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Assay Detail

CHEMBL4403830

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Activation of human Kv7.3 expressed in CHO cells assessed as increase in channel current amplitude by whole cell patch clamp electrophysiology assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Potassium voltage-gated channel subfamily KQT member 3 (CHEMBL2684)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Pharmacological Characterization of Conformationally Restricted Retigabine Analogues as Novel Neuronal Kv7 Channel Activators.
Ostacolo C, Miceli F, Di Sarno V, Nappi P, Iraci N, Soldovieri MV, Ciaglia T, Ambrosino P, Vestuto V, Lauritano A, Musella S, Pepe G, Basilicata MG, Manfra M, Perinelli DR, Novellino E, Bertamino A, Gomez-Monterrey IM, Campiglia P, Taglialatela M.
J Med Chem (2020) 63 : 163 -185
PubMed 31815462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 5.48 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4457044 1 6.04
CHEMBL41355 EZOGABINE 4.0 1 5.41
CHEMBL4545892 1 4.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4457044 EC50 = 920.0 nM 6.04
CHEMBL41355 EZOGABINE EC50 = 3900.0 nM 5.41
CHEMBL4545892 EC50 = 10500.0 nM 4.98