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Assay Detail

CHEMBL4406484

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

Binding
Inhibition of human placental microsome aromatase using [3H]androstenedione as substrate preincubated for 32 mins in presence of NADPH followed by substrate addition and measured after 10 mins
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Characterization of the First Selective and Potent Mechanism-Based Inhibitor of Cytochrome P450 4Z1.
Kowalski JP, McDonald MG, Pelletier RD, Hanenberg H, Wiek C, Rettie AE.
J Med Chem (2020) 63 : 4824 -4836
PubMed 32302132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.58 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1200374 EXEMESTANE 4.0 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1200374 EXEMESTANE Ki = 26.0 nM 7.58