Assay Detail
Binding
CHEMBL5166787
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Agonist activity at wild type human TR alpha LBD expressed in Escherichia coli BL21 (DE3) assessed as induction of N-terminal biotinylated coactivator SRC2-3 peptide recruitment by alphascreen assay
28
Total Activities
28
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 7.36 | 8.32 |
| Activity | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5172845 | — | — | 1 | 8.32 |
| CHEMBL5172205 | — | — | 1 | 8.05 |
| CHEMBL5209093 | — | — | 1 | 7.83 |
| CHEMBL5180999 | — | — | 1 | 7.80 |
| CHEMBL5188839 | — | — | 1 | 7.75 |
| CHEMBL5207186 | — | — | 1 | 7.62 |
| CHEMBL5186156 | — | — | 1 | 7.58 |
| CHEMBL4163070 | — | — | 1 | 7.53 |
| CHEMBL1544 | LIOTHYRONINE | 4.0 | 1 | 7.53 |
| CHEMBL2338329 | ROXADUSTAT | 4.0 | 1 | 7.49 |
| CHEMBL5179829 | — | — | 1 | 7.48 |
| CHEMBL5191021 | — | — | 1 | 7.44 |
| CHEMBL5171808 | — | — | 1 | 7.41 |
| CHEMBL5207720 | — | — | 1 | 7.35 |
| CHEMBL5193673 | — | — | 1 | 7.28 |
| CHEMBL5180738 | — | — | 1 | 7.25 |
| CHEMBL5207967 | — | — | 1 | 7.16 |
| CHEMBL5191155 | — | — | 1 | 7.04 |
| CHEMBL5206520 | — | — | 1 | 6.57 |
| CHEMBL5171818 | — | — | 1 | 6.52 |
| CHEMBL3261331 | RESMETIROM | 4.0 | 1 | 5.56 |
| CHEMBL5200322 | — | — | 1 | - |
| CHEMBL5178993 | — | — | 1 | - |
| CHEMBL5178553 | — | — | 1 | - |
| CHEMBL5181604 | — | — | 1 | - |
| CHEMBL5204264 | — | — | 1 | - |
| CHEMBL5205719 | — | — | 1 | - |
| CHEMBL5173831 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5172845 | — | EC50 | = | 4.8 | nM | 8.32 |
| CHEMBL5172205 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5209093 | — | EC50 | = | 14.7 | nM | 7.83 |
| CHEMBL5180999 | — | EC50 | = | 15.9 | nM | 7.80 |
| CHEMBL5188839 | — | EC50 | = | 17.6 | nM | 7.75 |
| CHEMBL5207186 | — | EC50 | = | 24.2 | nM | 7.62 |
| CHEMBL5186156 | — | EC50 | = | 26.6 | nM | 7.58 |
| CHEMBL4163070 | — | EC50 | = | 29.8 | nM | 7.53 |
| CHEMBL1544 | LIOTHYRONINE | EC50 | = | 29.7 | nM | 7.53 |
| CHEMBL2338329 | ROXADUSTAT | EC50 | = | 32.7 | nM | 7.49 |
| CHEMBL5179829 | — | EC50 | = | 32.8 | nM | 7.48 |
| CHEMBL5191021 | — | EC50 | = | 36.4 | nM | 7.44 |
| CHEMBL5171808 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5207720 | — | EC50 | = | 45.1 | nM | 7.35 |
| CHEMBL5193673 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5180738 | — | EC50 | = | 56.8 | nM | 7.25 |
| CHEMBL5207967 | — | EC50 | = | 69.1 | nM | 7.16 |
| CHEMBL5191155 | — | EC50 | = | 90.7 | nM | 7.04 |
| CHEMBL5206520 | — | EC50 | = | 270.4 | nM | 6.57 |
| CHEMBL5171818 | — | EC50 | = | 302.5 | nM | 6.52 |
| CHEMBL3261331 | RESMETIROM | EC50 | = | 2735.0 | nM | 5.56 |
| CHEMBL5200322 | — | Activity | - | — | - | |
| CHEMBL5178993 | — | Activity | - | — | - | |
| CHEMBL5178553 | — | Activity | - | — | - | |
| CHEMBL5181604 | — | Activity | - | — | - | |
| CHEMBL5204264 | — | Activity | - | — | - | |
| CHEMBL5205719 | — | Activity | - | — | - | |
| CHEMBL5173831 | — | Activity | - | — | - |