Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4013740

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

Binding
Downregulation of human ERalpha in human MCF-7 cells after 24 hrs by in-cell Western immunoassay method
12
Total Activities
12
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

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Adamantyl Antiestrogens with Novel Side Chains Reveal a Spectrum of Activities in Suppressing Estrogen Receptor Mediated Activities in Breast Cancer Cells.
Min J, Guillen VS, Sharma A, Zhao Y, Ziegler Y, Gong P, Mayne CG, Srinivasan S, Kim SH, Carlson KE, Nettles KW, Katzenellenbogen BS, Katzenellenbogen JA.
J Med Chem (2017) 60 : 6321 -6336
PubMed 28657320 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.39 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1358 FULVESTRANT 4.0 1 9.52
CHEMBL4078577 1 9.28
CHEMBL4065838 1 8.68
CHEMBL4070669 1 8.54
CHEMBL4102857 1 8.37
CHEMBL4099302 1 8.27
CHEMBL4060067 1 8.25
CHEMBL4098470 1 8.04
CHEMBL4073395 1 8.00
CHEMBL4100247 1 8.00
CHEMBL4062045 1 7.92
CHEMBL4083658 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1358 FULVESTRANT IC50 = 0.3 nM 9.52
CHEMBL4078577 IC50 = 0.53 nM 9.28
CHEMBL4065838 IC50 = 2.1 nM 8.68
CHEMBL4070669 IC50 = 2.9 nM 8.54
CHEMBL4102857 IC50 = 4.3 nM 8.37
CHEMBL4099302 IC50 = 5.4 nM 8.27
CHEMBL4060067 IC50 = 5.6 nM 8.25
CHEMBL4098470 IC50 = 9.1 nM 8.04
CHEMBL4073395 IC50 = 10.0 nM 8.00
CHEMBL4100247 IC50 = 10.0 nM 8.00
CHEMBL4062045 IC50 = 12.0 nM 7.92
CHEMBL4083658 IC50 = 17.0 nM 7.77