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Assay Detail

CHEMBL5130123

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

Binding
Activation of Kv7.2/Kv7.3 channel (unknown origin) expressed in CHO cells assessed as slope of fluorescent signal by FluxOR fluorescent dye based 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 7 — Homologous single protein target
Curated By Autocuration

Publication

Beyond Retigabine: Design, Synthesis, and Pharmacological Characterization of a Potent and Chemically Stable Neuronal Kv7 Channel Activator with Anticonvulsant Activity.
Musella S, Carotenuto L, Iraci N, Baroli G, Ciaglia T, Nappi P, Basilicata MG, Salviati E, Barrese V, Vestuto V, Pignataro G, Pepe G, Sommella E, Di Sarno V, Manfra M, Campiglia P, Gomez-Monterrey I, Bertamino A, Taglialatela M, Ostacolo C, Miceli F.
J Med Chem (2022) 65 : 11340 -11364
PubMed 35972998 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 5.28 5.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5204124 1 5.50
CHEMBL4438095 1 5.40
CHEMBL41355 EZOGABINE 4.0 1 4.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5204124 EC50 = 3200.0 nM 5.50
CHEMBL4438095 EC50 = 4000.0 nM 5.40
CHEMBL41355 EZOGABINE EC50 = 11200.0 nM 4.95