Assay Detail
Binding
CHEMBL2168485
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NaV1.7 F1737A mutant expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 4.72 | 5.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2164389 | — | — | 1 | 5.00 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 1 | 4.92 |
| CHEMBL698 | TETRACAINE | 4.0 | 1 | 4.48 |
| CHEMBL2164044 | — | — | 1 | 4.48 |
| CHEMBL2164042 | — | — | 1 | - |
| CHEMBL2164373 | — | — | 1 | - |
| CHEMBL2164371 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2164389 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL698 | TETRACAINE | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL2164044 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL2164042 | — | IC50 | - | — | - | |
| CHEMBL2164373 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2164371 | — | IC50 | > | 33000.0 | nM | - |