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Assay Detail

CHEMBL5363712

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

Binding
Inhibition of human Nav 1.4 expressed in HEK293T cells assessed as phasic block at 10 Hz 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 HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium channel protein type 4 subunit alpha (CHEMBL2072)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Riluzole Analogs with Improved Use-Dependent Inhibition of Skeletal Muscle Sodium Channels.
Farinato A, Cavalluzzi MM, Altamura C, Campanale C, Laghetti P, Saltarella I, Delre P, Barbault A, Tarantino N, Milani G, Rotondo NP, Di Cesare Mannelli L, Ghelardini C, Pierno S, Mangiatordi GF, Lentini G, Desaphy JF.
ACS Med Chem Lett (2023) 14 : 999 -1008
PubMed 37465302 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.25 4.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5394673 1 4.42
CHEMBL744 RILUZOLE 4.0 1 4.29
CHEMBL442384 1 4.28
CHEMBL5434746 1 4.20
CHEMBL97407 1 4.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5394673 IC50 = 38000.0 nM 4.42
CHEMBL744 RILUZOLE IC50 = 51000.0 nM 4.29
CHEMBL442384 IC50 = 53000.0 nM 4.28
CHEMBL5434746 IC50 = 63000.0 nM 4.20
CHEMBL97407 IC50 = 89000.0 nM 4.05