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Assay Detail

CHEMBL709825

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

Functional
In vitro inhibition of estrogen-stimulated MCF-7 cell proliferation
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF-7
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Estrogen receptor (CHEMBL2093866)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Novel nonsteroidal selective estrogen receptor modulators. Carbon and heteroatom replacement of oxygen in the ethoxypiperidine region of raloxifene.
Schmid CR, Sluka JP, Duke KM, Glasebrook AW.
Bioorg Med Chem Lett (1999) 9 : 523 -528
PubMed 10098655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.50 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 11.00
CHEMBL81 RALOXIFENE 4.0 1 9.70
CHEMBL150735 1 9.05
CHEMBL150492 1 8.70
CHEMBL150970 1 8.00
CHEMBL151318 1 8.00
CHEMBL423035 1 7.52
CHEMBL151400 1 6.00
CHEMBL146765 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL IC50 = 0.01 nM 11.00
CHEMBL81 RALOXIFENE IC50 = 0.2 nM 9.70
CHEMBL150735 IC50 = 0.9 nM 9.05
CHEMBL150492 IC50 = 2.0 nM 8.70
CHEMBL150970 IC50 = 10.0 nM 8.00
CHEMBL151318 IC50 = 10.0 nM 8.00
CHEMBL423035 IC50 = 30.0 nM 7.52
CHEMBL151400 IC50 = 1000.0 nM 6.00
CHEMBL146765 IC50 > 1000.0 nM -