Assay Detail
Binding
CHEMBL3887977
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Assay: The assay is based on the guanidine influx assay described by Reddy, N. L., et al., J. Med. Chem. (1998), 41(17):3298-302. The guanidine influx assay is a radiotracer flux assay used to determine ion flux activity of voltage-gated sodium channels in a high-throughput microplate-based format. The assay uses 14C-guanidine hydrochloride in combination with various known voltage-gated sodium channel modulators that produce maintained influx, to assay the potency of test agents.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 9 subunit alpha (CHEMBL4296) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthetic methods for spiro-oxindole compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.63 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3707218 | FUNAPIDE | 2.0 | 1 | 8.52 |
| CHEMBL3927599 | — | — | 1 | 8.30 |
| CHEMBL3968430 | — | — | 1 | 8.15 |
| CHEMBL3966364 | — | — | 1 | 7.82 |
| CHEMBL3907255 | — | — | 1 | 5.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3707218 | FUNAPIDE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3927599 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3968430 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3966364 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3907255 | — | IC50 | = | 4200.0 | nM | 5.38 |