Assay Detail
Binding
CHEMBL814598
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Binding affinity against human Thyroid hormone receptor alpha-1 (hTRalpha1) using radiolabeled T3
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 7 | 7.65 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1544 | LIOTHYRONINE | 4.0 | 1 | 10.00 |
| CHEMBL107400 | SOBETIROME | 2.0 | 1 | 8.74 |
| CHEMBL109430 | — | — | 1 | 8.28 |
| CHEMBL109279 | — | — | 1 | 7.03 |
| CHEMBL112087 | — | — | 1 | 6.70 |
| CHEMBL110158 | — | — | 1 | 6.48 |
| CHEMBL111953 | — | — | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1544 | LIOTHYRONINE | Kd | = | 0.1 | nM | 10.00 |
| CHEMBL107400 | SOBETIROME | Kd | = | 1.8 | nM | 8.74 |
| CHEMBL109430 | — | Kd | = | 5.2 | nM | 8.28 |
| CHEMBL109279 | — | Kd | = | 93.0 | nM | 7.03 |
| CHEMBL112087 | — | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL110158 | — | Kd | = | 330.0 | nM | 6.48 |
| CHEMBL111953 | — | Kd | = | 490.0 | nM | 6.31 |