Assay Detail
Binding
CHEMBL5250900
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Agonist activity at human THRalpha transfected in Huh7 cells co-transfected with luciferase reporter plasmid assessed as reduction in luciferase activity incubated for 16 hrs by Steady-Glo luciferase assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Huh-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Highly Potent and Selective Thyroid Hormone Receptor β Agonists for the Treatment of Nonalcoholic Steatohepatitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 6.81 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1544 | LIOTHYRONINE | 4.0 | 1 | 9.15 |
| CHEMBL5267199 | — | — | 1 | 7.70 |
| CHEMBL5266872 | — | — | 1 | 7.40 |
| CHEMBL5274251 | — | — | 1 | 7.30 |
| CHEMBL5286305 | — | — | 1 | 7.30 |
| CHEMBL5281631 | — | — | 1 | 6.92 |
| CHEMBL5281151 | — | — | 1 | 6.89 |
| CHEMBL5279191 | — | — | 1 | 6.66 |
| CHEMBL5284123 | — | — | 1 | 6.47 |
| CHEMBL5271234 | — | — | 1 | 6.37 |
| CHEMBL5269031 | — | — | 1 | 6.36 |
| CHEMBL5268293 | — | — | 1 | 6.13 |
| CHEMBL5284849 | — | — | 1 | 6.09 |
| CHEMBL5283585 | — | — | 1 | 5.85 |
| CHEMBL3261331 | RESMETIROM | 4.0 | 1 | 5.54 |
| CHEMBL5281233 | — | — | 1 | - |
| CHEMBL5290997 | — | — | 1 | - |
| CHEMBL5269734 | — | — | 1 | - |
| CHEMBL5277807 | — | — | 1 | - |
| CHEMBL5290804 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1544 | LIOTHYRONINE | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5267199 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5266872 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5274251 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5286305 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5281631 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5281151 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5279191 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5284123 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5271234 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5269031 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5268293 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL5284849 | — | EC50 | = | 810.0 | nM | 6.09 |
| CHEMBL5283585 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3261331 | RESMETIROM | EC50 | = | 2850.0 | nM | 5.54 |
| CHEMBL5281233 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5290997 | — | EC50 | > | 33000.0 | nM | - |
| CHEMBL5269734 | — | EC50 | > | 1200.0 | nM | - |
| CHEMBL5277807 | — | EC50 | > | 3700.0 | nM | - |
| CHEMBL5290804 | — | EC50 | > | 11000.0 | nM | - |