Assay Detail
Functional
CHEMBL676806
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Ability to activate estrogen receptor 1-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 | 6.45 | 9.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 9.32 |
| CHEMBL77620 | — | — | 1 | 7.34 |
| CHEMBL74758 | — | — | 1 | 7.23 |
| CHEMBL74757 | — | — | 1 | 7.19 |
| CHEMBL1405 | ESTRONE | 4.0 | 1 | 6.92 |
| CHEMBL264862 | — | — | 3 | 6.85 |
| CHEMBL77609 | — | — | 1 | 6.77 |
| CHEMBL77930 | — | — | 1 | 6.77 |
| CHEMBL73989 | — | — | 1 | 6.05 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 6.02 |
| CHEMBL74027 | — | — | 1 | 5.85 |
| CHEMBL306636 | — | — | 1 | 5.77 |
| CHEMBL74022 | — | — | 1 | 5.75 |
| CHEMBL77466 | — | — | 1 | 5.70 |
| CHEMBL307205 | — | — | 1 | 5.51 |
| CHEMBL77794 | — | — | 1 | 5.16 |
| CHEMBL77851 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | EC50 | = | 0.48 | nM | 9.32 |
| CHEMBL77620 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL74758 | — | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL74757 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1405 | ESTRONE | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL264862 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL264862 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL77609 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL77930 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL264862 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL73989 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL44 | GENISTEIN | EC50 | = | 950.0 | nM | 6.02 |
| CHEMBL74027 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL306636 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL74022 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL77466 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL307205 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL77794 | — | EC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL77851 | — | EC50 | = | 12000.0 | nM | 4.92 |