Assay Detail
ADMET
CHEMBL4195064
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Agonist activity at GAL4 DNA-binding domain-tagged RARalpha (unknown origin) ligand-binding domain expressed in human HG5LN cells incubated for 18 hrs by luciferase reporter gene assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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 | 25 | 6.90 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4212472 | — | — | 1 | 7.96 |
| CHEMBL1265 | ADAPALENE | 4.0 | 1 | 7.66 |
| CHEMBL4217953 | — | — | 1 | 7.47 |
| CHEMBL4205733 | — | — | 1 | 7.40 |
| CHEMBL4210595 | — | — | 1 | 7.37 |
| CHEMBL4203742 | — | — | 1 | 7.23 |
| CHEMBL3953756 | — | — | 1 | 6.99 |
| CHEMBL3939687 | — | — | 1 | 6.75 |
| CHEMBL3960035 | — | — | 1 | 6.75 |
| CHEMBL3916016 | — | — | 1 | 6.70 |
| CHEMBL4206237 | — | — | 1 | 6.67 |
| CHEMBL3891815 | — | — | 1 | 6.57 |
| CHEMBL4202830 | — | — | 1 | 6.50 |
| CHEMBL4210099 | — | — | 1 | 6.47 |
| CHEMBL97080 | — | — | 1 | 6.43 |
| CHEMBL3707313 | TRIFAROTENE | 4.0 | 1 | 6.30 |
| CHEMBL3936922 | — | — | 1 | 6.00 |
| CHEMBL4215021 | — | — | 1 | - |
| CHEMBL3934863 | — | — | 1 | - |
| CHEMBL1180 | O-DEMETHYLATED ADAPALENE | — | 1 | - |
| CHEMBL4216904 | — | — | 1 | - |
| CHEMBL4210286 | — | — | 1 | - |
| CHEMBL3910072 | — | — | 1 | - |
| CHEMBL4207978 | — | — | 1 | - |
| CHEMBL4211171 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4212472 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1265 | ADAPALENE | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4217953 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4205733 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4210595 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4203742 | — | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3953756 | — | EC50 | = | 103.0 | nM | 6.99 |
| CHEMBL3939687 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3960035 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3916016 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4206237 | — | EC50 | = | 212.0 | nM | 6.67 |
| CHEMBL3891815 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4202830 | — | EC50 | = | 317.0 | nM | 6.50 |
| CHEMBL4210099 | — | EC50 | = | 336.0 | nM | 6.47 |
| CHEMBL97080 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3707313 | TRIFAROTENE | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3936922 | — | EC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL4215021 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3934863 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1180 | O-DEMETHYLATED ADAPALENE | EC50 | > | 10000.0 | nM | - |
| CHEMBL4216904 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4210286 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3910072 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4207978 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4211171 | — | EC50 | > | 10000.0 | nM | - |