Assay Detail
Binding
CHEMBL4042886
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transrepression activity at glucocorticoid receptorin human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 8.23 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3893393 | — | — | 1 | 9.80 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 8.80 |
| CHEMBL4082878 | — | — | 1 | 8.40 |
| CHEMBL4069357 | — | — | 1 | 8.30 |
| CHEMBL1257572 | — | — | 1 | 8.30 |
| CHEMBL3962413 | — | — | 1 | 8.20 |
| CHEMBL4090392 | — | — | 1 | 8.20 |
| CHEMBL4085241 | — | — | 1 | 8.20 |
| CHEMBL4092066 | — | — | 1 | 7.80 |
| CHEMBL4072079 | — | — | 1 | 7.70 |
| CHEMBL4098118 | — | — | 1 | 7.70 |
| CHEMBL4064352 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3893393 | — | IC50 | = | 0.1585 | nM | 9.80 |
| CHEMBL384467 | DEXAMETHASONE | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL4082878 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4069357 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL1257572 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL3962413 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4090392 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4085241 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4092066 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4072079 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL4098118 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL4064352 | — | IC50 | = | 39.81 | nM | 7.40 |