Assay Detail
Functional
CHEMBL886325
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human recombinant ERbeta 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 | 7.24 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 8.68 |
| CHEMBL246138 | — | — | 1 | 8.40 |
| CHEMBL246139 | — | — | 1 | 7.68 |
| CHEMBL245378 | — | — | 1 | 7.55 |
| CHEMBL397344 | — | — | 1 | 7.07 |
| CHEMBL246341 | — | — | 1 | 6.88 |
| CHEMBL245575 | — | — | 1 | 6.70 |
| CHEMBL393278 | — | — | 1 | 6.66 |
| CHEMBL246140 | — | — | 1 | 6.42 |
| CHEMBL397343 | — | — | 1 | 6.36 |
| CHEMBL392000 | — | — | 1 | - |
| CHEMBL245771 | — | — | 1 | - |
| CHEMBL438863 | — | — | 1 | - |
| CHEMBL245577 | — | — | 1 | - |
| CHEMBL245576 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL246138 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL246139 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL245378 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL397344 | — | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL246341 | — | EC50 | = | 132.0 | nM | 6.88 |
| CHEMBL245575 | — | EC50 | = | 198.0 | nM | 6.70 |
| CHEMBL393278 | — | EC50 | = | 219.0 | nM | 6.66 |
| CHEMBL246140 | — | EC50 | = | 379.0 | nM | 6.42 |
| CHEMBL397343 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL392000 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL245771 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL438863 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL245577 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL245576 | — | EC50 | > | 1000.0 | nM | - |