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Assay Detail

CHEMBL3627341

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

Binding
Inhibition of aromatase (unknown origin) expressed in JEG-3 cells
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type JEG-3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health.
Thomas MP, Potter BV.
J Med Chem (2015) 58 : 7634 -7658
PubMed 25992880 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.54 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL592131 1 9.92
CHEMBL597808 1 9.82
CHEMBL3622064 1 9.60
CHEMBL3622055 1 9.59
CHEMBL3622054 1 9.55
CHEMBL3622056 1 9.38
CHEMBL3622057 1 9.35
CHEMBL3622058 1 9.29
CHEMBL3622059 1 9.14
CHEMBL1444 LETROZOLE 4.0 1 9.05
CHEMBL3622063 1 8.68
CHEMBL3622066 1 8.64
CHEMBL3622065 1 8.57
CHEMBL518761 1 8.52
CHEMBL479559 1 8.49
CHEMBL3622067 1 8.40
CHEMBL3622061 1 8.28
CHEMBL480321 1 7.84
CHEMBL3622060 1 7.82
CHEMBL224060 VOROZOLE 2.0 1 7.54
CHEMBL3622363 1 7.54
CHEMBL3622062 1 7.51
CHEMBL430879 1 7.00
CHEMBL479942 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL592131 IC50 = 0.12 nM 9.92
CHEMBL597808 IC50 = 0.15 nM 9.82
CHEMBL3622064 IC50 = 0.25 nM 9.60
CHEMBL3622055 IC50 = 0.26 nM 9.59
CHEMBL3622054 IC50 = 0.28 nM 9.55
CHEMBL3622056 IC50 = 0.42 nM 9.38
CHEMBL3622057 IC50 = 0.45 nM 9.35
CHEMBL3622058 IC50 = 0.51 nM 9.29
CHEMBL3622059 IC50 = 0.73 nM 9.14
CHEMBL1444 LETROZOLE IC50 = 0.89 nM 9.05
CHEMBL3622063 IC50 = 2.1 nM 8.68
CHEMBL3622066 IC50 = 2.3 nM 8.64
CHEMBL3622065 IC50 = 2.7 nM 8.57
CHEMBL518761 IC50 = 3.0 nM 8.52
CHEMBL479559 IC50 = 3.2 nM 8.49
CHEMBL3622067 IC50 = 4.0 nM 8.40
CHEMBL3622061 IC50 = 5.2 nM 8.28
CHEMBL480321 IC50 = 14.3 nM 7.84
CHEMBL3622060 IC50 = 15.0 nM 7.82
CHEMBL224060 VOROZOLE IC50 = 29.0 nM 7.54
CHEMBL3622363 IC50 = 29.0 nM 7.54
CHEMBL3622062 IC50 = 31.0 nM 7.51
CHEMBL430879 IC50 = 100.0 nM 7.00
CHEMBL479942 IC50 = 3044.0 nM 5.52