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Assay Detail

CHEMBL715113

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

MCF7 (CHEMBL387)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery and synthesis of [6-hydroxy-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]-2-(4-hydroxyphenyl)]b enzo[b]thiophene: a novel, highly potent, selective estrogen receptor modulator.
Palkowitz AD, Glasebrook AL, Thrasher KJ, Hauser KL, Short LL, Phillips DL, Muehl BS, Sato M, Shetler PK, Cullinan GJ, Pell TR, Bryant HU.
J Med Chem (1997) 40 : 1407 -1416
PubMed 9154963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 9.19 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL537254 1 10.30
CHEMBL552569 1 10.00
CHEMBL540775 1 9.72
CHEMBL542329 1 9.55
CHEMBL1116 RALOXIFENE HYDROCHLORIDE 4.0 1 9.40
CHEMBL1358 FULVESTRANT 4.0 1 9.31
CHEMBL2137046 1 8.93
CHEMBL83 TAMOXIFEN 4.0 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL537254 IC50 = 0.05 nM 10.30
CHEMBL552569 IC50 = 0.1 nM 10.00
CHEMBL540775 IC50 = 0.19 nM 9.72
CHEMBL542329 IC50 = 0.28 nM 9.55
CHEMBL1116 RALOXIFENE HYDROCHLORIDE IC50 = 0.4 nM 9.40
CHEMBL1358 FULVESTRANT IC50 = 0.49 nM 9.31
CHEMBL2137046 IC50 = 1.17 nM 8.93
CHEMBL83 TAMOXIFEN IC50 = 481.0 nM 6.32