retigabine
Ligand Summary
In vitro studies indicate that ezogabine enhances transmembrane potassium currents mediated by the KCNQ (Kv7.2 to 7.5) family of ion channels. By activating KCNQ channels, ezogabine is thought to stabilize the resting membrane potential and reduce brain excitability.
UNII: 12G01I6BBU
PubChem: 121892
Guide to Pharmacology: 2601
ChEMBL: CHEMBL41355
DrugCentral: 4181
LyCHI: FRQZ6WHCCCQN
Target Activities
KCNQ2
Potassium voltage-gated channel subfamily KQT member 2
5 Activities
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1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
EC50 | 5.6 | |||||
EC50 | 6.46 | Bioorg Med Chem Lett, (2018) 28:10:1731 | ||||
EC50 | 6.46 | Bioorg Med Chem Lett, (2018) 28:17:3004 | ||||
EC50 | 6.03 | J Med Chem, (2020) 63:1:163 | ||||
EC50 | 5.6 | ACTIVATOR | ||||
KCNQ4
Potassium voltage-gated channel subfamily KQT member 4
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
EC50 | 5.2 | |||||
EC50 | 5.7 | J Med Chem, (2020) 63:1:163 | ||||
EC50 | 5.23 | ACS Med Chem Lett, (2019) 10:1:27 | ||||
EC50 | 5.2 | ACTIVATOR | ||||
KCNQ5
Potassium voltage-gated channel subfamily KQT member 5
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
EC50 | 5 | |||||
EC50 | 6.1 | J Med Chem, (2020) 63:1:163 | ||||
EC50 | 5.46 | ACS Med Chem Lett, (2019) 10:1:27 | ||||
EC50 | 5 | ACTIVATOR | ||||
KCNQ3
Potassium voltage-gated channel subfamily KQT member 3
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
EC50 | 6.2 | |||||
EC50 | 5.41 | J Med Chem, (2020) 63:1:163 | ||||
EC50 | 6.2 | ACTIVATOR | ||||