Assay Detail
Binding
CHEMBL683101
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of estradiol binding to estrogen receptor in Human Breast cancer cytosol (3.3% ethanol)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
(S)-(+)-4-[7-(2,2-dimethyl-1-oxopropoxy)-4-methyl-2-[4-[2-(1-piperidinyl)-ethoxy]phenyl]-2H-1-benzopyran-3-yl]-phenyl 2,2-dimethylpropanoate (EM-800): a highly potent, specific, and orally active nonsteroidal antiestrogen.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 9.01 | 10.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68055 | ACOLBIFENE | 3.0 | 1 | 10.33 |
| CHEMBL411 | DIETHYLSTILBESTROL | 4.0 | 1 | 9.90 |
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 9.86 |
| CHEMBL2137046 | — | — | 1 | 9.60 |
| CHEMBL67837 | — | — | 1 | 8.68 |
| CHEMBL1222035 | — | — | 1 | 8.34 |
| CHEMBL308234 | — | — | 1 | 8.33 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 8.12 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 1 | 7.92 |
| CHEMBL441622 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68055 | ACOLBIFENE | Ki | = | 0.047 | nM | 10.33 |
| CHEMBL411 | DIETHYLSTILBESTROL | Ki | = | 0.126 | nM | 9.90 |
| CHEMBL135 | ESTRADIOL | Ki | = | 0.138 | nM | 9.86 |
| CHEMBL2137046 | — | Ki | = | 0.249 | nM | 9.60 |
| CHEMBL67837 | — | Ki | = | 2.09 | nM | 8.68 |
| CHEMBL1222035 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL308234 | — | Ki | = | 4.71 | nM | 8.33 |
| CHEMBL1358 | FULVESTRANT | Ki | = | 7.63 | nM | 8.12 |
| CHEMBL83 | TAMOXIFEN | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL441622 | — | Ki | > | 270.0 | nM | - |