Assay Detail
Binding
CHEMBL5377104
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of SERCA2a in mouse HL-1 cells assessed as increase in caffeine-induced calcium release incubated for 2 hrs by FLIPR Calcium 6 dye based caffeine assay
11
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HL-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sarcoplasmic/endoplasmic reticulum calcium ATPase 2 (CHEMBL4523144) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 8 | 5.16 | 5.82 |
| Activity | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5426069 | — | — | 1 | 5.82 |
| CHEMBL5437537 | — | — | 1 | 5.66 |
| CHEMBL5413930 | — | — | 1 | 5.12 |
| CHEMBL5398491 | — | — | 1 | 5.07 |
| CHEMBL5435124 | — | — | 1 | 5.04 |
| CHEMBL5409619 | — | — | 1 | 4.96 |
| CHEMBL4594418 | SURLORIAN | 2.0 | 2 | 4.46 |
| CHEMBL2104951 | ALADORIAN | 2.0 | 1 | - |
| CHEMBL2440854 | — | — | 1 | - |
| CHEMBL5409315 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5426069 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL5437537 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5413930 | — | EC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL5398491 | — | EC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL5435124 | — | EC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL5409619 | — | EC50 | = | 10900.0 | nM | 4.96 |
| CHEMBL4594418 | SURLORIAN | EC50 | = | 34300.0 | nM | 4.46 |
| CHEMBL4594418 | SURLORIAN | Activity | - | — | - | |
| CHEMBL2104951 | ALADORIAN | Activity | - | — | - | |
| CHEMBL2440854 | — | Activity | - | — | - | |
| CHEMBL5409315 | — | EC50 | > | 1000000.0 | nM | - |