Assay Detail
Binding
CHEMBL3889199
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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
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 |