Assay Detail
Binding
CHEMBL939184
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Effect on human TRbeta transactivation activity in HeLa cells by luciferase reporter assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Characterization of thyroid hormone receptor alpha (TRalpha)-specific analogs with varying inner- and outer-ring substituents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 7.13 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1544 | LIOTHYRONINE | 4.0 | 1 | 8.62 |
| CHEMBL264153 | — | — | 1 | 7.57 |
| CHEMBL263631 | — | — | 1 | 7.50 |
| CHEMBL263630 | — | — | 1 | 7.24 |
| CHEMBL260482 | — | — | 1 | 7.00 |
| CHEMBL264152 | — | — | 1 | 6.75 |
| CHEMBL259096 | — | — | 1 | 6.67 |
| CHEMBL264410 | — | — | 1 | 6.58 |
| CHEMBL258886 | — | — | 1 | 6.28 |
| CHEMBL407819 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1544 | LIOTHYRONINE | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL264153 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL263631 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL263630 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL260482 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL264152 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL259096 | — | EC50 | = | 216.0 | nM | 6.67 |
| CHEMBL264410 | — | EC50 | = | 265.0 | nM | 6.58 |
| CHEMBL258886 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL407819 | — | EC50 | > | 10000.0 | nM | - |