Assay Detail
Binding
CHEMBL5166788
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human TR beta LBD (202 to 461 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as induction of N-terminal biotinylated coactivator SRC2-3 peptide recruitment by alphascreen assay
32
Total Activities
32
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 | 28 | 7.66 | 8.60 |
| Activity | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5172845 | — | — | 1 | 8.60 |
| CHEMBL5209093 | — | — | 1 | 8.47 |
| CHEMBL5172205 | — | — | 1 | 8.30 |
| CHEMBL5186156 | — | — | 1 | 8.17 |
| CHEMBL5207186 | — | — | 1 | 8.16 |
| CHEMBL5179829 | — | — | 1 | 8.10 |
| CHEMBL5171808 | — | — | 1 | 8.06 |
| CHEMBL5188839 | — | — | 1 | 8.00 |
| CHEMBL5180999 | — | — | 1 | 7.92 |
| CHEMBL5191021 | — | — | 1 | 7.91 |
| CHEMBL4163070 | — | — | 1 | 7.90 |
| CHEMBL2338329 | ROXADUSTAT | 4.0 | 1 | 7.89 |
| CHEMBL5180738 | — | — | 1 | 7.89 |
| CHEMBL5193673 | — | — | 1 | 7.87 |
| CHEMBL5207720 | — | — | 1 | 7.76 |
| CHEMBL5191155 | — | — | 1 | 7.75 |
| CHEMBL5181604 | — | — | 1 | 7.75 |
| CHEMBL5178553 | — | — | 1 | 7.70 |
| CHEMBL5200322 | — | — | 1 | 7.68 |
| CHEMBL1544 | LIOTHYRONINE | 4.0 | 1 | 7.45 |
| CHEMBL5207967 | — | — | 1 | 7.32 |
| CHEMBL5178993 | — | — | 1 | 7.22 |
| CHEMBL5173831 | — | — | 1 | 7.16 |
| CHEMBL5171818 | — | — | 1 | 6.94 |
| CHEMBL5204264 | — | — | 1 | 6.82 |
| CHEMBL3261331 | RESMETIROM | 4.0 | 1 | 6.78 |
| CHEMBL5206520 | — | — | 1 | 6.65 |
| CHEMBL5205719 | — | — | 1 | 6.25 |
| CHEMBL5194312 | — | — | 1 | - |
| CHEMBL5176496 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5172845 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5209093 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5172205 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5186156 | — | EC50 | = | 6.8 | nM | 8.17 |
| CHEMBL5207186 | — | EC50 | = | 6.9 | nM | 8.16 |
| CHEMBL5179829 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5171808 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL5188839 | — | EC50 | = | 9.9 | nM | 8.00 |
| CHEMBL5180999 | — | EC50 | = | 11.9 | nM | 7.92 |
| CHEMBL5191021 | — | EC50 | = | 12.3 | nM | 7.91 |
| CHEMBL4163070 | — | EC50 | = | 12.6 | nM | 7.90 |
| CHEMBL2338329 | ROXADUSTAT | EC50 | = | 12.9 | nM | 7.89 |
| CHEMBL5180738 | — | EC50 | = | 12.9 | nM | 7.89 |
| CHEMBL5193673 | — | EC50 | = | 13.5 | nM | 7.87 |
| CHEMBL5207720 | — | EC50 | = | 17.2 | nM | 7.76 |
| CHEMBL5181604 | — | EC50 | = | 17.7 | nM | 7.75 |
| CHEMBL5191155 | — | EC50 | = | 17.8 | nM | 7.75 |
| CHEMBL5178553 | — | EC50 | = | 19.8 | nM | 7.70 |
| CHEMBL5200322 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1544 | LIOTHYRONINE | EC50 | = | 35.2 | nM | 7.45 |
| CHEMBL5207967 | — | EC50 | = | 48.3 | nM | 7.32 |
| CHEMBL5178993 | — | EC50 | = | 60.7 | nM | 7.22 |
| CHEMBL5173831 | — | EC50 | = | 69.1 | nM | 7.16 |
| CHEMBL5171818 | — | EC50 | = | 115.2 | nM | 6.94 |
| CHEMBL5204264 | — | EC50 | = | 151.4 | nM | 6.82 |
| CHEMBL3261331 | RESMETIROM | EC50 | = | 167.1 | nM | 6.78 |
| CHEMBL5206520 | — | EC50 | = | 222.0 | nM | 6.65 |
| CHEMBL5205719 | — | EC50 | = | 566.7 | nM | 6.25 |
| CHEMBL5194312 | — | Activity | - | — | - | |
| CHEMBL5176496 | — | Activity | - | — | - | |
| CHEMBL5204267 | — | Activity | - | — | - | |
| CHEMBL5208263 | — | Activity | - | — | - |