Assay Detail

CHEMBL4024655

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Functional

Antiproliferative activity against human MCF7 cells after 6 days in presence of estradiol by CellTiter-Glo assay

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 LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.

Tria GS, Abrams T, Baird J, Burks HE, Firestone B, Gaither LA, Hamann LG, He G, Kirby CA, Kim S, Lombardo F, Macchi KJ, McDonnell DP, Mishina Y, Norris JD, Nunez J, Springer C, Sun Y, Thomsen NM, Wang C, Wang J, Yu B, Tiong-Yip CL, Peukert S.
J Med Chem (2018) 61 : 2837 -2864
PubMed 29562737 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	3	8.38	8.77

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4076124	LSZ-102	1.0	1	8.77
CHEMBL1358	FULVESTRANT	4.0	1	8.36
CHEMBL489	AFIMOXIFENE	3.0	1	8.00

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4076124	LSZ-102	IC50	=	1.7	nM	8.77
CHEMBL1358	FULVESTRANT	IC50	=	4.4	nM	8.36
CHEMBL489	AFIMOXIFENE	IC50	=	9.9	nM	8.00