Assay Detail
Binding
CHEMBL4413809
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Binding affinity to ERalpha (unknown origin) using fluorescein-conjugated coactivator PGC-1alpha incubated for 1 hr by TR-FRET assay
16
Total Activities
16
Compounds Tested
1
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 Potent, Selective, and Orally Bioavailable Estrogen-Related Receptor-γ Inverse Agonists To Restore the Sodium Iodide Symporter Function in Anaplastic Thyroid Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.76 | 5.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4563806 | — | — | 1 | 5.94 |
| CHEMBL4436391 | — | — | 1 | 5.91 |
| CHEMBL4441903 | — | — | 1 | 5.78 |
| CHEMBL4438589 | — | — | 1 | 5.77 |
| CHEMBL4451327 | — | — | 1 | 5.71 |
| CHEMBL3932162 | — | — | 1 | 5.70 |
| CHEMBL4586542 | — | — | 1 | 5.67 |
| CHEMBL4513294 | — | — | 1 | 5.60 |
| CHEMBL4585424 | — | — | 1 | - |
| CHEMBL4443694 | — | — | 1 | - |
| CHEMBL4462077 | — | — | 1 | - |
| CHEMBL4472718 | — | — | 1 | - |
| CHEMBL4541589 | — | — | 1 | - |
| CHEMBL4437929 | — | — | 1 | - |
| CHEMBL4580171 | — | — | 1 | - |
| CHEMBL4579002 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4563806 | — | IC50 | = | 1142.0 | nM | 5.94 |
| CHEMBL4436391 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL4441903 | — | IC50 | = | 1658.0 | nM | 5.78 |
| CHEMBL4438589 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4451327 | — | IC50 | = | 1943.0 | nM | 5.71 |
| CHEMBL3932162 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4586542 | — | IC50 | = | 2116.0 | nM | 5.67 |
| CHEMBL4513294 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4585424 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4443694 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4462077 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4472718 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4541589 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4437929 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4580171 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4579002 | — | IC50 | > | 10000.0 | nM | - |