Assay Detail
Functional
CHEMBL1648868
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Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as transactivation activity by luciferase reporter gene assay
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 7.40 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1644760 | — | — | 2 | 9.10 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 8.28 |
| CHEMBL1644759 | — | — | 1 | 8.15 |
| CHEMBL1644756 | — | — | 1 | 8.13 |
| CHEMBL258191 | — | — | 1 | 7.70 |
| CHEMBL1644755 | — | — | 1 | 7.02 |
| CHEMBL1644761 | — | — | 1 | 6.98 |
| CHEMBL1644757 | — | — | 1 | 6.67 |
| CHEMBL1644754 | — | — | 1 | 6.63 |
| CHEMBL1644765 | — | — | 1 | 6.43 |
| CHEMBL1644758 | — | — | 1 | - |
| CHEMBL1644764 | — | — | 1 | - |
| CHEMBL1644763 | — | — | 1 | - |
| CHEMBL1644762 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1644760 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL131 | PREDNISOLONE | EC50 | = | 5.3 | nM | 8.28 |
| CHEMBL1644759 | — | EC50 | = | 7.1 | nM | 8.15 |
| CHEMBL1644756 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL258191 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1644755 | — | EC50 | = | 95.0 | nM | 7.02 |
| CHEMBL1644761 | — | EC50 | = | 105.0 | nM | 6.98 |
| CHEMBL1644757 | — | EC50 | = | 215.0 | nM | 6.67 |
| CHEMBL1644754 | — | EC50 | = | 235.0 | nM | 6.63 |
| CHEMBL1644765 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL1644760 | — | EC50 | = | 483.0 | nM | 6.32 |
| CHEMBL1644758 | — | EC50 | - | — | - | |
| CHEMBL1644764 | — | EC50 | - | — | - | |
| CHEMBL1644763 | — | EC50 | - | — | - | |
| CHEMBL1644762 | — | EC50 | - | — | - |