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Assay Detail

CHEMBL666795

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

Binding
Inhibition of human placental microsome cytochrome P450 19A1 aromatase
7
Total Activities
7
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

A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase.
Recanatini M, Bisi A, Cavalli A, Belluti F, Gobbi S, Rampa A, Valenti P, Palzer M, Palusczak A, Hartmann RW.
J Med Chem (2001) 44 : 672 -680
PubMed 11262078 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.32 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL159073 1 7.40
CHEMBL421149 1 7.37
CHEMBL421829 1 7.05
CHEMBL78322 1 6.03
CHEMBL307160 1 6.01
CHEMBL442373 1 5.64
CHEMBL488 AMINOGLUTETHIMIDE 4.0 1 4.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL159073 IC50 = 40.0 nM 7.40
CHEMBL421149 IC50 = 43.0 nM 7.37
CHEMBL421829 IC50 = 89.0 nM 7.05
CHEMBL78322 IC50 = 940.0 nM 6.03
CHEMBL307160 IC50 = 970.0 nM 6.01
CHEMBL442373 IC50 = 2300.0 nM 5.64
CHEMBL488 AMINOGLUTETHIMIDE IC50 = 18500.0 nM 4.73