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Assay Detail

CHEMBL2330132

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

Binding
Antagonist activity at ERalpha receptor in human MCF7 cells assessed as inhibition of cell growth after 6 days by crystal violet staining method
10
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MCF7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Steroid hormone receptor ERR1 (CHEMBL3429)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of novel estrogen receptor antagonists using metal-catalyzed coupling reactions and characterization of their biological activity.
Jiang XR, Wang P, Smith CL, Zhu BT.
J Med Chem (2013) 56 : 2779 -2790
PubMed 23448346 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.38 8.70
Inhibition 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1358 FULVESTRANT 4.0 1 8.70
CHEMBL2326068 2 7.30
CHEMBL2326075 2 7.30
CHEMBL2326074 2 7.30
CHEMBL2326070 2 7.00
CHEMBL83 TAMOXIFEN 4.0 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1358 FULVESTRANT IC50 = 2.0 nM 8.70
CHEMBL2326068 IC50 = 50.0 nM 7.30
CHEMBL2326075 IC50 = 50.0 nM 7.30
CHEMBL2326074 IC50 = 50.0 nM 7.30
CHEMBL2326070 IC50 = 100.0 nM 7.00
CHEMBL83 TAMOXIFEN IC50 = 200.0 nM 6.70
CHEMBL2326068 Inhibition - % -
CHEMBL2326070 Inhibition - % -
CHEMBL2326075 Inhibition - % -
CHEMBL2326074 Inhibition - % -