Assay Detail
Binding
CHEMBL941996
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Displacement of [3H]dexamethasone from human glucocorticoid receptor expressed in recombinant baculovirus
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 51 | 7.04 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1276308 | MIFEPRISTONE | 4.0 | 1 | 9.40 |
| CHEMBL78625 | — | — | 1 | 9.22 |
| CHEMBL246834 | — | — | 1 | 8.70 |
| CHEMBL250700 | — | — | 1 | 8.40 |
| CHEMBL247234 | — | — | 1 | 8.40 |
| CHEMBL400161 | — | — | 1 | 8.30 |
| CHEMBL401013 | — | — | 1 | 8.22 |
| CHEMBL246835 | — | — | 1 | 8.05 |
| CHEMBL247632 | — | — | 1 | 8.05 |
| CHEMBL247006 | — | — | 1 | 8.00 |
| CHEMBL248027 | — | — | 1 | 7.89 |
| CHEMBL247815 | — | — | 1 | 7.89 |
| CHEMBL247051 | — | — | 1 | 7.85 |
| CHEMBL247638 | — | — | 1 | 7.82 |
| CHEMBL247634 | — | — | 1 | 7.35 |
| CHEMBL247235 | — | — | 1 | 7.26 |
| CHEMBL398668 | — | — | 1 | 7.25 |
| CHEMBL247604 | — | — | 1 | 7.19 |
| CHEMBL247812 | — | — | 1 | 7.19 |
| CHEMBL250288 | — | — | 1 | 7.12 |
| CHEMBL247814 | — | — | 1 | 7.00 |
| CHEMBL397050 | — | — | 1 | 7.00 |
| CHEMBL247603 | — | — | 1 | 6.95 |
| CHEMBL395595 | — | — | 1 | 6.86 |
| CHEMBL247601 | — | — | 1 | 6.79 |
| CHEMBL247419 | — | — | 1 | 6.71 |
| CHEMBL247050 | — | — | 1 | 6.71 |
| CHEMBL247599 | — | — | 1 | 6.67 |
| CHEMBL393061 | — | — | 1 | 6.65 |
| CHEMBL247049 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1276308 | MIFEPRISTONE | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL78625 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL246834 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL250700 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL247234 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL400161 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL401013 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL246835 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL247632 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL247006 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL248027 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL247815 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL247051 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL247638 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL247634 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL247235 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL398668 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL247604 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL247812 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL250288 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL247814 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL397050 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL247603 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL395595 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL247601 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL247419 | — | Ki | = | 196.0 | nM | 6.71 |
| CHEMBL247050 | — | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL247599 | — | Ki | = | 216.0 | nM | 6.67 |
| CHEMBL393061 | — | Ki | = | 225.0 | nM | 6.65 |
| CHEMBL247049 | — | Ki | = | 432.0 | nM | 6.37 |
| CHEMBL247602 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL392667 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL247421 | — | Ki | = | 950.0 | nM | 6.02 |
| CHEMBL391182 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL393265 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL247418 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL247600 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL247236 | — | Ki | = | 1950.0 | nM | 5.71 |
| CHEMBL247420 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL247231 | — | Ki | = | 2250.0 | nM | 5.65 |
| CHEMBL247417 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL247048 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL247233 | — | Ki | = | 4450.0 | nM | 5.35 |
| CHEMBL247232 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL439025 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL247047 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL247046 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL247598 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL247597 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL397051 | — | Ki | > | 10000.0 | nM | - |