Assay Detail
ADMET
CHEMBL4042888
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Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of new selective glucocorticoid receptor agonist leads.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.73 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3893393 | — | — | 1 | 9.20 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.10 |
| CHEMBL3962413 | — | — | 1 | 8.00 |
| CHEMBL4069357 | — | — | 1 | 7.90 |
| CHEMBL4085241 | — | — | 1 | 7.90 |
| CHEMBL1257572 | — | — | 1 | 7.90 |
| CHEMBL4090392 | — | — | 1 | 7.60 |
| CHEMBL4092066 | — | — | 1 | 7.60 |
| CHEMBL4082878 | — | — | 1 | 7.60 |
| CHEMBL4098118 | — | — | 1 | 7.40 |
| CHEMBL4072079 | — | — | 1 | 6.80 |
| CHEMBL4064352 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3893393 | — | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL384467 | DEXAMETHASONE | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL3962413 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4069357 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4085241 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL1257572 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4090392 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4092066 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4082878 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4098118 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4072079 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4064352 | — | IC50 | = | 158.49 | nM | 6.80 |