Assay Detail
Binding
CHEMBL4151838
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Antagonist activity at GR in human PBMC assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 6 hrs by RT-qPCR method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 7.68 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1276308 | MIFEPRISTONE | 4.0 | 1 | 7.75 |
| CHEMBL4161754 | — | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1276308 | MIFEPRISTONE | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL4161754 | — | IC50 | = | 24.9 | nM | 7.60 |