Assay Detail
Binding
CHEMBL867061
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Displacement of [3H]4-OHT from ERRgamma
11
Total Activities
11
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
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.92 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL203472 | — | — | 1 | 8.30 |
| CHEMBL2137046 | — | — | 1 | 7.89 |
| CHEMBL1402 | 4-HYDROXYTORMIFENE | — | 1 | 7.89 |
| CHEMBL201013 | — | — | 1 | 7.10 |
| CHEMBL383112 | — | — | 1 | 6.89 |
| CHEMBL202615 | — | — | 1 | 6.80 |
| CHEMBL204697 | — | — | 1 | 6.70 |
| CHEMBL204376 | — | — | 1 | 6.60 |
| CHEMBL383533 | — | — | 1 | 6.10 |
| CHEMBL369935 | — | — | 1 | 6.00 |
| CHEMBL204970 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL203472 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2137046 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1402 | 4-HYDROXYTORMIFENE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL201013 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL383112 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL202615 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL204697 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL204376 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL383533 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL369935 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL204970 | — | IC50 | = | 1300.0 | nM | 5.89 |