Assay Detail
Binding
CHEMBL5733230
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Breast Cancer Cell Viability Assay: MCF-7 cells were adjusted to a concentration of 40,000 cells per mL in RPMI containing 10% FBS and 20 mM HEPES. 16 microliters of the cell suspension (640 cells) was added to each well of a 384 well plate, and the cells were incubated overnight to allow the cells to adhere. The following day a 10 point, serial 1:5 dilution of each compound was added to the cells in 16 μL at a final concentration ranging from 10-0.000005 μM. After 5 days' compound exposure, 16 μL of CellTiter-GLo (Promega, Madison Wis.) was added to the cells, and the relative luminescence units (RLUs) of each well were determined. CellTiter-Glo added to 32 μL of medium without cells was used to obtain a background value. The Percent viability of each sample was determined as follows: (RLU sample−RLU background/RLU untreated cells−RLU background)×100=% viability. % Viability relative to Fulvestrant is calculated as follows: 100−{100*[(100−% viability of Example)/(100−% viability of Fulvestrant)]}.
24
Total Activities
8
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Estrogen receptor modulators and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.47 | 10.15 |
| kon | 8 | - | - |
| k_off | 8 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447340 | — | — | 3 | 10.15 |
| CHEMBL4164133 | — | — | 3 | 9.89 |
| CHEMBL4524752 | — | — | 3 | 9.68 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 3 | 9.24 |
| CHEMBL4452393 | — | — | 3 | 8.37 |
| CHEMBL4159755 | — | — | 3 | 7.00 |
| CHEMBL4165523 | — | — | 3 | 6.70 |
| CHEMBL5969381 | — | — | 3 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447340 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL4164133 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL4524752 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL1358 | FULVESTRANT | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL4452393 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4159755 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4165523 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5969381 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4524752 | — | kon | = | - | — | - |
| CHEMBL4524752 | — | k_off | = | - | s-1 | - |
| CHEMBL4452393 | — | kon | = | - | — | - |
| CHEMBL4452393 | — | k_off | = | - | s-1 | - |
| CHEMBL4447340 | — | kon | = | - | — | - |
| CHEMBL4447340 | — | k_off | = | - | s-1 | - |
| CHEMBL4165523 | — | kon | = | - | — | - |
| CHEMBL4165523 | — | k_off | = | - | s-1 | - |
| CHEMBL5969381 | — | kon | = | - | — | - |
| CHEMBL5969381 | — | k_off | = | - | s-1 | - |
| CHEMBL4159755 | — | kon | = | - | — | - |
| CHEMBL4159755 | — | k_off | = | - | s-1 | - |
| CHEMBL4164133 | — | kon | = | - | — | - |
| CHEMBL4164133 | — | k_off | = | - | s-1 | - |
| CHEMBL1358 | FULVESTRANT | kon | = | - | — | - |
| CHEMBL1358 | FULVESTRANT | k_off | = | - | s-1 | - |