Assay Detail

CHEMBL4429356

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Binding

Downregulation of ER-alpha expression in human tamoxifen-resistant T47D cells over-expressing PKC-alpha measured after 5 days by Western blot analysis

ChEMBL ↗

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Target

Estrogen receptor (CHEMBL206) ↗

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Primary target Estrogen receptor

CHEMBL206

Anchored from Assay target.

Protein identity Estrogen receptor

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Cell Type	T47D
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Estrogen receptor (CHEMBL206) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD).

Liu J, Zheng S, Akerstrom VL, Yuan C, Ma Y, Zhong Q, Zhang C, Zhang Q, Guo S, Ma P, Skripnikova EV, Bratton MR, Pannuti A, Miele L, Wiese TE, Wang G.
J Med Chem (2016) 59 : 8134 -8140
PubMed 27529700 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Inhibition	2	-	-
IC50	2	7.99	8.07

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1358	FULVESTRANT	4.0	2	8.07
CHEMBL4526356	ZB-716	1.0	2	7.90

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1358	FULVESTRANT	IC50	=	8.5	nM	8.07
CHEMBL4526356	ZB-716	IC50	=	12.7	nM	7.90
CHEMBL1358	FULVESTRANT	Inhibition		-	%	-
CHEMBL4526356	ZB-716	Inhibition		-	%	-