Assay Detail
Functional
CHEMBL897788
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Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation
30
Total Activities
12
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Log IC50 | 14 | - | - |
| IC50 | 8 | 6.65 | 7.94 |
| Inhibition | 8 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1276308 | MIFEPRISTONE | 4.0 | 2 | 7.94 |
| CHEMBL235205 | — | — | 3 | 6.56 |
| CHEMBL391874 | — | — | 5 | 6.51 |
| CHEMBL392319 | — | — | 4 | 6.22 |
| CHEMBL236320 | — | — | 1 | - |
| CHEMBL235208 | — | — | 3 | - |
| CHEMBL234988 | — | — | 2 | - |
| CHEMBL393011 | — | — | 3 | - |
| CHEMBL237973 | — | — | 2 | - |
| CHEMBL394168 | — | — | 1 | - |
| CHEMBL236947 | — | — | 2 | - |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1276308 | MIFEPRISTONE | IC50 | = | 11.48 | nM | 7.94 |
| CHEMBL235205 | — | IC50 | = | 275.42 | nM | 6.56 |
| CHEMBL391874 | — | IC50 | = | 309.03 | nM | 6.51 |
| CHEMBL392319 | — | IC50 | = | 602.56 | nM | 6.22 |
| CHEMBL392319 | — | IC50 | = | 933.25 | nM | 6.03 |
| CHEMBL391874 | — | Log IC50 | - | — | - | |
| CHEMBL235208 | — | Log IC50 | - | — | - | |
| CHEMBL391874 | — | Log IC50 | - | — | - | |
| CHEMBL236947 | — | Log IC50 | - | — | - | |
| CHEMBL236947 | — | Log IC50 | - | — | - | |
| CHEMBL394168 | — | Log IC50 | - | — | - | |
| CHEMBL237973 | — | Log IC50 | - | — | - | |
| CHEMBL237973 | — | Log IC50 | - | — | - | |
| CHEMBL393011 | — | Log IC50 | - | — | - | |
| CHEMBL235205 | — | Log IC50 | - | — | - | |
| CHEMBL234988 | — | Log IC50 | - | — | - | |
| CHEMBL234988 | — | Log IC50 | - | — | - | |
| CHEMBL391874 | — | Log IC50 | - | — | - | |
| CHEMBL236320 | — | Log IC50 | - | — | - | |
| CHEMBL235208 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL393011 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL384467 | DEXAMETHASONE | Inhibition | = | 7.0 | % | - |
| CHEMBL391874 | — | Inhibition | = | 67.0 | % | - |
| CHEMBL392319 | — | Inhibition | = | 87.0 | % | - |
| CHEMBL392319 | — | Inhibition | = | 93.0 | % | - |
| CHEMBL393011 | — | Inhibition | = | 11.0 | % | - |
| CHEMBL235205 | — | Inhibition | = | 93.0 | % | - |
| CHEMBL235208 | — | Inhibition | = | 4.0 | % | - |
| CHEMBL1276308 | MIFEPRISTONE | Inhibition | = | 100.0 | % | - |
| CHEMBL384467 | DEXAMETHASONE | IC50 | < | 1000.0 | nM | - |