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Assay Detail

CHEMBL4415864

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

Binding
Inhibition of recombinant human full length SCN1B/Nav1.6 N1768D mutant co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -60 mV holding potential by whole cell patch clamp assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
IC50 5 6.90 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4435054 1 7.08
CHEMBL4471825 1 6.91
CHEMBL4460028 1 6.72
CHEMBL4580996 1 -
CHEMBL4466858 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4435054 IC50 = 84.0 nM 7.08
CHEMBL4471825 IC50 = 122.0 nM 6.91
CHEMBL4460028 IC50 = 189.0 nM 6.72
CHEMBL4580996 IC50 - -
CHEMBL4466858 IC50 - -