Assay Detail
Functional
CHEMBL925469
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Agonist activity at ERalpha expressed in HEK293 cells by transactivation assay
34
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Androstene-3,5-dienes as ER-beta selective SERMs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 6.83 | 9.12 |
| Activity | 17 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 2 | 9.12 |
| CHEMBL440283 | ANDROSTENEDIOL | -1.0 | 2 | 7.58 |
| CHEMBL398841 | — | — | 2 | 6.89 |
| CHEMBL400480 | — | — | 2 | 6.37 |
| CHEMBL249904 | — | — | 2 | 6.31 |
| CHEMBL250110 | — | — | 2 | 6.27 |
| CHEMBL430395 | — | — | 2 | 6.09 |
| CHEMBL246138 | — | — | 2 | 6.01 |
| CHEMBL246140 | — | — | 2 | - |
| CHEMBL249700 | — | — | 2 | - |
| CHEMBL250109 | — | — | 2 | - |
| CHEMBL398634 | — | — | 2 | - |
| CHEMBL398840 | — | — | 2 | - |
| CHEMBL249903 | — | — | 2 | - |
| CHEMBL398456 | — | — | 2 | - |
| CHEMBL251515 | — | — | 2 | - |
| CHEMBL398455 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | EC50 | = | 0.75 | nM | 9.12 |
| CHEMBL440283 | ANDROSTENEDIOL | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL398841 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL400480 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL249904 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL250110 | — | EC50 | = | 540.0 | nM | 6.27 |
| CHEMBL430395 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL246138 | — | EC50 | = | 980.0 | nM | 6.01 |
| CHEMBL398634 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL246138 | — | Activity | = | 35.0 | % | - |
| CHEMBL249904 | — | Activity | = | 15.0 | % | - |
| CHEMBL250109 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL398841 | — | Activity | = | 82.0 | % | - |
| CHEMBL440283 | ANDROSTENEDIOL | Activity | = | 91.0 | % | - |
| CHEMBL400480 | — | Activity | = | 49.0 | % | - |
| CHEMBL249700 | — | Activity | = | 29.0 | % | - |
| CHEMBL249700 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL250110 | — | Activity | = | 49.0 | % | - |
| CHEMBL246140 | — | Activity | = | 12.0 | % | - |
| CHEMBL246140 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL135 | ESTRADIOL | Activity | = | 100.0 | % | - |
| CHEMBL398455 | — | Activity | = | 28.0 | % | - |
| CHEMBL398455 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL251515 | — | Activity | = | 27.0 | % | - |
| CHEMBL251515 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL398456 | — | Activity | = | 4.0 | % | - |
| CHEMBL398456 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL249903 | — | Activity | = | 3.0 | % | - |
| CHEMBL249903 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL398840 | — | Activity | = | - | % | - |
| CHEMBL398840 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL430395 | — | Activity | = | 38.0 | % | - |
| CHEMBL250109 | — | Activity | = | 13.0 | % | - |
| CHEMBL398634 | — | Activity | = | 4.0 | % | - |