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Assay Detail

CHEMBL5733230

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
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

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Estrogen receptor modulators and uses thereof
(2019)

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 -