Assay Detail
Binding
CHEMBL683104
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Apparent inhibition constant for estrogen receptor in Human uterine cytosol in 3.3%ethanol
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Uterus |
| Subcellular | Cytosol |
| 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 | 6 | 9.37 | 10.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68055 | ACOLBIFENE | 3.0 | 1 | 10.38 |
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 9.92 |
| CHEMBL411 | DIETHYLSTILBESTROL | 4.0 | 1 | 9.89 |
| CHEMBL2137046 | — | — | 1 | 9.46 |
| CHEMBL1222035 | — | — | 1 | 8.63 |
| CHEMBL308234 | — | — | 1 | 7.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68055 | ACOLBIFENE | Ki | = | 0.042 | nM | 10.38 |
| CHEMBL135 | ESTRADIOL | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL411 | DIETHYLSTILBESTROL | Ki | = | 0.128 | nM | 9.89 |
| CHEMBL2137046 | — | Ki | = | 0.346 | nM | 9.46 |
| CHEMBL1222035 | — | Ki | = | 2.33 | nM | 8.63 |
| CHEMBL308234 | — | Ki | = | 11.14 | nM | 7.95 |