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

CHEMBL1954673

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

Binding
Agonist activity at human N-His6-tagged terbium-labelled NRID-SRC3 of ERalpha ligand binding domain expressed in Escherichia coli BL21 cells after 1 hr by TR-FRET assay
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BL21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estrogen receptor (CHEMBL206)
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 8.62 9.25
Activity 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 2 9.25
CHEMBL198159 2 8.54
CHEMBL334773 DIARYLPROPIONITRILE 2 8.47
CHEMBL1950809 2 8.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL EC50 = 0.56 nM 9.25
CHEMBL198159 EC50 = 2.9 nM 8.54
CHEMBL334773 DIARYLPROPIONITRILE EC50 = 3.4 nM 8.47
CHEMBL1950809 EC50 = 6.2 nM 8.21
CHEMBL334773 DIARYLPROPIONITRILE Activity - -
CHEMBL135 ESTRADIOL Activity - -
CHEMBL198159 Activity - -
CHEMBL1950809 Activity - -