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Assay Detail

CHEMBL1010834

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Functional
Antagonist activity at human ERalpha receptor expressed in HEC1 cells assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEC-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Analogs of methyl-piperidinopyrazole (MPP): antiestrogens with estrogen receptor alpha selective activity.
Zhou HB, Carlson KE, Stossi F, Katzenellenbogen BS, Katzenellenbogen JA.
Bioorg Med Chem Lett (2009) 19 : 108 -110
PubMed 19014882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.93 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL481189 1 7.70
CHEMBL520107 1 7.10
CHEMBL519599 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL481189 IC50 = 20.0 nM 7.70
CHEMBL520107 IC50 = 80.0 nM 7.10
CHEMBL519599 IC50 = 1000.0 nM 6.00