Assay Detail
Binding
CHEMBL2168491
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -90 mV holding potential by patch clamp electrophysiological assay
64
Total Activities
56
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
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 | 64 | 5.71 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2164389 | — | — | 3 | 7.10 |
| CHEMBL2164369 | — | — | 1 | 6.75 |
| CHEMBL2164390 | — | — | 1 | 6.66 |
| CHEMBL2164368 | — | — | 1 | 6.55 |
| CHEMBL2164356 | — | — | 1 | 6.43 |
| CHEMBL2164363 | — | — | 1 | 6.28 |
| CHEMBL698 | TETRACAINE | 4.0 | 1 | 6.21 |
| CHEMBL2164042 | — | — | 1 | 6.11 |
| CHEMBL2164387 | — | — | 1 | 6.09 |
| CHEMBL2164392 | — | — | 1 | 6.03 |
| CHEMBL2164373 | — | — | 3 | 6.00 |
| CHEMBL2164044 | — | — | 1 | 6.00 |
| CHEMBL2164393 | — | — | 1 | 5.85 |
| CHEMBL2164364 | — | — | 1 | 5.80 |
| CHEMBL2164039 | — | — | 1 | 5.77 |
| CHEMBL2164365 | — | — | 1 | 5.72 |
| CHEMBL2164370 | — | — | 1 | 5.70 |
| CHEMBL2164375 | — | — | 1 | 5.66 |
| CHEMBL2164374 | — | — | 1 | 5.66 |
| CHEMBL2164395 | — | — | 1 | 5.64 |
| CHEMBL2164383 | — | — | 1 | 5.64 |
| CHEMBL2163357 | — | — | 1 | 5.60 |
| CHEMBL2164371 | — | — | 3 | 5.42 |
| CHEMBL2164357 | — | — | 1 | 5.34 |
| CHEMBL2164361 | — | — | 1 | 5.24 |
| CHEMBL2164378 | — | — | 1 | 5.18 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 1 | 5.16 |
| CHEMBL2164376 | — | — | 1 | 5.07 |
| CHEMBL2164380 | — | — | 1 | 5.00 |
| CHEMBL2164381 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2164389 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2164369 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2164390 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2164368 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2164356 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL2164389 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL2164363 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL698 | TETRACAINE | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL2164042 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL2164387 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL2164392 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL2164044 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL2164373 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2164393 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2164364 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2164039 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2164365 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2164370 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2164375 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2164374 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2164395 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL2164383 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL2163357 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2164371 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL2164357 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL2164361 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL2164378 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL2164376 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL2164380 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2164381 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2164358 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL2164367 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL2164037 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2164372 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL2164396 | — | IC50 | - | — | - | |
| CHEMBL2164045 | — | IC50 | - | — | - | |
| CHEMBL2164384 | — | IC50 | - | — | - | |
| CHEMBL2164385 | — | IC50 | - | — | - | |
| CHEMBL2164386 | — | IC50 | - | — | - | |
| CHEMBL2164043 | — | IC50 | - | — | - | |
| CHEMBL2164367 | — | IC50 | - | — | - | |
| CHEMBL2164041 | — | IC50 | - | — | - | |
| CHEMBL2164040 | — | IC50 | - | — | - | |
| CHEMBL2164389 | — | IC50 | - | — | - | |
| CHEMBL2164038 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL2164391 | — | IC50 | - | — | - | |
| CHEMBL2164394 | — | IC50 | > | 10500.0 | nM | - |
| CHEMBL2164367 | — | IC50 | - | — | - | |
| CHEMBL2164388 | — | IC50 | - | — | - |