Assay Detail
Binding
CHEMBL5732258
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Electrophysiological Assay : 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 α-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. Nav1.7 and Nav1.5 cDNAs (NM_002977 and AC137587; SCN5A, respectively) were stably expressed in HEK-293 cells. The β1 subunit was coexpressed only in the Nav1.7 cell line.
288
Total Activities
57
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Benzenesulfonamide compounds and their use as therapeutic agents
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 96 | 6.85 | 9.10 |
| kon | 96 | - | - |
| k_off | 96 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5781390 | — | — | 6 | 9.10 |
| CHEMBL5897347 | — | — | 6 | 9.05 |
| CHEMBL3325526 | — | — | 6 | 8.96 |
| CHEMBL6011175 | — | — | 6 | 8.59 |
| CHEMBL5982736 | — | — | 12 | 8.48 |
| CHEMBL5766935 | — | — | 6 | 8.48 |
| CHEMBL3325537 | — | — | 6 | 8.32 |
| CHEMBL5803464 | — | — | 6 | 8.17 |
| CHEMBL6028339 | — | — | 6 | 8.07 |
| CHEMBL5807668 | — | — | 6 | 7.92 |
| CHEMBL5797625 | — | — | 6 | 7.67 |
| CHEMBL6051990 | — | — | 6 | 7.64 |
| CHEMBL5847974 | — | — | 6 | 7.50 |
| CHEMBL5934221 | — | — | 6 | 7.48 |
| CHEMBL5833824 | — | — | 6 | 7.42 |
| CHEMBL5943670 | — | — | 6 | 7.42 |
| CHEMBL5945564 | — | — | 6 | 7.30 |
| CHEMBL3325530 | — | — | 6 | 7.29 |
| CHEMBL5859656 | — | — | 6 | 7.27 |
| CHEMBL5872027 | — | — | 6 | 7.15 |
| CHEMBL5804891 | — | — | 6 | 7.12 |
| CHEMBL5908065 | — | — | 6 | 7.09 |
| CHEMBL5967832 | — | — | 6 | 7.07 |
| CHEMBL5742819 | — | — | 6 | 7.03 |
| CHEMBL5876192 | — | — | 6 | 6.94 |
| CHEMBL5853880 | — | — | 6 | 6.89 |
| CHEMBL5962861 | — | — | 3 | 6.88 |
| CHEMBL5801875 | — | — | 6 | 6.79 |
| CHEMBL5989696 | — | — | 6 | 6.77 |
| CHEMBL5760755 | — | — | 3 | 6.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5781390 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5897347 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3325526 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL6011175 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5982736 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5766935 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3325537 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL5803464 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL6028339 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL5807668 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5797625 | — | IC50 | = | 21.6 | nM | 7.67 |
| CHEMBL6051990 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5847974 | — | IC50 | = | 31.7 | nM | 7.50 |
| CHEMBL5934221 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5833824 | — | IC50 | = | 38.1 | nM | 7.42 |
| CHEMBL5943670 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5945564 | — | IC50 | = | 49.9 | nM | 7.30 |
| CHEMBL3325530 | — | IC50 | = | 50.7 | nM | 7.29 |
| CHEMBL5859656 | — | IC50 | = | 53.2 | nM | 7.27 |
| CHEMBL5982736 | — | IC50 | = | 58.8 | nM | 7.23 |
| CHEMBL5872027 | — | IC50 | = | 70.5 | nM | 7.15 |
| CHEMBL5943670 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5804891 | — | IC50 | = | 76.4 | nM | 7.12 |
| CHEMBL5908065 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL5967832 | — | IC50 | = | 84.4 | nM | 7.07 |
| CHEMBL5742819 | — | IC50 | = | 93.7 | nM | 7.03 |
| CHEMBL5876192 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL5853880 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5962861 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL5801875 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL5989696 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL5760755 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL6006694 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL5805300 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL5861673 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL5996787 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5765046 | — | IC50 | = | 326.0 | nM | 6.49 |
| CHEMBL5983136 | — | IC50 | = | 323.0 | nM | 6.49 |
| CHEMBL3325536 | — | IC50 | = | 331.0 | nM | 6.48 |
| CHEMBL5879530 | — | IC50 | = | 393.0 | nM | 6.41 |
| CHEMBL5804743 | — | IC50 | = | 426.0 | nM | 6.37 |
| CHEMBL5991925 | — | IC50 | = | 436.0 | nM | 6.36 |
| CHEMBL5801875 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5876192 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL6006694 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5996787 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5853880 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3325536 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5805300 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5989696 | — | IC50 | = | 550.0 | nM | 6.26 |