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Assay Detail

CHEMBL3819974

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

Binding
Inhibition of human placental microsomal aromatase using [1beta-3H] androstenedione as substrate assessed as tritiated H2O release preincubated for 5 mins followed by protein addition measured after 20 mins by beta counting method
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

Recent Progress in the Discovery of Next Generation Inhibitors of Aromatase from the Structure-Function Perspective.
Ghosh D, Lo J, Egbuta C.
J Med Chem (2016) 59 : 5131 -5148
PubMed 26689671 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.45 6.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3818725 1 6.78
CHEMBL3819184 1 6.75
CHEMBL3818442 1 6.29
CHEMBL3623216 1 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3818725 IC50 = 168.0 nM 6.78
CHEMBL3819184 IC50 = 180.0 nM 6.75
CHEMBL3818442 IC50 = 512.0 nM 6.29
CHEMBL3623216 IC50 = 1019.8 nM 5.99