Assay Detail
Binding
CHEMBL3707743
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Electrophysiological Assay: Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and allows the determination of the time- and voltage-dependence of block which has been interpreted as differential binding to the resting, open, and inactivated states of the sodium channel (Hille, B., Journal of General Physiology (1977), 69: 497-515).The following patch voltage clamp electrophysiology studies were performed on representative compounds of the invention using human embryonic kidney cells (HEK), permanently transfected with an expression vector containing the full-length cDNA coding for the desired human sodium channel alpha -subunit, grown in culture media containing 10% FBS, 1% PSG, and 0.5 mg/mL G418 at 37 C. with 5% CO2. HEK cells used for the electrophysiology (EP) recordings had a passage number of less than 40 for all studies and were used within three days from the time of plating.
228
Total Activities
210
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| 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
N-substituted benzamides and methods of use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 228 | 7.38 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3657851 | — | — | 1 | 9.52 |
| CHEMBL3657855 | — | — | 1 | 9.40 |
| CHEMBL3662236 | — | — | 1 | 9.00 |
| CHEMBL3662238 | — | — | 1 | 9.00 |
| CHEMBL3657877 | — | — | 1 | 8.88 |
| CHEMBL3657932 | — | — | 1 | 8.85 |
| CHEMBL3662094 | — | — | 3 | 8.70 |
| CHEMBL3662081 | — | — | 1 | 8.70 |
| CHEMBL3662177 | — | — | 1 | 8.70 |
| CHEMBL3662192 | — | — | 1 | 8.70 |
| CHEMBL3662093 | — | — | 1 | 8.70 |
| CHEMBL3657840 | — | — | 1 | 8.66 |
| CHEMBL3662122 | — | — | 2 | 8.52 |
| CHEMBL3662193 | — | — | 1 | 8.52 |
| CHEMBL3657854 | — | — | 1 | 8.52 |
| CHEMBL3658002 | — | — | 1 | 8.52 |
| CHEMBL3662205 | — | — | 1 | 8.52 |
| CHEMBL3662229 | — | — | 1 | 8.51 |
| CHEMBL3657846 | — | — | 1 | 8.51 |
| CHEMBL3657837 | — | — | 1 | 8.48 |
| CHEMBL3657929 | — | — | 2 | 8.44 |
| CHEMBL3654182 | — | — | 1 | 8.42 |
| CHEMBL3662190 | — | — | 1 | 8.40 |
| CHEMBL3662078 | — | — | 1 | 8.40 |
| CHEMBL3657967 | — | — | 1 | 8.40 |
| CHEMBL3657950 | — | — | 1 | 8.40 |
| CHEMBL3657934 | — | — | 1 | 8.37 |
| CHEMBL3657839 | — | — | 1 | 8.34 |
| CHEMBL3658000 | — | — | 1 | 8.30 |
| CHEMBL3658005 | — | — | 1 | 8.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3657851 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3657855 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3662238 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3662236 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3657877 | — | IC50 | = | 1.31 | nM | 8.88 |
| CHEMBL3657932 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3662192 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3662093 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3662177 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3662094 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3662081 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3662094 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3657840 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3662205 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3658002 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3657854 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3662193 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3662122 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3657846 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3662229 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3657837 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3657929 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3657929 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3654182 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3657967 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3657950 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3662190 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3662078 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3657934 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3657839 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3658005 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3658000 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3657805 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3341985 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3657954 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3662099 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3657954 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3657931 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL3657808 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4115551 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3657887 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL3657852 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL3657828 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL3662230 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL3658020 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3662072 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3657998 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3662090 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3657806 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL3657807 | — | IC50 | = | 8.7 | nM | 8.06 |