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Assay Detail

CHEMBL3583449

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

Binding
Inhibition of Nav1.7 (unknown origin) expressed in CHO cells after 45 mins by FLIPR assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium channel protein type 9 subunit alpha (CHEMBL4296)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dibenzazepines and dibenzoxazepines as sodium channel blockers.
Lynch SM, Tafesse L, Carlin K, Ghatak P, Kyle DJ.
Bioorg Med Chem Lett (2014) 25 : 43 -47
PubMed 25466191 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.85 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3581056 1 6.43
CHEMBL3581051 1 6.08
CHEMBL3581058 1 5.99
CHEMBL3581059 1 5.98
CHEMBL3581054 1 5.97
CHEMBL3581057 1 5.75
CHEMBL3581050 1 5.71
CHEMBL3581055 1 5.59
CHEMBL3581053 1 5.12
CHEMBL3581052 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3581056 IC50 = 370.0 nM 6.43
CHEMBL3581051 IC50 = 840.0 nM 6.08
CHEMBL3581058 IC50 = 1030.0 nM 5.99
CHEMBL3581059 IC50 = 1050.0 nM 5.98
CHEMBL3581054 IC50 = 1080.0 nM 5.97
CHEMBL3581057 IC50 = 1800.0 nM 5.75
CHEMBL3581050 IC50 = 1960.0 nM 5.71
CHEMBL3581055 IC50 = 2570.0 nM 5.59
CHEMBL3581053 IC50 = 7620.0 nM 5.12
CHEMBL3581052 IC50 > 10000.0 nM -