Assay Detail
Binding
CHEMBL676811
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]17-beta-estradiol binding to human recombinant Estrogen receptor alpha.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 19 | 6.17 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL411 | DIETHYLSTILBESTROL | 4.0 | 1 | 7.92 |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 7.66 |
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 7.62 |
| CHEMBL31721 | — | — | 1 | 6.47 |
| CHEMBL1405 | ESTRONE | 4.0 | 1 | 6.32 |
| CHEMBL286452 | ALFATRADIOL | 2.0 | 1 | 6.24 |
| CHEMBL31684 | — | — | 1 | 5.99 |
| CHEMBL431698 | RALOXIFENE CORE | — | 1 | 5.85 |
| CHEMBL284054 | — | — | 1 | 5.66 |
| CHEMBL31333 | — | — | 1 | 5.44 |
| CHEMBL32511 | — | — | 1 | 5.43 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 5.41 |
| CHEMBL32459 | — | — | 1 | 5.30 |
| CHEMBL31236 | — | — | 1 | 5.13 |
| CHEMBL32072 | — | — | 1 | - |
| CHEMBL418212 | — | — | 1 | - |
| CHEMBL284949 | — | — | 1 | - |
| CHEMBL31685 | — | — | 1 | - |
| CHEMBL280645 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL411 | DIETHYLSTILBESTROL | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL81 | RALOXIFENE | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL135 | ESTRADIOL | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL31721 | — | EC50 | = | 341.0 | nM | 6.47 |
| CHEMBL1405 | ESTRONE | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL286452 | ALFATRADIOL | EC50 | = | 570.0 | nM | 6.24 |
| CHEMBL31684 | — | EC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL431698 | RALOXIFENE CORE | EC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL284054 | — | EC50 | = | 2210.0 | nM | 5.66 |
| CHEMBL31333 | — | EC50 | = | 3650.0 | nM | 5.44 |
| CHEMBL32511 | — | EC50 | = | 3710.0 | nM | 5.43 |
| CHEMBL44 | GENISTEIN | EC50 | = | 3920.0 | nM | 5.41 |
| CHEMBL32459 | — | EC50 | = | 4980.0 | nM | 5.30 |
| CHEMBL31236 | — | EC50 | = | 7440.0 | nM | 5.13 |
| CHEMBL32072 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL418212 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL284949 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL31685 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL280645 | — | EC50 | > | 10000.0 | nM | - |