Assay Detail
Binding
CHEMBL3405048
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Orai1/STIM1 expressed in HEK293 cells assessed as inhibition of channel-mediated calcium current by electrophysiology assay in presence of 10 mM EGTA
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Calcium release-activated calcium channel protein 1 (CHEMBL2384891) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 7-azaindole derivatives as potent Orai inhibitors showing efficacy in a preclinical model of asthma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.67 | 6.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3403751 | — | — | 1 | 6.98 |
| CHEMBL3403753 | — | — | 1 | 6.36 |
| CHEMBL3403744 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3403751 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL3403753 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL3403744 | — | IC50 | < | 100.0 | nM | - |