Assay Detail
Functional
CHEMBL941997
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Antagonist activity at human glucocorticoid receptor in SW1353 cells assessed as inhibition of dexamethasone-induced luciferase expression by MMTV5 reporter gene assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SW1353 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.08 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1276308 | MIFEPRISTONE | 4.0 | 1 | 8.92 |
| CHEMBL78625 | — | — | 1 | 8.40 |
| CHEMBL246834 | — | — | 1 | 6.75 |
| CHEMBL250700 | — | — | 1 | 6.70 |
| CHEMBL247632 | — | — | 1 | 6.70 |
| CHEMBL247234 | — | — | 1 | 6.70 |
| CHEMBL401013 | — | — | 1 | 6.64 |
| CHEMBL248027 | — | — | 1 | 6.49 |
| CHEMBL247006 | — | — | 1 | 6.40 |
| CHEMBL246835 | — | — | 1 | - |
| CHEMBL398668 | — | — | 1 | - |
| CHEMBL247815 | — | — | 1 | - |
| CHEMBL247638 | — | — | 1 | - |
| CHEMBL400161 | — | — | 1 | - |
| CHEMBL250288 | — | — | 1 | - |
| CHEMBL247814 | — | — | 1 | - |
| CHEMBL247812 | — | — | 1 | - |
| CHEMBL247051 | — | — | 1 | - |
| CHEMBL247634 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1276308 | MIFEPRISTONE | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL78625 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL246834 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL250700 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL247632 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL247234 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL401013 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL248027 | — | Ki | = | 323.0 | nM | 6.49 |
| CHEMBL247006 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL246835 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL398668 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL247815 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL247638 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL400161 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL250288 | — | Ki | - | — | - | |
| CHEMBL247814 | — | Ki | - | — | - | |
| CHEMBL247812 | — | Ki | - | — | - | |
| CHEMBL247051 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL247634 | — | Ki | - | — | - |