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Assay Detail

CHEMBL3591305

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

Binding
Antagonist activity at ER-alpha (unknown origin) transfected in HEK293T cells assessed as inhibition of transcriptional activity after 24 hrs by luciferase reporter gene assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer.
Tang C, Li C, Zhang S, Hu Z, Wu J, Dong C, Huang J, Zhou HB.
J Med Chem (2015) 58 : 4550 -4572
PubMed 25993269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.38 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3589346 1 7.85
CHEMBL3589349 1 7.30
CHEMBL3589367 1 6.89
CHEMBL3589361 1 6.85
CHEMBL3589701 1 6.80
CHEMBL3589356 1 6.34
CHEMBL3589365 1 6.19
CHEMBL3589364 1 6.10
CHEMBL3589368 1 6.04
CHEMBL3589352 1 5.97
CHEMBL3588865 1 5.92
CHEMBL3589363 1 5.77
CHEMBL3589347 1 4.97
CHEMBL3589354 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3589346 IC50 = 14.0 nM 7.85
CHEMBL3589349 IC50 = 50.0 nM 7.30
CHEMBL3589367 IC50 = 130.0 nM 6.89
CHEMBL3589361 IC50 = 140.0 nM 6.85
CHEMBL3589701 IC50 = 160.0 nM 6.80
CHEMBL3589356 IC50 = 460.0 nM 6.34
CHEMBL3589365 IC50 = 640.0 nM 6.19
CHEMBL3589364 IC50 = 790.0 nM 6.10
CHEMBL3589368 IC50 = 920.0 nM 6.04
CHEMBL3589352 IC50 = 1080.0 nM 5.97
CHEMBL3588865 IC50 = 1210.0 nM 5.92
CHEMBL3589363 IC50 = 1700.0 nM 5.77
CHEMBL3589347 IC50 = 10800.0 nM 4.97
CHEMBL3589354 IC50 = 115600.0 nM -