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Assay Detail

CHEMBL3889199

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Binding
Electrophysiological Assay: Sodium currents were measured using the patch clamp technique in the whole-cell configuration using either a PatchXpress automated voltage clamp or manually using an Axopatch 200B (Axon Instruments) or Model 2400 (A-M systems) amplifier. The manual voltage clamp protocol was as follows: Borosilicate glass micropipettes were fire-polished to a tip diameter yielding a resistance of 2-4 Mohms in the working solutions. The pipette was filled with a solution comprised of 5 mM NaCl, 10 mM CsCl, 120 mM CsF, 0.1 mM CaCl2, 2 mM MgCl2, 10 mM HEPES, 10 mM EGTA; and adjusted to pH 7.2 with CsOH. The external solution had the following composition: 140 mM NaCl, 5 mM KCl, 2 mM CaCl2, 1 mM MgCl2, 10 mM HEPES; and adjusted to pH 7.4 with NaOH. In some studies, the external sodium was reduced by equimolar replacement with choline.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Substituted benzoxazoles and methods of use thereof
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.05 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3985190 1 6.00
CHEMBL3892900 1 5.70
CHEMBL3952472 1 5.52
CHEMBL3893022 1 5.25
CHEMBL3925668 1 5.00
CHEMBL3924410 1 4.89
CHEMBL3963354 1 4.85
CHEMBL3922136 1 4.13
CHEMBL3897960 1 4.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3985190 IC50 = 1000.0 nM 6.00
CHEMBL3892900 IC50 = 2000.0 nM 5.70
CHEMBL3952472 IC50 = 3000.0 nM 5.52
CHEMBL3893022 IC50 = 5600.0 nM 5.25
CHEMBL3925668 IC50 = 10000.0 nM 5.00
CHEMBL3924410 IC50 = 13000.0 nM 4.89
CHEMBL3963354 IC50 = 14000.0 nM 4.85
CHEMBL3922136 IC50 = 74000.0 nM 4.13
CHEMBL3897960 IC50 = 86000.0 nM 4.07