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Assay Detail

CHEMBL715966

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

Functional
Antagonist effect in breast tissue was assayed by inhibition of estrogen stimulated MCF-7 cell proliferation
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type MCF-7
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Estrogen receptor (CHEMBL2093866)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Versatile raloxifene triflates
Martin MJ, Grese TA, Glasebrook AL, Matsumoto K, Pennington LD, Phillips D, Short LL
Bioorg Med Chem Lett (1997) 7 : 887 -892
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.23 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81 RALOXIFENE 4.0 1 9.70
CHEMBL43779 1 9.10
CHEMBL297549 1 8.15
CHEMBL170001 1 8.10
CHEMBL46921 1 7.70
CHEMBL47811 1 7.70
CHEMBL169162 1 7.52
CHEMBL416088 1 7.50
CHEMBL355304 1 7.40
CHEMBL170884 1 7.40
CHEMBL170427 1 7.40
CHEMBL297996 1 7.30
CHEMBL47217 1 7.30
CHEMBL297813 1 7.22
CHEMBL45107 1 6.70
CHEMBL416268 1 6.70
CHEMBL297830 1 6.68
CHEMBL295540 1 6.49
CHEMBL83 TAMOXIFEN 4.0 1 6.28
CHEMBL170995 1 6.00
CHEMBL353709 1 6.00
CHEMBL297782 1 6.00
CHEMBL171483 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81 RALOXIFENE IC50 = 0.2 nM 9.70
CHEMBL43779 IC50 = 0.8 nM 9.10
CHEMBL297549 IC50 = 7.0 nM 8.15
CHEMBL170001 IC50 = 8.0 nM 8.10
CHEMBL46921 IC50 = 20.0 nM 7.70
CHEMBL47811 IC50 = 20.0 nM 7.70
CHEMBL169162 IC50 = 30.0 nM 7.52
CHEMBL416088 IC50 = 32.0 nM 7.50
CHEMBL355304 IC50 = 40.0 nM 7.40
CHEMBL170884 IC50 = 40.0 nM 7.40
CHEMBL170427 IC50 = 40.0 nM 7.40
CHEMBL297996 IC50 = 50.0 nM 7.30
CHEMBL47217 IC50 = 50.0 nM 7.30
CHEMBL297813 IC50 = 60.0 nM 7.22
CHEMBL45107 IC50 = 200.0 nM 6.70
CHEMBL416268 IC50 = 200.0 nM 6.70
CHEMBL297830 IC50 = 210.0 nM 6.68
CHEMBL295540 IC50 = 325.0 nM 6.49
CHEMBL83 TAMOXIFEN IC50 = 530.0 nM 6.28
CHEMBL170995 IC50 = 1000.0 nM 6.00
CHEMBL353709 IC50 = 1000.0 nM 6.00
CHEMBL297782 IC50 = 1000.0 nM 6.00
CHEMBL171483 IC50 = 1000.0 nM 6.00