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Assay Detail

CHEMBL1958525

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

Binding
Inhibition of human aromatase coexpressed with P450 reductase by fluorimetry
10
Total Activities
10
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

New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series.
Stauffer F, Furet P, Floersheimer A, Lang M.
Bioorg Med Chem Lett (2012) 22 : 1860 -1863
PubMed 22335894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.75 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1444 LETROZOLE 4.0 1 9.00
CHEMBL1956186 1 7.23
CHEMBL1955869 1 7.03
CHEMBL1956188 1 6.94
CHEMBL1956180 1 6.64
CHEMBL1956171 1 6.54
CHEMBL1956179 1 6.52
CHEMBL1956183 1 6.28
CHEMBL1956175 1 6.01
CHEMBL1728910 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1444 LETROZOLE IC50 = 1.0 nM 9.00
CHEMBL1956186 IC50 = 59.0 nM 7.23
CHEMBL1955869 IC50 = 93.0 nM 7.03
CHEMBL1956188 IC50 = 114.0 nM 6.94
CHEMBL1956180 IC50 = 229.0 nM 6.64
CHEMBL1956171 IC50 = 289.0 nM 6.54
CHEMBL1956179 IC50 = 304.0 nM 6.52
CHEMBL1956183 IC50 = 523.0 nM 6.28
CHEMBL1956175 IC50 = 986.0 nM 6.01
CHEMBL1728910 IC50 = 5030.0 nM 5.30