Assay Detail

CHEMBL5381633

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Functional

Antiproliferative activity against human MCF7 cells harbouring Y537S mutant assessed as reduction in cell growth incubated for 6 days

ChEMBL ↗

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Target

MCF7 (CHEMBL387) ↗

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Primary target MCF7

CHEMBL387

Anchored from Assay target.

Protein identity MCF7

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	Functional
Organism	Homo sapiens
Cell Type	MCF7
Confidence	1 — Organism
Curated By	Autocuration

Target

MCF7 (CHEMBL387) ↗

Type	CELL-LINE
Organism	Homo sapiens

Publication

Discovery of a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists.

Scott JS, Stead D, Barlaam B, Breed J, Carbajo RJ, Chiarparin E, Cureton N, Davey PRJ, Fisher DI, Gangl ET, Grebe T, Greenwood RD, Hande S, Hatoum-Mokdad H, Hughes SJ, Hunt TA, Johnson T, Kavanagh SL, Klinowska TCM, Larner CJB, Lawson M, Lister AS, Longmire D, Marden S, McGuire TM, McMillan C, McMurray L, Morrow CJ, Nissink JWM, Moss TA, O'Donovan DH, Polanski R, Stokes S, Thakur K, Trueman D, Truman C, Tucker MJ, Wang H, Whalley N, Wu D, Wu Y, Yang B, Yang W.
J Med Chem (2023) 66 : 2918 -2945
PubMed 36727211 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.40	7.40

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL5426983	—	—	1	7.40

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL5426983	—	IC50	=	39.81	nM	7.40