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Assay Detail

CHEMBL3414093

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

Binding
Inhibition of human placental microsome aromatase expressed in human MCF7 cells using [1beta-3H] androstenedione as substrate after 1 hr by liquid scintillation counting
5
Total Activities
5
Compounds Tested
1
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

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exemestane metabolites: Synthesis, stereochemical elucidation, biochemical activity and anti-proliferative effects in a hormone-dependent breast cancer cell line.
Varela CL, Amaral C, Tavares da Silva E, Lopes A, Correia-da-Silva G, Carvalho RA, Costa SC, Roleira FM, Teixeira N.
Eur J Med Chem (2014) 87 : 336 -345
PubMed 25277066 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.15 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3407538 1 6.60
CHEMBL3407536 1 6.14
CHEMBL1200374 EXEMESTANE 4.0 1 6.05
CHEMBL3407539 1 6.01
CHEMBL3407537 1 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3407538 IC50 = 250.0 nM 6.60
CHEMBL3407536 IC50 = 730.0 nM 6.14
CHEMBL1200374 EXEMESTANE IC50 = 900.0 nM 6.05
CHEMBL3407539 IC50 = 980.0 nM 6.01
CHEMBL3407537 IC50 = 1180.0 nM 5.93