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Assay Detail

CHEMBL4415876

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

Binding
Inhibition of human ERG expressed in HEK293 cells by IonWorks barracuda patch clamp method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

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 3 4.62 4.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4460028 1 4.65
CHEMBL4471825 1 4.58
CHEMBL4435054 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4460028 IC50 = 22200.0 nM 4.65
CHEMBL4471825 IC50 = 26300.0 nM 4.58
CHEMBL4435054 IC50 > 30000.0 nM -