Assay Detail

CHEMBL3625856

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Binding

Antagonist activity at ERalpha receptor in human MCF7 cells in presence of 0.25 uM tamoxifen

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	MCF7
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Estrogen receptor (CHEMBL206) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.

De Savi C, Bradbury RH, Rabow AA, Norman RA, de Almeida C, Andrews DM, Ballard P, Buttar D, Callis RJ, Currie GS, Curwen JO, Davies CD, Donald CS, Feron LJ, Gingell H, Glossop SC, Hayter BR, Hussain S, Karoutchi G, Lamont SG, MacFaul P, Moss TA, Pearson SE, Tonge M, Walker GE, Weir HM, Wilson Z.
J Med Chem (2015) 58 : 8128 -8140
PubMed 26407012 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	9.68	9.68

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3623004	AZD-9496	1.0	1	9.68

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3623004	AZD-9496	IC50	=	0.2089	nM	9.68