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Assay Detail

CHEMBL663244

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

Binding
In vitro inhibition of cytochrome P450 19A1
13
Total Activities
12
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

Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.
Browne LJ, Gude C, Rodriguez H, Steele RE, Bhatnager A.
J Med Chem (1991) 34 : 725 -736
PubMed 1825337 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.88 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1203762 1 8.70
CHEMBL9298 FADROZOLE 2.0 2 8.34
CHEMBL468419 FADROZOLE HYDROCHLORIDE -1.0 1 8.19
CHEMBL1203766 1 8.12
CHEMBL162834 1 7.85
CHEMBL348913 1 7.84
CHEMBL349822 1 7.82
CHEMBL162496 1 7.82
CHEMBL1203757 1 7.75
CHEMBL1203760 1 7.68
CHEMBL163420 1 7.03
CHEMBL163413 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1203762 IC50 = 2.0 nM 8.70
CHEMBL9298 FADROZOLE IC50 = 4.6 nM 8.34
CHEMBL468419 FADROZOLE HYDROCHLORIDE IC50 = 6.4 nM 8.19
CHEMBL1203766 IC50 = 7.6 nM 8.12
CHEMBL162834 IC50 = 14.1 nM 7.85
CHEMBL348913 IC50 = 14.3 nM 7.84
CHEMBL349822 IC50 = 15.0 nM 7.82
CHEMBL162496 IC50 = 15.0 nM 7.82
CHEMBL1203757 IC50 = 17.6 nM 7.75
CHEMBL1203760 IC50 = 21.0 nM 7.68
CHEMBL9298 FADROZOLE IC50 = 39.0 nM 7.41
CHEMBL163420 IC50 = 92.9 nM 7.03
CHEMBL163413 IC50 > 1000.0 nM -