Assay Detail
Binding
CHEMBL5033032
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at in human TLX LBD expressed in human HEK293T cells coexpressing Gal4-VP 16 assessed as increase in reporter activity measured after 14 hrs by luciferase reporter gene assay relative to control
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Nuclear receptor subfamily 2 group E member 1 (CHEMBL1961788) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 4.39 | 5.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL779 | TADALAFIL | 4.0 | 1 | 5.30 |
| CHEMBL31888 | — | — | 1 | 4.71 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 4.50 |
| CHEMBL275742 | DEXPROPRANOLOL | 2.0 | 1 | 4.40 |
| CHEMBL631 | PROPAFENONE | 4.0 | 1 | 4.33 |
| CHEMBL139737 | — | — | 1 | 4.30 |
| CHEMBL5083628 | — | — | 1 | 4.28 |
| CHEMBL3304960 | — | — | 1 | 4.17 |
| CHEMBL452861 | LEVOPROPRANOLOL | 2.0 | 1 | 4.14 |
| CHEMBL269236 | TRYPTOLINE | — | 1 | 4.13 |
| CHEMBL5088115 | — | — | 1 | 4.08 |
| CHEMBL24 | ATENOLOL | 4.0 | 1 | - |
| CHEMBL471 | SOTALOL | 4.0 | 1 | - |
| CHEMBL5070124 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL779 | TADALAFIL | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL31888 | — | EC50 | = | 19400.0 | nM | 4.71 |
| CHEMBL27 | PROPRANOLOL | EC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL275742 | DEXPROPRANOLOL | EC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL631 | PROPAFENONE | EC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL139737 | — | EC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL5083628 | — | EC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL3304960 | — | EC50 | = | 67000.0 | nM | 4.17 |
| CHEMBL452861 | LEVOPROPRANOLOL | EC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL269236 | TRYPTOLINE | EC50 | = | 74000.0 | nM | 4.13 |
| CHEMBL5088115 | — | EC50 | = | 83000.0 | nM | 4.08 |
| CHEMBL24 | ATENOLOL | EC50 | - | — | - | |
| CHEMBL471 | SOTALOL | EC50 | - | — | - | |
| CHEMBL5070124 | — | EC50 | > | 100000.0 | nM | - |