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Assay Detail

CHEMBL3225086

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

Binding
Inhibition of CYP19 isolated from microsomal fraction of human term placental tissue using [1beta-3H] androstenedione as substrate preincubated for 5 mins followed by enzyme addition measured after 20 mins by beta scintillation counting analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of imidazolylmethylacridones as cytochrome P-450 enzymes inhibitors
Abadi AH, Abou-Seri SM, Hu Q, Negri M, Hartmann RW
Medchemcomm (2012) 3 : 663 -666
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.64 7.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3219070 1 7.84
CHEMBL1444 LETROZOLE 4.0 1 7.44
CHEMBL3219071 1 -
CHEMBL934 METYRAPONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3219070 IC50 = 14.4 nM 7.84
CHEMBL1444 LETROZOLE IC50 = 36.2 nM 7.44
CHEMBL3219071 IC50 - -
CHEMBL934 METYRAPONE IC50 - -