Assay Detail
Binding
CHEMBL3370897
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Agonist activity at glucocorticoid receptor in human A549 cells assessed as E-selectin transrepression by luciferase reporter gene assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 7.94 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3315066 | — | — | 1 | 9.22 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.96 |
| CHEMBL3315061 | — | — | 1 | 8.92 |
| CHEMBL3315064 | — | — | 1 | 8.85 |
| CHEMBL3315052 | — | — | 1 | 8.49 |
| CHEMBL3315051 | — | — | 1 | 8.44 |
| CHEMBL3315070 | — | — | 1 | 8.42 |
| CHEMBL3315063 | — | — | 1 | 8.32 |
| CHEMBL3315065 | — | — | 1 | 8.30 |
| CHEMBL3315049 | — | — | 1 | 8.16 |
| CHEMBL3315067 | — | — | 1 | 7.91 |
| CHEMBL3315069 | — | — | 1 | 7.83 |
| CHEMBL3315068 | — | — | 1 | 7.79 |
| CHEMBL3315057 | — | — | 1 | 7.79 |
| CHEMBL3315054 | — | — | 1 | 7.75 |
| CHEMBL3315059 | — | — | 1 | 7.48 |
| CHEMBL3315055 | — | — | 1 | 7.48 |
| CHEMBL1911270 | — | — | 1 | 7.47 |
| CHEMBL3315058 | — | — | 1 | 7.44 |
| CHEMBL3315053 | — | — | 1 | 7.13 |
| CHEMBL3315050 | — | — | 1 | 6.96 |
| CHEMBL3315060 | — | — | 1 | 6.83 |
| CHEMBL3315056 | — | — | 1 | 6.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3315066 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3315061 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3315064 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3315052 | — | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3315051 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3315070 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3315063 | — | EC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3315065 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3315049 | — | EC50 | = | 6.89 | nM | 8.16 |
| CHEMBL3315067 | — | EC50 | = | 12.2 | nM | 7.91 |
| CHEMBL3315069 | — | EC50 | = | 14.7 | nM | 7.83 |
| CHEMBL3315068 | — | EC50 | = | 16.3 | nM | 7.79 |
| CHEMBL3315057 | — | EC50 | = | 16.1 | nM | 7.79 |
| CHEMBL3315054 | — | EC50 | = | 17.6 | nM | 7.75 |
| CHEMBL3315059 | — | EC50 | = | 32.8 | nM | 7.48 |
| CHEMBL3315055 | — | EC50 | = | 32.8 | nM | 7.48 |
| CHEMBL1911270 | — | EC50 | = | 33.8 | nM | 7.47 |
| CHEMBL3315058 | — | EC50 | = | 36.4 | nM | 7.44 |
| CHEMBL3315053 | — | EC50 | = | 74.8 | nM | 7.13 |
| CHEMBL3315050 | — | EC50 | = | 109.1 | nM | 6.96 |
| CHEMBL3315060 | — | EC50 | = | 148.8 | nM | 6.83 |
| CHEMBL3315056 | — | EC50 | = | 203.2 | nM | 6.69 |