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Assay Detail

CHEMBL3820547

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

Binding
Inhibition of human placental microsomal aromatase using testosterone as substrate assessed as formation of estradiol after 10 mins
3
Total Activities
3
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 3 6.37 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2386284 1 7.52
CHEMBL1093458 ENDOXIFEN 3.0 1 5.22
CHEMBL489 AFIMOXIFENE 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2386284 IC50 = 30.0 nM 7.52
CHEMBL1093458 ENDOXIFEN IC50 = 6000.0 nM 5.22
CHEMBL489 AFIMOXIFENE IC50 = 530000.0 nM -