Assay Detail
Binding
CHEMBL4056898
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Inhibition of slow inactivated human NaV1.7 expressed in HEK293 cells at -20 mV holding potential after 5 mins by IonWorks electrophysiology method
27
Total Activities
27
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
Discovery of a biarylamide series of potent, state-dependent NaV1.7 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.06 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3979498 | — | — | 1 | 8.30 |
| CHEMBL4079509 | — | — | 1 | 8.15 |
| CHEMBL4100413 | — | — | 1 | 7.96 |
| CHEMBL4085326 | — | — | 1 | 7.80 |
| CHEMBL4077551 | — | — | 1 | 7.80 |
| CHEMBL4076874 | — | — | 1 | 7.75 |
| CHEMBL4076051 | — | — | 1 | 7.70 |
| CHEMBL4062344 | — | — | 1 | 7.64 |
| CHEMBL1480490 | — | — | 1 | 7.51 |
| CHEMBL4098932 | — | — | 1 | 7.42 |
| CHEMBL4064479 | — | — | 1 | 7.37 |
| CHEMBL4099561 | — | — | 1 | 7.37 |
| CHEMBL4063274 | — | — | 1 | 7.32 |
| CHEMBL4100514 | — | — | 1 | 7.27 |
| CHEMBL4084926 | — | — | 1 | 7.21 |
| CHEMBL4076380 | — | — | 1 | 7.18 |
| CHEMBL4082401 | — | — | 1 | 6.82 |
| CHEMBL4071906 | — | — | 1 | 6.82 |
| CHEMBL4092683 | — | — | 1 | 6.31 |
| CHEMBL4080898 | — | — | 1 | 6.29 |
| CHEMBL4081556 | — | — | 1 | 6.11 |
| CHEMBL4073701 | — | — | 1 | 5.77 |
| CHEMBL4084060 | — | — | 1 | 5.77 |
| CHEMBL4086749 | — | — | 1 | 5.41 |
| CHEMBL4075358 | — | — | 1 | 5.37 |
| CHEMBL4069695 | — | — | 1 | - |
| CHEMBL4075864 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3979498 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4079509 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4100413 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4085326 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4077551 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4076874 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4076051 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4062344 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1480490 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4098932 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4064479 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4099561 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4063274 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4100514 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4084926 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4076380 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4082401 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4071906 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4092683 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4080898 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4081556 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4073701 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4084060 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4086749 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4075358 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4069695 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4075864 | — | IC50 | > | 25000.0 | nM | - |