Assay Detail
Functional
CHEMBL806326
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Sodium channel block, determined by % block of [14C]guanidinium flux in CHO line expressing rat type IIA sodium channels derived from rat brain
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium channel protein type 2 subunit alpha (CHEMBL3399) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.05 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL112806 | — | — | 1 | 6.96 |
| CHEMBL109210 | — | — | 1 | 6.89 |
| CHEMBL112132 | — | — | 1 | 6.85 |
| CHEMBL326502 | — | — | 1 | 6.72 |
| CHEMBL112515 | — | — | 1 | 6.37 |
| CHEMBL81626 | — | — | 1 | 6.34 |
| CHEMBL326774 | — | — | 1 | 6.17 |
| CHEMBL110909 | — | — | 1 | 6.10 |
| CHEMBL331126 | — | — | 1 | 6.08 |
| CHEMBL326741 | — | — | 1 | 6.08 |
| CHEMBL326130 | — | — | 1 | 6.07 |
| CHEMBL78083 | — | — | 1 | 5.86 |
| CHEMBL320340 | — | — | 1 | 5.81 |
| CHEMBL28853 | — | — | 1 | 5.79 |
| CHEMBL325215 | — | — | 1 | 5.75 |
| CHEMBL28854 | SIPATRIGINE | 2.0 | 1 | 5.59 |
| CHEMBL744 | RILUZOLE | 4.0 | 1 | 5.33 |
| CHEMBL114716 | — | — | 1 | 5.09 |
| CHEMBL81602 | — | — | 1 | 5.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL112806 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL109210 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL112132 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL326502 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL112515 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL81626 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL326774 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL110909 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL331126 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL326741 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL326130 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL78083 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL320340 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL28853 | — | IC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL325215 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL28854 | SIPATRIGINE | IC50 | = | 2550.0 | nM | 5.59 |
| CHEMBL744 | RILUZOLE | IC50 | = | 4730.0 | nM | 5.33 |
| CHEMBL114716 | — | IC50 | = | 8190.0 | nM | 5.09 |
| CHEMBL81602 | — | IC50 | = | 9210.0 | nM | 5.04 |