Assay Detail
Binding
CHEMBL4009750
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human Nav1.7 expressed in HEK293 cells assessed as reduction in peak inward current at -60 mV holding potential measured after 600 secs by IonWorks Barracuda patch-clamp assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 9 subunit alpha (CHEMBL4296) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of New Benzenesulfonamides As Potent and Selective Nav1.7 Inhibitors for the Treatment of Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 7.22 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3325524 | — | — | 1 | 8.70 |
| CHEMBL4078268 | — | — | 1 | 8.22 |
| CHEMBL4094887 | — | — | 1 | 8.10 |
| CHEMBL4060154 | — | — | 1 | 8.10 |
| CHEMBL4076444 | — | — | 1 | 8.08 |
| CHEMBL4101437 | — | — | 1 | 8.05 |
| CHEMBL4098912 | — | — | 1 | 8.00 |
| CHEMBL4092078 | — | — | 1 | 7.96 |
| CHEMBL4078252 | — | — | 1 | 7.92 |
| CHEMBL4071098 | — | — | 1 | 7.85 |
| CHEMBL4080712 | — | — | 1 | 7.85 |
| CHEMBL4102633 | — | — | 1 | 7.82 |
| CHEMBL4088581 | — | — | 1 | 7.82 |
| CHEMBL4076627 | — | — | 1 | 7.80 |
| CHEMBL4064193 | — | — | 1 | 7.57 |
| CHEMBL4103940 | — | — | 1 | 7.54 |
| CHEMBL4096299 | — | — | 1 | 7.38 |
| CHEMBL4085278 | — | — | 1 | 7.31 |
| CHEMBL4062380 | — | — | 1 | 7.24 |
| CHEMBL4072007 | — | — | 1 | 7.19 |
| CHEMBL4089010 | — | — | 1 | 7.16 |
| CHEMBL4091922 | — | — | 1 | 7.16 |
| CHEMBL4093720 | — | — | 1 | 7.11 |
| CHEMBL4067455 | — | — | 1 | 7.11 |
| CHEMBL4063378 | — | — | 1 | 6.98 |
| CHEMBL4077266 | — | — | 1 | 6.79 |
| CHEMBL4096711 | — | — | 1 | 6.73 |
| CHEMBL4072107 | — | — | 1 | 6.68 |
| CHEMBL4067257 | — | — | 1 | 6.58 |
| CHEMBL4098339 | — | — | 1 | 6.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3325524 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4078268 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4060154 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4094887 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4076444 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4101437 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4098912 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4092078 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4078252 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4071098 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4080712 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4102633 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4088581 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4076627 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4064193 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4103940 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4096299 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4085278 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4062380 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4072007 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4091922 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4089010 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4093720 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4067455 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4063378 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL4077266 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL4096711 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL4072107 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL4067257 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL4098339 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL4071551 | — | IC50 | = | 339.0 | nM | 6.47 |
| CHEMBL4087898 | — | IC50 | = | 383.0 | nM | 6.42 |
| CHEMBL4065188 | — | IC50 | = | 388.0 | nM | 6.41 |
| CHEMBL4097237 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL4098978 | — | IC50 | = | 458.0 | nM | 6.34 |
| CHEMBL4062566 | — | IC50 | = | 473.0 | nM | 6.33 |
| CHEMBL4078527 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4091238 | — | IC50 | = | 963.0 | nM | 6.02 |
| CHEMBL4083450 | — | IC50 | = | 1820.0 | nM | 5.74 |