Assay Detail
Binding
CHEMBL3370899
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at glucocorticoid receptor in human HeLa cells assessed as NP-1 transactivation 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 | HeLa |
| 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 | 7.01 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3315066 | — | — | 1 | 8.89 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.35 |
| CHEMBL3315064 | — | — | 1 | 8.28 |
| CHEMBL3315061 | — | — | 1 | 8.26 |
| CHEMBL3315062 | — | — | 1 | 7.97 |
| CHEMBL3315063 | — | — | 1 | 7.96 |
| CHEMBL3315052 | — | — | 1 | 7.85 |
| CHEMBL3315051 | — | — | 1 | 7.57 |
| CHEMBL3315065 | — | — | 1 | 7.31 |
| CHEMBL3315070 | — | — | 1 | 7.23 |
| CHEMBL3315049 | — | — | 1 | 7.01 |
| CHEMBL3315069 | — | — | 1 | 6.97 |
| CHEMBL3315067 | — | — | 1 | 6.95 |
| CHEMBL3315068 | — | — | 1 | 6.84 |
| CHEMBL3315054 | — | — | 1 | 6.75 |
| CHEMBL1911270 | — | — | 1 | 6.62 |
| CHEMBL3315058 | — | — | 1 | 6.62 |
| CHEMBL3315057 | — | — | 1 | 6.52 |
| CHEMBL3315055 | — | — | 1 | 6.23 |
| CHEMBL3315059 | — | — | 1 | 6.17 |
| CHEMBL3315053 | — | — | 1 | 5.98 |
| CHEMBL3315050 | — | — | 1 | 5.98 |
| CHEMBL3315056 | — | — | 1 | 5.05 |
| CHEMBL3315060 | — | — | 1 | 4.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3315066 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3315064 | — | EC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3315061 | — | EC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3315062 | — | EC50 | = | 10.8 | nM | 7.97 |
| CHEMBL3315063 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3315052 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3315051 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3315065 | — | EC50 | = | 49.3 | nM | 7.31 |
| CHEMBL3315070 | — | EC50 | = | 59.2 | nM | 7.23 |
| CHEMBL3315049 | — | EC50 | = | 98.5 | nM | 7.01 |
| CHEMBL3315069 | — | EC50 | = | 107.4 | nM | 6.97 |
| CHEMBL3315067 | — | EC50 | = | 112.6 | nM | 6.95 |
| CHEMBL3315068 | — | EC50 | = | 142.9 | nM | 6.84 |
| CHEMBL3315054 | — | EC50 | = | 177.0 | nM | 6.75 |
| CHEMBL1911270 | — | EC50 | = | 242.0 | nM | 6.62 |
| CHEMBL3315058 | — | EC50 | = | 241.0 | nM | 6.62 |
| CHEMBL3315057 | — | EC50 | = | 302.0 | nM | 6.52 |
| CHEMBL3315055 | — | EC50 | = | 586.0 | nM | 6.23 |
| CHEMBL3315059 | — | EC50 | = | 676.0 | nM | 6.17 |
| CHEMBL3315053 | — | EC50 | = | 1043.0 | nM | 5.98 |
| CHEMBL3315050 | — | EC50 | = | 1046.0 | nM | 5.98 |
| CHEMBL3315056 | — | EC50 | = | 8912.0 | nM | 5.05 |
| CHEMBL3315060 | — | EC50 | = | 10530.0 | nM | 4.98 |