Assay Detail
ADMET
CHEMBL4056897
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Inhibition of human NaV1.5 expressed in HEK293 cells at -50 mV holding potential after 3 to 5 mins by PatchXpress automated electrophysiology method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 5 subunit alpha (CHEMBL1980) ↗| 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 | 17 | 6.02 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4079509 | — | — | 1 | 7.75 |
| CHEMBL4100413 | — | — | 1 | 6.66 |
| CHEMBL4076874 | — | — | 1 | 6.40 |
| CHEMBL4077551 | — | — | 1 | 6.37 |
| CHEMBL4063274 | — | — | 1 | 6.32 |
| CHEMBL4076051 | — | — | 1 | 6.28 |
| CHEMBL4085326 | — | — | 1 | 6.18 |
| CHEMBL4076380 | — | — | 1 | 6.09 |
| CHEMBL1480490 | — | — | 1 | 6.01 |
| CHEMBL4100514 | — | — | 1 | 5.96 |
| CHEMBL4064479 | — | — | 1 | 5.92 |
| CHEMBL4084926 | — | — | 1 | 5.72 |
| CHEMBL4098932 | — | — | 1 | 5.62 |
| CHEMBL4082401 | — | — | 1 | 5.57 |
| CHEMBL4071906 | — | — | 1 | 5.41 |
| CHEMBL4080898 | — | — | 1 | 5.17 |
| CHEMBL4092683 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4079509 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4100413 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4076874 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4077551 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4063274 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4076051 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4085326 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4076380 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL1480490 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4100514 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4064479 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4084926 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4098932 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4082401 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4071906 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4080898 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL4092683 | — | IC50 | = | 13000.0 | nM | 4.89 |