Assay Detail
Functional
CHEMBL780602
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of Calcium flux into brain synaptosomes (Values are means of at least three separate determinations)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Design, synthesis, and pharmacological evaluation of conformationally constrained analogues of N,N'-diaryl- and N-aryl-N-aralkylguanidines as potent inhibitors of neuronal Na+ channels.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.91 | 6.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL543868 | — | — | 1 | 6.41 |
| CHEMBL544098 | — | — | 1 | 6.05 |
| CHEMBL545504 | — | — | 1 | 5.60 |
| CHEMBL28853 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL543868 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL544098 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL545504 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL28853 | — | IC50 | = | 2700.0 | nM | 5.57 |