Assay Detail
Binding
CHEMBL3405047
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Inhibition of Orai channel in phytohemagglutinin-stimulated human Jurkat E6-1 cells assessed as NFAT-induced transcription measured as IL-2 level after 20 hrs by ELISA
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Jurkat |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 23 | 6.99 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3403742 | — | — | 1 | 8.00 |
| CHEMBL262766 | — | — | 1 | 8.00 |
| CHEMBL3403744 | — | — | 1 | 7.64 |
| CHEMBL3403751 | — | — | 1 | 7.40 |
| CHEMBL3403763 | — | — | 1 | 7.25 |
| CHEMBL3403753 | — | — | 1 | 7.17 |
| CHEMBL3403745 | — | — | 1 | 7.14 |
| CHEMBL3403762 | — | — | 1 | 6.93 |
| CHEMBL3403750 | — | — | 1 | 6.92 |
| CHEMBL3403758 | — | — | 1 | 6.92 |
| CHEMBL3403752 | — | — | 1 | 6.82 |
| CHEMBL3403757 | — | — | 1 | 6.75 |
| CHEMBL3403746 | — | — | 1 | 6.74 |
| CHEMBL3403743 | — | — | 1 | 6.58 |
| CHEMBL3403747 | — | — | 1 | 6.57 |
| CHEMBL3403760 | — | — | 1 | 6.54 |
| CHEMBL3403749 | — | — | 1 | 5.52 |
| CHEMBL3403755 | — | — | 1 | - |
| CHEMBL3403754 | — | — | 1 | - |
| CHEMBL3403756 | — | — | 1 | - |
| CHEMBL3403748 | — | — | 1 | - |
| CHEMBL3403759 | — | — | 1 | - |
| CHEMBL3403761 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3403742 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL262766 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3403744 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3403751 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3403763 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3403753 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3403745 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3403762 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL3403750 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3403758 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL3403752 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3403757 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3403746 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL3403743 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3403747 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3403760 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3403749 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3403755 | — | IC50 | - | — | - | |
| CHEMBL3403754 | — | IC50 | - | — | - | |
| CHEMBL3403756 | — | IC50 | - | — | - | |
| CHEMBL3403748 | — | IC50 | - | — | - | |
| CHEMBL3403759 | — | IC50 | - | — | - | |
| CHEMBL3403761 | — | IC50 | - | — | - |