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Assay Detail

CHEMBL932215

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

Binding
Inhibition of human aromatase in placental microsomes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Placenta
Subcellular Microsomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.
Yahiaoui S, Fagnere C, Pouget C, Buxeraud J, Chulia AJ.
Bioorg Med Chem (2008) 16 : 1474 -1480
PubMed 18042388 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.56 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439241 1 6.21
CHEMBL256665 1 6.20
CHEMBL258257 1 5.86
CHEMBL255108 1 5.81
CHEMBL283196 ALPHA-NAPHTHOFLAVONE 1 5.70
CHEMBL252642 LIQUIRTIGENIN 1 5.68
CHEMBL255110 1 5.47
CHEMBL256407 1 5.46
CHEMBL402970 1 5.43
CHEMBL97542 7-HYDROXYFLAVANONE 1 5.42
CHEMBL404225 1 5.37
CHEMBL9687 1 5.10
CHEMBL274318 FLAVANONE 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439241 IC50 = 610.0 nM 6.21
CHEMBL256665 IC50 = 630.0 nM 6.20
CHEMBL258257 IC50 = 1370.0 nM 5.86
CHEMBL255108 IC50 = 1540.0 nM 5.81
CHEMBL283196 ALPHA-NAPHTHOFLAVONE IC50 = 2000.0 nM 5.70
CHEMBL252642 LIQUIRTIGENIN IC50 = 2100.0 nM 5.68
CHEMBL255110 IC50 = 3400.0 nM 5.47
CHEMBL256407 IC50 = 3500.0 nM 5.46
CHEMBL402970 IC50 = 3700.0 nM 5.43
CHEMBL97542 7-HYDROXYFLAVANONE IC50 = 3800.0 nM 5.42
CHEMBL404225 IC50 = 4300.0 nM 5.37
CHEMBL9687 IC50 = 8000.0 nM 5.10
CHEMBL274318 FLAVANONE IC50 = 28000.0 nM 4.55