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Assay Detail

CHEMBL905158

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

Binding
Inhibition of human aromatase
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of (+/-)-abyssinone II and its analogues as aromatase inhibitors for chemoprevention of breast cancer.
Maiti A, Cuendet M, Croy VL, Endringer DC, Pezzuto JM, Cushman M.
J Med Chem (2007) 50 : 2799 -2806
PubMed 17511439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.04 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL488 AMINOGLUTETHIMIDE 4.0 1 6.57
CHEMBL229908 LIQUIRITIGENIN DIMETHYL ETHER 1 5.73
CHEMBL229635 1 5.43
CHEMBL229789 1 5.39
CHEMBL229906 1 5.33
CHEMBL388374 1 5.32
CHEMBL425670 1 5.12
CHEMBL1162951 1 4.92
CHEMBL229945 1 4.86
CHEMBL229790 1 4.60
CHEMBL228985 1 4.54
CHEMBL558103 ABYSSINONE II 1 4.39
CHEMBL229094 1 4.26
CHEMBL389925 1 4.08
CHEMBL390731 1 -
CHEMBL229885 LICOAGROCHALCONE A 1 -
CHEMBL229893 1 -
CHEMBL229907 1 -
CHEMBL229841 1 -
CHEMBL229944 1 -
CHEMBL229633 1 -
CHEMBL390364 1 -
CHEMBL388375 1 -
CHEMBL229905 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL488 AMINOGLUTETHIMIDE IC50 = 270.0 nM 6.57
CHEMBL229908 LIQUIRITIGENIN DIMETHYL ETHER IC50 = 1860.0 nM 5.73
CHEMBL229635 IC50 = 3670.0 nM 5.43
CHEMBL229789 IC50 = 4080.0 nM 5.39
CHEMBL229906 IC50 = 4670.0 nM 5.33
CHEMBL388374 IC50 = 4750.0 nM 5.32
CHEMBL425670 IC50 = 7670.0 nM 5.12
CHEMBL1162951 IC50 = 12100.0 nM 4.92
CHEMBL229945 IC50 = 13950.0 nM 4.86
CHEMBL229790 IC50 = 25140.0 nM 4.60
CHEMBL228985 IC50 = 28650.0 nM 4.54
CHEMBL558103 ABYSSINONE II IC50 = 40950.0 nM 4.39
CHEMBL229094 IC50 = 54670.0 nM 4.26
CHEMBL389925 IC50 = 82940.0 nM 4.08
CHEMBL390731 IC50 > 261500.0 nM -
CHEMBL229885 LICOAGROCHALCONE A IC50 > 308300.0 nM -
CHEMBL229893 IC50 > 261500.0 nM -
CHEMBL229907 IC50 > 351700.0 nM -
CHEMBL229841 IC50 > 295500.0 nM -
CHEMBL229944 IC50 > 242400.0 nM -
CHEMBL229633 IC50 > 283750.0 nM -
CHEMBL390364 IC50 > 271400.0 nM -
CHEMBL388375 IC50 > 310170.0 nM -
CHEMBL229905 IC50 > 310200.0 nM -