
Published: 2025
Subjects:
Biochemistry
Medicine
Neuroscience
Pharmacology
Chemical Sciences not elsewhere classified
Information Systems not elsewhere classified
therapeutic gap left
slightly reduced potency
several medical indications
potential drug candidates
potent compounds aimed
key physicochemical parameters
dimensional bulky structure
increased solubility compared
42 vs 7
positive allosteric k
30 showed activity
7 vs 1
v </ sub
50 </ sub
aqueous solubility
1 μm
withdrawn activators
theoretically enhanced
target engagement
recently reported
publication describes
probable onset
gaining attention
chameleonic behavior
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