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Assay Detail

CHEMBL832321

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

Binding
In vitro inhibition of [1,2,6,7-3H]androstenedione binding to Aromatase of human placental microsomes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors.
Yahiaoui S, Pouget C, Fagnere C, Champavier Y, Habrioux G, Chulia AJ.
Bioorg Med Chem Lett (2004) 14 : 5215 -5218
PubMed 15380230 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.23 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95919 1 7.40
CHEMBL95109 1 7.05
CHEMBL187185 1 6.37
CHEMBL185165 1 5.85
CHEMBL184952 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95919 IC50 = 40.0 nM 7.40
CHEMBL95109 IC50 = 90.0 nM 7.05
CHEMBL187185 IC50 = 430.0 nM 6.37
CHEMBL185165 IC50 = 1400.0 nM 5.85
CHEMBL184952 IC50 = 31600.0 nM 4.50