Assay Detail
Functional
CHEMBL673864
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Ability to activate estrogen receptor 2-mediated transcription.
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationship of 3-arylbenzoxazines as selective estrogen receptor beta agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 19 | 7.32 | 9.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 9.17 |
| CHEMBL74758 | — | — | 1 | 8.15 |
| CHEMBL77609 | — | — | 1 | 8.10 |
| CHEMBL77620 | — | — | 1 | 7.80 |
| CHEMBL306636 | — | — | 1 | 7.75 |
| CHEMBL77930 | — | — | 1 | 7.58 |
| CHEMBL74757 | — | — | 1 | 7.52 |
| CHEMBL264862 | — | — | 3 | 7.33 |
| CHEMBL73989 | — | — | 1 | 7.11 |
| CHEMBL74027 | — | — | 1 | 6.92 |
| CHEMBL1405 | ESTRONE | 4.0 | 1 | 6.92 |
| CHEMBL307205 | — | — | 1 | 6.85 |
| CHEMBL77794 | — | — | 1 | 6.80 |
| CHEMBL77466 | — | — | 1 | 6.75 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 6.70 |
| CHEMBL77851 | — | — | 1 | 6.62 |
| CHEMBL74022 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | EC50 | = | 0.67 | nM | 9.17 |
| CHEMBL74758 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL77609 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL77620 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL306636 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL77930 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL74757 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL264862 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL264862 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL264862 | — | EC50 | = | 74.0 | nM | 7.13 |
| CHEMBL73989 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL74027 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1405 | ESTRONE | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL307205 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL77794 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL77466 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL44 | GENISTEIN | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL77851 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL74022 | — | EC50 | = | 270.0 | nM | 6.57 |