Assay Detail

CHEMBL4619355

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Binding

Induction of ERalpha degradation in human T47D cells

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

Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.

Liang J, Blake R, Chang J, Friedman LS, Goodacre S, Hartman S, Ingalla ER, Kiefer JR, Kleinheinz T, Labadie S, Li J, Lai KW, Liao J, Mody V, McLean N, Metcalfe C, Nannini M, Otwine D, Ran Y, Ray N, Roussel F, Sambrone A, Sampath D, Vinogradova M, Wai J, Wang T, Yeap K, Young A, Zbieg J, Zhang B, Zheng X, Zhong Y, Wang X.
ACS Med Chem Lett (2020) 11 : 1342 -1347
PubMed 32551022 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	4	9.45	10.51

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4649161	—	—	1	10.51
CHEMBL4447340	—	—	1	9.42
CHEMBL1358	FULVESTRANT	4.0	1	9.08
CHEMBL3581693	BRILANESTRANT	2.0	1	8.77

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4649161	—	IC50	=	0.031	nM	10.51
CHEMBL4447340	—	IC50	=	0.38	nM	9.42
CHEMBL1358	FULVESTRANT	IC50	=	0.84	nM	9.08
CHEMBL3581693	BRILANESTRANT	IC50	=	1.7	nM	8.77