Assay Detail
Binding
CHEMBL960265
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Displacement of [3H]ryanodine from RyR1 calcium channel in sarcoplasmic reticulum assessed as calcium mobilization
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Cationic reduction of bastadin-4 to bastadin-5. Preparation of 5-[2h]-bastadin-5 by site-specific isotopic labeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 5.22 | 5.58 |
| ED50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL505907 | — | — | 1 | 5.58 |
| CHEMBL504851 | — | — | 1 | 5.24 |
| CHEMBL455487 | BASTADIN 4 | — | 1 | 4.83 |
| CHEMBL439151 | BASTADIN 5 | — | 1 | - |
| CHEMBL508830 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL505907 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL504851 | — | EC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL455487 | BASTADIN 4 | EC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL439151 | BASTADIN 5 | ED50 | = | 2.3 | uM | - |
| CHEMBL508830 | — | EC50 | > | 100000.0 | nM | - |