Assay Detail
Binding
CHEMBL832383
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 beta; 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 | 6.57 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL328190 | LASOFOXIFENE | 4.0 | 1 | 7.62 |
| CHEMBL195212 | — | — | 1 | 7.01 |
| CHEMBL195465 | — | — | 1 | 6.97 |
| CHEMBL192187 | — | — | 1 | 6.79 |
| CHEMBL427533 | — | — | 1 | 6.75 |
| CHEMBL195466 | — | — | 1 | 6.57 |
| CHEMBL191646 | — | — | 1 | 6.56 |
| CHEMBL364492 | — | — | 1 | 6.54 |
| CHEMBL101382 | — | — | 1 | 6.54 |
| CHEMBL194334 | — | — | 1 | 6.54 |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 6.47 |
| CHEMBL195216 | — | — | 1 | 6.40 |
| CHEMBL426461 | — | — | 1 | 6.33 |
| CHEMBL195118 | — | — | 1 | 6.31 |
| CHEMBL372029 | — | — | 1 | 6.30 |
| CHEMBL192055 | — | — | 1 | 5.35 |
| CHEMBL372011 | — | — | 1 | - |
| CHEMBL83 | TAMOXIFEN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL328190 | LASOFOXIFENE | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL195212 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL195465 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL192187 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL427533 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL195466 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL191646 | — | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL364492 | — | IC50 | = | 286.0 | nM | 6.54 |
| CHEMBL101382 | — | IC50 | = | 289.0 | nM | 6.54 |
| CHEMBL194334 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 341.0 | nM | 6.47 |
| CHEMBL195216 | — | IC50 | = | 399.0 | nM | 6.40 |
| CHEMBL426461 | — | IC50 | = | 464.0 | nM | 6.33 |
| CHEMBL195118 | — | IC50 | = | 491.0 | nM | 6.31 |
| CHEMBL372029 | — | IC50 | = | 496.0 | nM | 6.30 |
| CHEMBL192055 | — | IC50 | = | 4454.0 | nM | 5.35 |
| CHEMBL372011 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL83 | TAMOXIFEN | IC50 | > | 1000.0 | nM | - |