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Assay Detail

CHEMBL5097761

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

Binding
Inhibition of human recombinant aromatase expressed in baculovirus insect cell using 7-methoxy-trifluoromethyl coumarin (MFC) as substrate preincubated for 10 mins followed by substrate addition and measured for 30 mins by fluorescence based assay
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

Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies.
Arya GC, Kaur K, Jaitak V.
Eur J Med Chem (2021) 221 : 113511 -113511
PubMed 34000484 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.80 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5195433 1 8.64
CHEMBL1444 LETROZOLE 4.0 1 8.55
CHEMBL185 FLUOROURACIL 4.0 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5195433 IC50 = 2.3 nM 8.64
CHEMBL1444 LETROZOLE IC50 = 2.8 nM 8.55
CHEMBL185 FLUOROURACIL IC50 = 630.0 nM 6.20