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Assay Detail

CHEMBL856242

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

Functional
Half maximal inhibitory concentration against estrogen-induced proliferation of MCF-7 breast cells by 10 pM E2
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF7
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Estrogen receptor (CHEMBL2093866)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats.
Hummel CW, Geiser AG, Bryant HU, Cohen IR, Dally RD, Fong KC, Frank SA, Hinklin R, Jones SA, Lewis G, McCann DJ, Rudmann DG, Shepherd TA, Tian H, Wallace OB, Wang M, Wang Y, Dodge JA.
J Med Chem (2005) 48 : 6772 -6775
PubMed 16250633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 9.23 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL539849 1 9.70
CHEMBL537638 1 9.47
CHEMBL1116 RALOXIFENE HYDROCHLORIDE 4.0 1 9.43
CHEMBL536733 1 9.07
CHEMBL557981 1 8.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL539849 IC50 = 0.2 nM 9.70
CHEMBL537638 IC50 = 0.34 nM 9.47
CHEMBL1116 RALOXIFENE HYDROCHLORIDE IC50 = 0.37 nM 9.43
CHEMBL536733 IC50 = 0.86 nM 9.07
CHEMBL557981 IC50 = 3.4 nM 8.47