Assay Detail
Binding
CHEMBL5377103
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Modulator activity at wild type RyR2 (unknown origin) expressed in HEK293T co-expressed with R-CEPIA1er assessed as decrease in RyR2-mediated calcium leak in presence of calcium chloride by time-lapse fluorescence analysis
10
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1,4-Benzothiazepines with Cyclopropanol Groups and Their Structural Analogues Exhibit Both RyR2-Stabilizing and SERCA2a-Stimulating Activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 6.69 | 7.99 |
| Activity | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5413930 | — | — | 1 | 7.99 |
| CHEMBL5409619 | — | — | 1 | 7.73 |
| CHEMBL5398491 | — | — | 1 | 7.09 |
| CHEMBL5435124 | — | — | 1 | 5.57 |
| CHEMBL5437537 | — | — | 1 | 5.09 |
| CHEMBL2104951 | ALADORIAN | 2.0 | 1 | - |
| CHEMBL2440854 | — | — | 1 | - |
| CHEMBL4594418 | SURLORIAN | 2.0 | 1 | - |
| CHEMBL5409315 | — | — | 1 | - |
| CHEMBL5426069 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5413930 | — | EC50 | = | 10.2 | nM | 7.99 |
| CHEMBL5409619 | — | EC50 | = | 18.6 | nM | 7.73 |
| CHEMBL5398491 | — | EC50 | = | 81.5 | nM | 7.09 |
| CHEMBL5435124 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL5437537 | — | EC50 | = | 8170.0 | nM | 5.09 |
| CHEMBL2104951 | ALADORIAN | Activity | - | — | - | |
| CHEMBL2440854 | — | Activity | - | — | - | |
| CHEMBL4594418 | SURLORIAN | Activity | - | — | - | |
| CHEMBL5409315 | — | Activity | - | — | - | |
| CHEMBL5426069 | — | EC50 | > | 23000.0 | nM | - |