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Assay Detail

CHEMBL666797

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

Binding
In vitro inhibition of [1,2,6,7-3H]-androstenedione binding to human placental microsome cytochrome P450 19A1
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New aromatase inhibitors. Synthesis and inhibitory activity of pyridinyl-substituted flavanone derivatives.
Pouget C, Fagnere C, Basly JP, Habrioux G, Chulia AJ.
Bioorg Med Chem Lett (2002) 12 : 1059 -1061
PubMed 11909717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.50 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10137 1 6.21
CHEMBL10026 1 6.10
CHEMBL267508 1 5.80
CHEMBL10072 1 5.48
CHEMBL488 AMINOGLUTETHIMIDE 4.0 1 5.28
CHEMBL9687 1 5.10
CHEMBL274318 FLAVANONE 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10137 IC50 = 620.0 nM 6.21
CHEMBL10026 IC50 = 800.0 nM 6.10
CHEMBL267508 IC50 = 1600.0 nM 5.80
CHEMBL10072 IC50 = 3300.0 nM 5.48
CHEMBL488 AMINOGLUTETHIMIDE IC50 = 5200.0 nM 5.28
CHEMBL9687 IC50 = 8000.0 nM 5.10
CHEMBL274318 FLAVANONE IC50 = 28500.0 nM 4.54