Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3861278

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

Binding
Inhibition of recombinant human microsomal CYP19 using MFC as substrate measured after 30 mins by fluorometric analysis
14
Total Activities
14
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

A new Suzuki synthesis of triphenylethylenes that inhibit aromatase and bind to estrogen receptors α and β.
Zhao LM, Jin HS, Liu J, Skaar TC, Ipe J, Lv W, Flockhart DA, Cushman M.
Bioorg Med Chem (2016) 24 : 5400 -5409
PubMed 27647367 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.48 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3948254 1 8.06
CHEMBL3944017 1 7.87
CHEMBL3905734 1 7.21
CHEMBL2386285 1 7.12
CHEMBL3350384 1 6.99
CHEMBL3916057 1 6.75
CHEMBL3984531 1 6.66
CHEMBL3977491 1 6.64
CHEMBL3961452 1 6.54
CHEMBL3961033 1 6.19
CHEMBL2386284 1 5.99
CHEMBL3942918 1 5.03
CHEMBL3925065 1 5.01
CHEMBL149791 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3948254 IC50 = 8.8 nM 8.06
CHEMBL3944017 IC50 = 13.4 nM 7.87
CHEMBL3905734 IC50 = 62.2 nM 7.21
CHEMBL2386285 IC50 = 76.8 nM 7.12
CHEMBL3350384 IC50 = 102.2 nM 6.99
CHEMBL3916057 IC50 = 177.1 nM 6.75
CHEMBL3984531 IC50 = 220.8 nM 6.66
CHEMBL3977491 IC50 = 230.0 nM 6.64
CHEMBL3961452 IC50 = 286.9 nM 6.54
CHEMBL3961033 IC50 = 645.3 nM 6.19
CHEMBL2386284 IC50 = 1029.0 nM 5.99
CHEMBL3942918 IC50 = 9257.0 nM 5.03
CHEMBL3925065 IC50 = 9724.0 nM 5.01
CHEMBL149791 IC50 = 24880.0 nM 4.60