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Assay Detail

CHEMBL2388440

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

Binding
Inhibition of human recombinant placental aromatase
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 of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities.
Lv W, Liu J, Lu D, Flockhart DA, Cushman M.
J Med Chem (2013) 56 : 4611 -4618
PubMed 23731360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.44 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2386285 1 7.05
CHEMBL3350384 1 7.05
CHEMBL1093458 ENDOXIFEN 3.0 1 5.22
CHEMBL2137046 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2386285 IC50 = 90.0 nM 7.05
CHEMBL3350384 IC50 = 90.0 nM 7.05
CHEMBL1093458 ENDOXIFEN IC50 = 6000.0 nM 5.22
CHEMBL2137046 IC50 = 530000.0 nM -