Assay Detail
Binding
CHEMBL4685966
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of fluorescent-labelled E2 from recombinant human GST-tagged ERalpha by LanthaScreen TR-FRET assay
13
Total Activities
13
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
Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.51 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 9.48 |
| CHEMBL4761289 | — | — | 1 | 9.38 |
| CHEMBL4758245 | — | — | 1 | 8.89 |
| CHEMBL4790840 | — | — | 1 | 8.78 |
| CHEMBL279301 | — | — | 1 | 8.65 |
| CHEMBL4790191 | — | — | 1 | 8.63 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 8.54 |
| CHEMBL4755319 | — | — | 1 | 8.45 |
| CHEMBL195515 | — | — | 1 | 8.27 |
| CHEMBL4784145 | — | — | 1 | 8.19 |
| CHEMBL4793264 | — | — | 1 | 7.87 |
| CHEMBL4794674 | — | — | 1 | 7.82 |
| CHEMBL4791340 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL4761289 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL4758245 | — | IC50 | = | 1.28 | nM | 8.89 |
| CHEMBL4790840 | — | IC50 | = | 1.67 | nM | 8.78 |
| CHEMBL279301 | — | IC50 | = | 2.24 | nM | 8.65 |
| CHEMBL4790191 | — | IC50 | = | 2.35 | nM | 8.63 |
| CHEMBL1358 | FULVESTRANT | IC50 | = | 2.85 | nM | 8.54 |
| CHEMBL4755319 | — | IC50 | = | 3.52 | nM | 8.45 |
| CHEMBL195515 | — | IC50 | = | 5.35 | nM | 8.27 |
| CHEMBL4784145 | — | IC50 | = | 6.43 | nM | 8.19 |
| CHEMBL4793264 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL4794674 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL4791340 | — | IC50 | = | 18.9 | nM | 7.72 |