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Assay Detail

CHEMBL1954681

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

Functional
Agonist activity at human ERbeta expressed in HEC-1 cells coexpressing beta-gal assessed as luciferase activity after 24 hrs by reporter gene assay
4
Total Activities
4
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 beta (CHEMBL242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Diarylpropionitrile (DPN) enantiomers: synthesis and evaluation of estrogen receptor β-selective ligands.
Carroll VM, Jeyakumar M, Carlson KE, Katzenellenbogen JA.
J Med Chem (2012) 55 : 528 -537
PubMed 22122563 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 8.80 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 9.70
CHEMBL1950809 1 8.52
CHEMBL198159 1 8.49
CHEMBL334773 DIARYLPROPIONITRILE 1 8.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL EC50 = 0.2 nM 9.70
CHEMBL1950809 EC50 = 3.0 nM 8.52
CHEMBL198159 EC50 = 3.2 nM 8.49
CHEMBL334773 DIARYLPROPIONITRILE EC50 = 3.3 nM 8.48