Assay Detail
Binding
CHEMBL909042
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Binding affinity to human GR
20
Total Activities
20
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
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 8.65 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222900 | — | — | 1 | 10.00 |
| CHEMBL376264 | — | — | 1 | 9.40 |
| CHEMBL221492 | — | — | 1 | 9.40 |
| CHEMBL218214 | — | — | 1 | 9.22 |
| CHEMBL220955 | — | — | 1 | 9.15 |
| CHEMBL221491 | — | — | 1 | 9.15 |
| CHEMBL221686 | — | — | 1 | 9.05 |
| CHEMBL1276308 | MIFEPRISTONE | 4.0 | 1 | 8.96 |
| CHEMBL219684 | — | — | 1 | 8.92 |
| CHEMBL222515 | — | — | 1 | 8.82 |
| CHEMBL223675 | — | — | 1 | 8.82 |
| CHEMBL384444 | — | — | 1 | 8.60 |
| CHEMBL374507 | — | — | 1 | 8.51 |
| CHEMBL222127 | — | — | 1 | 8.49 |
| CHEMBL426386 | — | — | 1 | 8.35 |
| CHEMBL374732 | — | — | 1 | 8.31 |
| CHEMBL221646 | — | — | 1 | 8.21 |
| CHEMBL221426 | — | — | 1 | 8.05 |
| CHEMBL221545 | — | — | 1 | 7.22 |
| CHEMBL373841 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222900 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL376264 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL221492 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL218214 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL220955 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL221491 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL221686 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1276308 | MIFEPRISTONE | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL219684 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL222515 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL223675 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL384444 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL374507 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL222127 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL426386 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL374732 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL221646 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL221426 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL221545 | — | IC50 | = | 60.7 | nM | 7.22 |
| CHEMBL373841 | — | IC50 | = | 481.5 | nM | 6.32 |