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Assay Detail

CHEMBL3583448

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

Binding
Inhibition of Nav1.7 (unknown origin) by electrophysiological assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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
Ki 7 5.83 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3581056 1 6.36
CHEMBL3581058 1 6.25
CHEMBL3581050 1 6.19
CHEMBL3581059 1 6.04
CHEMBL3581054 1 5.99
CHEMBL3581053 1 5.52
CHEMBL108 CARBAMAZEPINE 4.0 1 4.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3581056 Ki = 440.0 nM 6.36
CHEMBL3581058 Ki = 560.0 nM 6.25
CHEMBL3581050 Ki = 650.0 nM 6.19
CHEMBL3581059 Ki = 920.0 nM 6.04
CHEMBL3581054 Ki = 1030.0 nM 5.99
CHEMBL3581053 Ki = 3030.0 nM 5.52
CHEMBL108 CARBAMAZEPINE Ki = 32700.0 nM 4.49