Assay Detail
Binding
CHEMBL3889237
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Electrophysiological Assay (In vitro 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 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_00297
37
Total Activities
37
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
Biaryl ether sulfonamides and their use as therapeutic agents
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 8.21 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3955386 | — | — | 1 | 9.70 |
| CHEMBL3965272 | — | — | 1 | 9.52 |
| CHEMBL3617063 | — | — | 1 | 9.52 |
| CHEMBL3806065 | — | — | 1 | 9.30 |
| CHEMBL3957974 | — | — | 1 | 9.30 |
| CHEMBL3341983 | — | — | 1 | 9.22 |
| CHEMBL3910564 | — | — | 1 | 9.15 |
| CHEMBL3925113 | — | — | 1 | 9.10 |
| CHEMBL3906826 | — | — | 1 | 9.00 |
| CHEMBL3963109 | — | — | 1 | 9.00 |
| CHEMBL3907762 | — | — | 1 | 8.92 |
| CHEMBL3928901 | — | — | 1 | 8.85 |
| CHEMBL3912540 | — | — | 1 | 8.85 |
| CHEMBL3805973 | — | — | 1 | 8.77 |
| CHEMBL3805722 | — | — | 1 | 8.77 |
| CHEMBL3805837 | — | — | 1 | 8.77 |
| CHEMBL3950598 | — | — | 1 | 8.74 |
| CHEMBL3805201 | — | — | 1 | 8.52 |
| CHEMBL3969795 | — | — | 1 | 8.46 |
| CHEMBL3805347 | — | — | 1 | 8.44 |
| CHEMBL3804898 | — | — | 1 | 8.36 |
| CHEMBL3805897 | — | — | 1 | 8.28 |
| CHEMBL3952736 | — | — | 1 | 8.13 |
| CHEMBL3978280 | — | — | 1 | 8.10 |
| CHEMBL3805563 | — | — | 1 | 8.06 |
| CHEMBL3934922 | — | — | 1 | 7.97 |
| CHEMBL3805265 | — | — | 1 | 7.87 |
| CHEMBL3958847 | — | — | 1 | 7.76 |
| CHEMBL3949421 | — | — | 1 | 7.75 |
| CHEMBL3955084 | — | — | 1 | 7.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3955386 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3965272 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3617063 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3806065 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3957974 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3341983 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3910564 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3925113 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3906826 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3963109 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3907762 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3928901 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3912540 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3805837 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3805722 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3805973 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3950598 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3805201 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3969795 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3805347 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3804898 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3805897 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3952736 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL3978280 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3805563 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL3934922 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL3805265 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL3958847 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL3949421 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL3955084 | — | IC50 | = | 23.2 | nM | 7.63 |
| CHEMBL3805138 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3966575 | — | IC50 | = | 67.8 | nM | 7.17 |
| CHEMBL3805199 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL3963256 | — | IC50 | = | 674.6 | nM | 6.17 |
| CHEMBL3805875 | — | IC50 | = | 2308.8 | nM | 5.64 |
| CHEMBL3983385 | — | IC50 | = | 2375.6 | nM | 5.62 |
| CHEMBL3893190 | — | IC50 | = | 3378.2 | nM | 5.47 |