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Assay Detail

CHEMBL4013746

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

Binding
Downregulation of ERalpha in human MCF-7 cells assessed as reduction of estradiol-induced pS2 mRNA levels after 24 hrs by RT-PCR method
2
Total Activities
2
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 2 6.80 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4078577 1 7.30
CHEMBL4083658 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4078577 IC50 = 50.0 nM 7.30
CHEMBL4083658 IC50 = 500.0 nM 6.30