Assay Detail
Binding
CHEMBL1019341
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transrepression activity at GR in PMA-stimulated human A549 cells assessed as inhibition of AP1 response element-induced luciferase reporter gene activity
30
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 novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 6.69 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.60 |
| CHEMBL474189 | — | — | 3 | 8.28 |
| CHEMBL514630 | — | — | 3 | 7.94 |
| CHEMBL131 | PREDNISOLONE | 4.0 | 1 | 7.80 |
| CHEMBL514646 | — | — | 1 | 6.94 |
| CHEMBL474188 | — | — | 1 | 6.92 |
| CHEMBL514636 | — | — | 1 | 6.64 |
| CHEMBL473801 | — | — | 1 | 6.61 |
| CHEMBL475159 | — | — | 1 | 6.57 |
| CHEMBL515738 | — | — | 1 | 6.53 |
| CHEMBL515127 | — | — | 1 | 6.48 |
| CHEMBL474770 | — | — | 3 | 6.46 |
| CHEMBL474576 | — | — | 1 | 6.26 |
| CHEMBL473802 | — | — | 1 | 6.08 |
| CHEMBL474966 | — | — | 1 | 6.06 |
| CHEMBL514455 | — | — | 1 | 6.04 |
| CHEMBL516386 | — | — | 1 | 5.97 |
| CHEMBL514481 | — | — | 1 | 5.94 |
| CHEMBL474965 | — | — | 1 | 5.91 |
| CHEMBL474381 | — | — | 1 | - |
| CHEMBL474771 | — | — | 1 | - |
| CHEMBL514185 | — | — | 1 | - |
| CHEMBL472801 | — | — | 1 | - |
| CHEMBL472800 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL474189 | — | EC50 | = | 5.3 | nM | 8.28 |
| CHEMBL514630 | — | EC50 | = | 11.4 | nM | 7.94 |
| CHEMBL474189 | — | EC50 | = | 14.7 | nM | 7.83 |
| CHEMBL131 | PREDNISOLONE | EC50 | = | 15.8 | nM | 7.80 |
| CHEMBL514630 | — | EC50 | = | 16.9 | nM | 7.77 |
| CHEMBL514646 | — | EC50 | = | 114.9 | nM | 6.94 |
| CHEMBL474188 | — | EC50 | = | 118.8 | nM | 6.92 |
| CHEMBL514636 | — | EC50 | = | 229.4 | nM | 6.64 |
| CHEMBL473801 | — | EC50 | = | 243.1 | nM | 6.61 |
| CHEMBL475159 | — | EC50 | = | 268.0 | nM | 6.57 |
| CHEMBL515738 | — | EC50 | = | 294.9 | nM | 6.53 |
| CHEMBL515127 | — | EC50 | = | 330.6 | nM | 6.48 |
| CHEMBL474770 | — | EC50 | = | 345.0 | nM | 6.46 |
| CHEMBL474576 | — | EC50 | = | 543.5 | nM | 6.26 |
| CHEMBL474770 | — | EC50 | = | 609.8 | nM | 6.21 |
| CHEMBL474189 | — | EC50 | = | 800.4 | nM | 6.10 |
| CHEMBL473802 | — | EC50 | = | 836.8 | nM | 6.08 |
| CHEMBL474966 | — | EC50 | = | 874.2 | nM | 6.06 |
| CHEMBL514455 | — | EC50 | = | 922.6 | nM | 6.04 |
| CHEMBL474770 | — | EC50 | = | 972.5 | nM | 6.01 |
| CHEMBL516386 | — | EC50 | = | 1067.3 | nM | 5.97 |
| CHEMBL514481 | — | EC50 | = | 1159.6 | nM | 5.94 |
| CHEMBL474965 | — | EC50 | = | 1236.0 | nM | 5.91 |
| CHEMBL514630 | — | EC50 | = | 3835.0 | nM | 5.42 |
| CHEMBL474381 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL474771 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL472801 | — | EC50 | > | 2500.0 | nM | - |
| CHEMBL472800 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL514185 | — | EC50 | > | 5000.0 | nM | - |