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Assay Detail

CHEMBL870913

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Binding
Inhibition of CYP19
19
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 Expert

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme.
Gobbi S, Cavalli A, Rampa A, Belluti F, Piazzi L, Paluszcak A, Hartmann RW, Recanatini M, Bisi A.
J Med Chem (2006) 49 : 4777 -4780
PubMed 16854084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.58 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL213588 2 7.35
CHEMBL9298 FADROZOLE 2.0 1 7.28
CHEMBL209731 2 7.16
CHEMBL213587 2 7.15
CHEMBL212473 2 7.10
CHEMBL377766 2 6.36
CHEMBL212168 2 6.33
CHEMBL158635 2 6.26
CHEMBL377626 2 5.75
CHEMBL209047 2 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL213588 IC50 = 45.0 nM 7.35
CHEMBL213588 IC50 = 44.67 nM 7.35
CHEMBL9298 FADROZOLE IC50 = 52.0 nM 7.28
CHEMBL209731 IC50 = 69.18 nM 7.16
CHEMBL209731 IC50 = 69.0 nM 7.16
CHEMBL213587 IC50 = 70.79 nM 7.15
CHEMBL213587 IC50 = 71.0 nM 7.15
CHEMBL212473 IC50 = 80.0 nM 7.10
CHEMBL212473 IC50 = 79.43 nM 7.10
CHEMBL377766 IC50 = 440.0 nM 6.36
CHEMBL377766 IC50 = 436.52 nM 6.36
CHEMBL212168 IC50 = 467.74 nM 6.33
CHEMBL212168 IC50 = 470.0 nM 6.33
CHEMBL158635 IC50 = 550.0 nM 6.26
CHEMBL158635 IC50 = 549.54 nM 6.26
CHEMBL377626 IC50 = 1800.0 nM 5.75
CHEMBL377626 IC50 = 1819.7 nM 5.74
CHEMBL209047 IC50 = 4073.8 nM 5.39
CHEMBL209047 IC50 = 4100.0 nM 5.39