Assay Detail
Functional
CHEMBL886324
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Agonist activity at human recombinant ERalpha expressed in HEK293 cells by transactivation assay
15
Total Activities
15
Compounds Tested
1
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
Bridged androstenediol analogs as ER-beta selective SERMs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.61 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 9.12 |
| CHEMBL245378 | — | — | 1 | 7.36 |
| CHEMBL246139 | — | — | 1 | 6.46 |
| CHEMBL397344 | — | — | 1 | 6.39 |
| CHEMBL245575 | — | — | 1 | 6.36 |
| CHEMBL246138 | — | — | 1 | 6.01 |
| CHEMBL393278 | — | — | 1 | 5.89 |
| CHEMBL246341 | — | — | 1 | 5.31 |
| CHEMBL246140 | — | — | 1 | - |
| CHEMBL245771 | — | — | 1 | - |
| CHEMBL438863 | — | — | 1 | - |
| CHEMBL245577 | — | — | 1 | - |
| CHEMBL245576 | — | — | 1 | - |
| CHEMBL397343 | — | — | 1 | - |
| CHEMBL392000 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | EC50 | = | 0.75 | nM | 9.12 |
| CHEMBL245378 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL246139 | — | EC50 | = | 344.0 | nM | 6.46 |
| CHEMBL397344 | — | EC50 | = | 407.0 | nM | 6.39 |
| CHEMBL245575 | — | EC50 | = | 435.0 | nM | 6.36 |
| CHEMBL246138 | — | EC50 | = | 980.0 | nM | 6.01 |
| CHEMBL393278 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL246341 | — | EC50 | = | 4893.0 | nM | 5.31 |
| CHEMBL246140 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL245771 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL438863 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL245577 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL245576 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL397343 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL392000 | — | EC50 | > | 1000.0 | nM | - |