Assay Detail
Binding
CHEMBL4151790
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human GR expressed in CHO-K1 cells assessed as reduction in dexamethasone-induced response incubated for 20 hrs by luciferase reporter gene assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 | 28 | 7.78 | 8.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4172624 | — | — | 1 | 8.71 |
| CHEMBL1276308 | MIFEPRISTONE | 4.0 | 1 | 8.48 |
| CHEMBL4161754 | — | — | 1 | 8.25 |
| CHEMBL4159987 | — | — | 1 | 8.25 |
| CHEMBL4159692 | — | — | 1 | 8.07 |
| CHEMBL4167905 | — | — | 1 | 8.02 |
| CHEMBL4164157 | — | — | 1 | 7.95 |
| CHEMBL4164900 | — | — | 1 | 7.91 |
| CHEMBL4171957 | — | — | 1 | 7.88 |
| CHEMBL4159430 | — | — | 1 | 7.85 |
| CHEMBL4169685 | — | — | 1 | 7.84 |
| CHEMBL4163069 | — | — | 1 | 7.84 |
| CHEMBL4174418 | — | — | 1 | 7.80 |
| CHEMBL4170986 | — | — | 1 | 7.79 |
| CHEMBL4161175 | — | — | 1 | 7.78 |
| CHEMBL4173222 | — | — | 1 | 7.78 |
| CHEMBL4166499 | — | — | 1 | 7.76 |
| CHEMBL4167332 | — | — | 1 | 7.74 |
| CHEMBL4162539 | — | — | 1 | 7.71 |
| CHEMBL4167608 | — | — | 1 | 7.58 |
| CHEMBL4161483 | — | — | 1 | 7.55 |
| CHEMBL4174812 | — | — | 1 | 7.50 |
| CHEMBL4172798 | — | — | 1 | 7.37 |
| CHEMBL4165975 | — | — | 1 | 7.37 |
| CHEMBL4169408 | — | — | 1 | 7.32 |
| CHEMBL4161968 | — | — | 1 | 7.19 |
| CHEMBL4169100 | — | — | 1 | 6.69 |
| CHEMBL4174549 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4172624 | — | IC50 | = | 1.93 | nM | 8.71 |
| CHEMBL1276308 | MIFEPRISTONE | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4161754 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4159987 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4159692 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL4167905 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL4164157 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL4164900 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL4171957 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL4159430 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL4169685 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL4163069 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL4174418 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4170986 | — | IC50 | = | 16.1 | nM | 7.79 |
| CHEMBL4161175 | — | IC50 | = | 16.6 | nM | 7.78 |
| CHEMBL4173222 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL4166499 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL4167332 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL4162539 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL4167608 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4161483 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4174812 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4172798 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4165975 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4169408 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4161968 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4169100 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL4174549 | — | IC50 | > | 5000.0 | nM | - |