Assay Detail
Binding
CHEMBL832939
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human estrogen receptor 2 using tritiated estradiol incubated for 3 hr
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.66 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 8.96 |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 8.72 |
| CHEMBL183090 | — | — | 1 | 8.28 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 8.08 |
| CHEMBL182690 | — | — | 1 | 8.04 |
| CHEMBL304552 | — | — | 1 | 7.37 |
| CHEMBL180300 | — | — | 1 | 7.35 |
| CHEMBL182404 | — | — | 1 | 7.35 |
| CHEMBL183049 | — | — | 1 | 7.30 |
| CHEMBL182402 | — | — | 1 | 7.28 |
| CHEMBL362623 | — | — | 1 | 7.19 |
| CHEMBL183067 | — | — | 1 | 7.16 |
| CHEMBL180792 | — | — | 1 | 7.15 |
| CHEMBL183584 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL183090 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL1358 | FULVESTRANT | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL182690 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL304552 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL180300 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL182404 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL183049 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL182402 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL362623 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL183067 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL180792 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL183584 | — | IC50 | = | 87.0 | nM | 7.06 |