Assay Detail
Binding
CHEMBL4195063
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Agonist activity at GAL4 DNA-binding domain-tagged RARgamma (unknown origin) ligand-binding domain expressed in human HG5LN cells incubated for 18 hrs by luciferase reporter gene assay
32
Total Activities
32
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 | 32 | 7.82 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4210595 | — | — | 1 | 9.66 |
| CHEMBL4205733 | — | — | 1 | 9.04 |
| CHEMBL4202830 | — | — | 1 | 8.85 |
| CHEMBL3939687 | — | — | 1 | 8.72 |
| CHEMBL4206237 | — | — | 1 | 8.70 |
| CHEMBL3916016 | — | — | 1 | 8.68 |
| CHEMBL1265 | ADAPALENE | 4.0 | 1 | 8.51 |
| CHEMBL3936922 | — | — | 1 | 8.44 |
| CHEMBL4210099 | — | — | 1 | 8.36 |
| CHEMBL3960035 | — | — | 1 | 8.33 |
| CHEMBL4217953 | — | — | 1 | 8.22 |
| CHEMBL4216161 | — | — | 1 | 8.13 |
| CHEMBL3707313 | TRIFAROTENE | 4.0 | 1 | 8.11 |
| CHEMBL4215021 | — | — | 1 | 8.10 |
| CHEMBL3953756 | — | — | 1 | 8.00 |
| CHEMBL4212472 | — | — | 1 | 7.96 |
| CHEMBL4207786 | — | — | 1 | 7.82 |
| CHEMBL3891815 | — | — | 1 | 7.70 |
| CHEMBL4203742 | — | — | 1 | 7.66 |
| CHEMBL97080 | — | — | 1 | 7.34 |
| CHEMBL4217018 | — | — | 1 | 7.33 |
| CHEMBL1180 | O-DEMETHYLATED ADAPALENE | — | 1 | 7.31 |
| CHEMBL4216904 | — | — | 1 | 7.29 |
| CHEMBL4214493 | — | — | 1 | 7.22 |
| CHEMBL4207978 | — | — | 1 | 7.17 |
| CHEMBL4212684 | — | — | 1 | 7.07 |
| CHEMBL4215630 | — | — | 1 | 6.92 |
| CHEMBL4211195 | — | — | 1 | 6.78 |
| CHEMBL4205304 | — | — | 1 | 6.55 |
| CHEMBL4203950 | — | — | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4210595 | — | EC50 | = | 0.22 | nM | 9.66 |
| CHEMBL4205733 | — | EC50 | = | 0.92 | nM | 9.04 |
| CHEMBL4202830 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3939687 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4206237 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3916016 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1265 | ADAPALENE | EC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3936922 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4210099 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3960035 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4217953 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4216161 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL3707313 | TRIFAROTENE | EC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4215021 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3953756 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4212472 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4207786 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3891815 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4203742 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL97080 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4217018 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL1180 | O-DEMETHYLATED ADAPALENE | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4216904 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4214493 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4207978 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4212684 | — | EC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4215630 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4211195 | — | EC50 | = | 168.0 | nM | 6.78 |
| CHEMBL4205304 | — | EC50 | = | 279.0 | nM | 6.55 |
| CHEMBL4203950 | — | EC50 | = | 422.0 | nM | 6.38 |
| CHEMBL3910072 | — | EC50 | = | 918.0 | nM | 6.04 |
| CHEMBL4211171 | — | EC50 | > | 10000.0 | nM | - |