Assay Detail
Binding
CHEMBL3887284
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Electrophysiology Assay: Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons were isolated from the dorsal root ganglions and maintained in culture for 2 to 10 days in the presence of NGF (50 ng/ml) (culture media consisted of NeurobasalA supplemented with B27, glutamine and antibiotics). Small diameter neurons (nociceptors, 8-12 um in diameter) were visually identified and probed with fine tip glass electrodes connected to an amplifier (Axon Instruments). The "voltage clamp" mode was used to assess the compound's IC50 holding the cells at -60 mV. In addition, the "current clamp" mode was employed to test the efficacy of the compounds in blocking action potential generation in response to current injections.
80
Total Activities
80
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 10 subunit alpha (CHEMBL4017) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Substituted quinoxalines as sodium channel modulators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 80 | 7.21 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3973953 | — | — | 1 | 9.00 |
| CHEMBL3915190 | — | — | 1 | 8.70 |
| CHEMBL3946608 | — | — | 1 | 8.52 |
| CHEMBL3937776 | — | — | 1 | 8.40 |
| CHEMBL3945576 | — | — | 1 | 8.30 |
| CHEMBL3941645 | — | — | 1 | 8.22 |
| CHEMBL3951908 | — | — | 1 | 8.22 |
| CHEMBL3969972 | — | — | 1 | 8.15 |
| CHEMBL3943899 | — | — | 1 | 8.15 |
| CHEMBL3964266 | — | — | 1 | 8.10 |
| CHEMBL3964079 | — | — | 1 | 7.96 |
| CHEMBL3943157 | — | — | 1 | 7.96 |
| CHEMBL3914004 | — | — | 1 | 7.89 |
| CHEMBL3915196 | — | — | 1 | 7.89 |
| CHEMBL3959428 | — | — | 1 | 7.85 |
| CHEMBL3909843 | — | — | 1 | 7.85 |
| CHEMBL3936668 | — | — | 1 | 7.85 |
| CHEMBL3931931 | — | — | 1 | 7.82 |
| CHEMBL3939244 | — | — | 1 | 7.82 |
| CHEMBL3907141 | — | — | 1 | 7.80 |
| CHEMBL3954662 | — | — | 1 | 7.77 |
| CHEMBL3939539 | — | — | 1 | 7.72 |
| CHEMBL3965344 | — | — | 1 | 7.72 |
| CHEMBL3889926 | — | — | 1 | 7.66 |
| CHEMBL3946211 | — | — | 1 | 7.66 |
| CHEMBL3974970 | — | — | 1 | 7.66 |
| CHEMBL3973225 | — | — | 1 | 7.62 |
| CHEMBL3928399 | — | — | 1 | 7.58 |
| CHEMBL3971232 | — | — | 1 | 7.57 |
| CHEMBL3912507 | — | — | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3973953 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3915190 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3946608 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3937776 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3945576 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3941645 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3951908 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3969972 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3943899 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3964266 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3964079 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3943157 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3915196 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3914004 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3936668 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3959428 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3909843 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3931931 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3939244 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3907141 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3954662 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3939539 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3965344 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3974970 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3889926 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3946211 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3973225 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3928399 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3971232 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3912507 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3983371 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3943712 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3965855 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3929599 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3960604 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3958675 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3924193 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3953683 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3956547 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3892827 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3944297 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3961839 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3938496 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3919212 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3935327 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3954231 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3949386 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3920688 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3962886 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3912126 | — | IC50 | = | 86.0 | nM | 7.07 |