Assay Detail
Binding
CHEMBL909043
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Activity at GR expressed in CHO cells assessed as decrease in dexamethasone-stimulated alkaline phosphatase production by GRAF assay
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.94 | 8.96 |
| Activity | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222900 | — | — | 1 | 8.96 |
| CHEMBL218214 | — | — | 1 | 8.74 |
| CHEMBL221492 | — | — | 1 | 8.55 |
| CHEMBL220955 | — | — | 1 | 8.38 |
| CHEMBL376264 | — | — | 1 | 8.33 |
| CHEMBL1276308 | MIFEPRISTONE | 4.0 | 1 | 8.30 |
| CHEMBL221686 | — | — | 1 | 8.12 |
| CHEMBL219684 | — | — | 1 | 8.00 |
| CHEMBL221491 | — | — | 1 | 8.00 |
| CHEMBL222127 | — | — | 1 | 7.82 |
| CHEMBL222515 | — | — | 1 | 7.73 |
| CHEMBL223675 | — | — | 1 | 7.68 |
| CHEMBL384444 | — | — | 1 | 7.63 |
| CHEMBL426386 | — | — | 1 | 7.54 |
| CHEMBL374507 | — | — | 1 | 7.51 |
| CHEMBL221426 | — | — | 1 | 7.50 |
| CHEMBL221646 | — | — | 1 | 7.37 |
| CHEMBL374732 | — | — | 1 | 6.70 |
| CHEMBL221545 | — | — | 1 | - |
| CHEMBL373841 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222900 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL218214 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL221492 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL220955 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL376264 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL1276308 | MIFEPRISTONE | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL221686 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL219684 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL221491 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL222127 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL222515 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL223675 | — | IC50 | = | 20.9 | nM | 7.68 |
| CHEMBL384444 | — | IC50 | = | 23.5 | nM | 7.63 |
| CHEMBL426386 | — | IC50 | = | 28.6 | nM | 7.54 |
| CHEMBL374507 | — | IC50 | = | 30.7 | nM | 7.51 |
| CHEMBL221426 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL221646 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL374732 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL221545 | — | Activity | - | — | - | |
| CHEMBL373841 | — | Activity | - | — | - |