Assay Detail
Binding
CHEMBL3370895
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Agonist activity at glucocorticoid receptor in human A549 cells assessed as AP-1 transrepression by luciferase reporter gene assay
24
Total Activities
24
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 | 24 | 7.87 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3315066 | — | — | 1 | 9.10 |
| CHEMBL3315064 | — | — | 1 | 8.80 |
| CHEMBL3315062 | — | — | 1 | 8.68 |
| CHEMBL3315061 | — | — | 1 | 8.68 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.60 |
| CHEMBL3315052 | — | — | 1 | 8.30 |
| CHEMBL3315051 | — | — | 1 | 8.29 |
| CHEMBL3315063 | — | — | 1 | 8.21 |
| CHEMBL3315070 | — | — | 1 | 8.17 |
| CHEMBL3315065 | — | — | 1 | 8.06 |
| CHEMBL3315057 | — | — | 1 | 7.97 |
| CHEMBL3315067 | — | — | 1 | 7.78 |
| CHEMBL3315059 | — | — | 1 | 7.76 |
| CHEMBL3315055 | — | — | 1 | 7.76 |
| CHEMBL3315049 | — | — | 1 | 7.75 |
| CHEMBL3315054 | — | — | 1 | 7.74 |
| CHEMBL3315068 | — | — | 1 | 7.69 |
| CHEMBL3315069 | — | — | 1 | 7.66 |
| CHEMBL3315053 | — | — | 1 | 7.62 |
| CHEMBL1911270 | — | — | 1 | 7.48 |
| CHEMBL3315058 | — | — | 1 | 7.47 |
| CHEMBL3315050 | — | — | 1 | 6.67 |
| CHEMBL3315060 | — | — | 1 | 6.61 |
| CHEMBL3315056 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3315066 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3315064 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3315062 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3315061 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3315052 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3315051 | — | EC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3315063 | — | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3315070 | — | EC50 | = | 6.7 | nM | 8.17 |
| CHEMBL3315065 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL3315057 | — | EC50 | = | 10.7 | nM | 7.97 |
| CHEMBL3315067 | — | EC50 | = | 16.5 | nM | 7.78 |
| CHEMBL3315059 | — | EC50 | = | 17.5 | nM | 7.76 |
| CHEMBL3315055 | — | EC50 | = | 17.5 | nM | 7.76 |
| CHEMBL3315049 | — | EC50 | = | 17.7 | nM | 7.75 |
| CHEMBL3315054 | — | EC50 | = | 18.4 | nM | 7.74 |
| CHEMBL3315068 | — | EC50 | = | 20.3 | nM | 7.69 |
| CHEMBL3315069 | — | EC50 | = | 21.9 | nM | 7.66 |
| CHEMBL3315053 | — | EC50 | = | 23.7 | nM | 7.62 |
| CHEMBL1911270 | — | EC50 | = | 33.2 | nM | 7.48 |
| CHEMBL3315058 | — | EC50 | = | 34.2 | nM | 7.47 |
| CHEMBL3315050 | — | EC50 | = | 212.6 | nM | 6.67 |
| CHEMBL3315060 | — | EC50 | = | 243.6 | nM | 6.61 |
| CHEMBL3315056 | — | EC50 | = | 907.0 | nM | 6.04 |