Assay Detail
Binding
CHEMBL2330135
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]E2 from human recombinant ERbeta receptor after overnight incubation by liquid scintillation counting analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of novel estrogen receptor antagonists using metal-catalyzed coupling reactions and characterization of their biological activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.97 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 8.06 |
| CHEMBL2326072 | — | — | 1 | 7.72 |
| CHEMBL2326068 | — | — | 1 | 7.38 |
| CHEMBL2326070 | — | — | 1 | 6.95 |
| CHEMBL2326073 | — | — | 1 | 6.92 |
| CHEMBL2326069 | — | — | 1 | 6.82 |
| CHEMBL2326076 | — | — | 1 | 6.73 |
| CHEMBL2326074 | — | — | 1 | 6.48 |
| CHEMBL2326075 | — | — | 1 | 6.36 |
| CHEMBL2326071 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL2326072 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL2326068 | — | IC50 | = | 41.2 | nM | 7.38 |
| CHEMBL2326070 | — | IC50 | = | 111.9 | nM | 6.95 |
| CHEMBL2326073 | — | IC50 | = | 120.7 | nM | 6.92 |
| CHEMBL2326069 | — | IC50 | = | 150.6 | nM | 6.82 |
| CHEMBL2326076 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL2326074 | — | IC50 | = | 331.1 | nM | 6.48 |
| CHEMBL2326075 | — | IC50 | = | 436.4 | nM | 6.36 |
| CHEMBL2326071 | — | IC50 | = | 565.9 | nM | 6.25 |