Assay Detail
Binding
CHEMBL3423886
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of fluorescein-labeled ES2 from human recombinant ERbeta receptor after 2 hrs by fluorescence polarization assay
18
Total Activities
18
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
Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 7.15 | 8.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3422028 | — | — | 1 | 8.02 |
| CHEMBL3422051 | — | — | 1 | 7.88 |
| CHEMBL3422034 | — | — | 1 | 7.71 |
| CHEMBL3422050 | — | — | 1 | 7.67 |
| CHEMBL3422035 | — | — | 1 | 7.56 |
| CHEMBL2386285 | — | — | 1 | 7.45 |
| CHEMBL3422037 | — | — | 1 | 7.44 |
| CHEMBL3422043 | — | — | 1 | 7.32 |
| CHEMBL3422029 | — | — | 1 | 7.31 |
| CHEMBL3422033 | — | — | 1 | 7.30 |
| CHEMBL3422036 | — | — | 1 | 7.28 |
| CHEMBL3422044 | — | — | 1 | 7.24 |
| CHEMBL3422032 | — | — | 1 | 6.74 |
| CHEMBL3422030 | — | — | 1 | 6.70 |
| CHEMBL3422052 | — | — | 1 | 6.53 |
| CHEMBL3422039 | — | — | 1 | 6.32 |
| CHEMBL3422042 | — | — | 1 | 6.29 |
| CHEMBL3422045 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3422028 | — | EC50 | = | 9.5 | nM | 8.02 |
| CHEMBL3422051 | — | EC50 | = | 13.3 | nM | 7.88 |
| CHEMBL3422034 | — | EC50 | = | 19.5 | nM | 7.71 |
| CHEMBL3422050 | — | EC50 | = | 21.3 | nM | 7.67 |
| CHEMBL3422035 | — | EC50 | = | 27.8 | nM | 7.56 |
| CHEMBL2386285 | — | EC50 | = | 35.2 | nM | 7.45 |
| CHEMBL3422037 | — | EC50 | = | 36.5 | nM | 7.44 |
| CHEMBL3422043 | — | EC50 | = | 47.7 | nM | 7.32 |
| CHEMBL3422029 | — | EC50 | = | 49.2 | nM | 7.31 |
| CHEMBL3422033 | — | EC50 | = | 49.9 | nM | 7.30 |
| CHEMBL3422036 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3422044 | — | EC50 | = | 57.5 | nM | 7.24 |
| CHEMBL3422032 | — | EC50 | = | 182.0 | nM | 6.74 |
| CHEMBL3422030 | — | EC50 | = | 202.0 | nM | 6.70 |
| CHEMBL3422052 | — | EC50 | = | 293.0 | nM | 6.53 |
| CHEMBL3422039 | — | EC50 | = | 478.0 | nM | 6.32 |
| CHEMBL3422042 | — | EC50 | = | 519.0 | nM | 6.29 |
| CHEMBL3422045 | — | EC50 | = | 1350.0 | nM | 5.87 |