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Assay Detail

CHEMBL4415908

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

Functional
Anticonvulsant activity in po dosed SCN8A N1768D mutant harboring C57BL/6J/C3HeB/FeJ mouse model of 6Hz electroshock-induced seizure assessed as plasma concentration causing 50% reduction in seizure frequency pretreated for 2 hrs followed by 6 Hz electrical stimulation
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 1 — Organism
Curated By Autocuration

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

Publication

Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective Na<sub>V</sub>1.6 Inhibitors with Efficacy in Mouse Models of Epilepsy.
Focken T, Burford K, Grimwood ME, Zenova A, Andrez JC, Gong W, Wilson M, Taron M, Decker S, Lofstrand V, Chowdhury S, Shuart N, Lin S, Goodchild SJ, Young C, Soriano M, Tari PK, Waldbrook M, Nelkenbrecher K, Kwan R, Lindgren A, de Boer G, Lee S, Sojo L, DeVita RJ, Cohen CJ, Wesolowski SS, Johnson JP, Dehnhardt CM, Empfield JR.
J Med Chem (2019) 62 : 9618 -9641
PubMed 31525968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.56 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4435054 1 7.22
CHEMBL4471825 1 6.33
CHEMBL4460028 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4435054 EC50 = 60.0 nM 7.22
CHEMBL4471825 EC50 = 470.0 nM 6.33
CHEMBL4460028 EC50 = 720.0 nM 6.14