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Assay Detail

CHEMBL4415917

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

Functional
Anticonvulsant activity in po dosed CF-1 mouse model of maximal electroshock-induced seizure assessed as plasma level causing 50% reduction in hind limb extension pretreated for 2 hrs followed by electrical stimulation and measured for 5 mins
1
Total Activities
1
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 1 6.51 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4471825 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4471825 EC50 = 310.0 nM 6.51