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Assay Detail

CHEMBL2014374

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

Binding
Inhibition of aromatase
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of a new class of aromatase inhibitors: design, synthesis and inhibitory activity of 3-phenylchroman-4-one (isoflavanone) derivatives.
Bonfield K, Amato E, Bankemper T, Agard H, Steller J, Keeler JM, Roy D, McCallum A, Paula S, Ma L.
Bioorg Med Chem (2012) 20 : 2603 -2613
PubMed 22444875 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.87 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1399 ANASTROZOLE 4.0 1 7.92
CHEMBL117 CHRYSIN 1 5.82
CHEMBL131921 BIOCHANIN 1 -
CHEMBL2011191 1 -
CHEMBL2011192 1 -
CHEMBL2011193 1 -
CHEMBL274826 ANDROSTENEDIONE -1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1399 ANASTROZOLE IC50 = 12.0 nM 7.92
CHEMBL117 CHRYSIN IC50 = 1500.0 nM 5.82
CHEMBL131921 BIOCHANIN IC50 = 113000.0 nM -
CHEMBL2011191 IC50 = 170000.0 nM -
CHEMBL2011192 IC50 = 160000.0 nM -
CHEMBL2011193 IC50 >= 200000.0 nM -
CHEMBL274826 ANDROSTENEDIONE IC50 >= 260.0 nM -