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Assay Detail

CHEMBL4670525

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Binding
Antagonist activity at ER-alpha in human MCF-7:WS8 cells transfected with an estrogen response element assessed as suppression of estrogen-induced response incubated for 18 hrs by luciferase reporter gene assay
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MCF7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors.
Cooper L,Schafer A,Li Y,Cheng H,Medegan Fagla B,Shen Z,Nowar R,Dye K,Anantpadma M,Davey RA,Thatcher GRJ,Rong L,Xiong R
J Med Chem (2020) 63 : 11085 -11099
PubMed 32886512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.73 9.22
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL392916 1 9.22
CHEMBL81 RALOXIFENE 4.0 1 8.23
CHEMBL4754810 1 -
CHEMBL4782391 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL392916 IC50 = 0.6 nM 9.22
CHEMBL81 RALOXIFENE IC50 = 5.9 nM 8.23
CHEMBL4754810 Inhibition - % -
CHEMBL4782391 Inhibition - % -