Assay Detail
Binding
CHEMBL4195072
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Inverse agonist activity at GAL4 DNA-binding domain-tagged RARabetaa (unknown origin) ligand-binding domain expressed in human HG5LN cells incubated for 18 hrs by luciferase reporter gene assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-based design of Trifarotene (CD5789), a potent and selective RARγ agonist for the treatment of acne.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 2 | 7.32 | 8.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3934863 | — | — | 1 | 8.02 |
| CHEMBL4210286 | — | — | 1 | 6.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3934863 | — | EC50 | = | 9.5 | nM | 8.02 |
| CHEMBL4210286 | — | EC50 | = | 248.0 | nM | 6.61 |