Assay Detail
Binding
CHEMBL831007
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor alpha; ERE assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.46 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 8.62 |
| CHEMBL328190 | LASOFOXIFENE | 4.0 | 1 | 8.51 |
| CHEMBL101382 | — | — | 1 | 7.78 |
| CHEMBL364492 | — | — | 1 | 7.75 |
| CHEMBL194334 | — | — | 1 | 7.74 |
| CHEMBL195466 | — | — | 1 | 7.71 |
| CHEMBL191646 | — | — | 1 | 7.66 |
| CHEMBL195212 | — | — | 1 | 7.63 |
| CHEMBL372029 | — | — | 1 | 7.51 |
| CHEMBL195118 | — | — | 1 | 7.50 |
| CHEMBL195465 | — | — | 1 | 7.46 |
| CHEMBL192187 | — | — | 1 | 7.34 |
| CHEMBL426461 | — | — | 1 | 7.33 |
| CHEMBL427533 | — | — | 1 | 7.26 |
| CHEMBL195216 | — | — | 1 | 7.19 |
| CHEMBL372011 | — | — | 1 | 6.82 |
| CHEMBL192055 | — | — | 1 | 6.29 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL81 | RALOXIFENE | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL328190 | LASOFOXIFENE | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL101382 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL364492 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL194334 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL195466 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL191646 | — | IC50 | = | 21.8 | nM | 7.66 |
| CHEMBL195212 | — | IC50 | = | 23.2 | nM | 7.63 |
| CHEMBL372029 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL195118 | — | IC50 | = | 31.5 | nM | 7.50 |
| CHEMBL195465 | — | IC50 | = | 34.9 | nM | 7.46 |
| CHEMBL192187 | — | IC50 | = | 46.1 | nM | 7.34 |
| CHEMBL426461 | — | IC50 | = | 46.6 | nM | 7.33 |
| CHEMBL427533 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL195216 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL372011 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL192055 | — | IC50 | = | 512.0 | nM | 6.29 |
| CHEMBL83 | TAMOXIFEN | IC50 | = | 622.0 | nM | 6.21 |