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Assay Detail

CHEMBL666789

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

Binding
Inhibition of aromatase activity in human placental microsomes determined by radiometric assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Placenta
Subcellular Microsomes
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Role of hydrophilic interaction in binding of hydroxylated 3-deoxy C(19) steroids to the active site of aromatase.
Numazawa M, Yamada K, Nitta S, Sasaki C, Kidokoro K.
J Med Chem (2001) 44 : 4277 -4283
PubMed 11708928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.21 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1630274 1 7.51
CHEMBL1629805 1 7.31
CHEMBL1630261 1 7.30
CHEMBL1629806 1 6.72
CHEMBL3349864 1 6.55
CHEMBL2311169 1 6.18
CHEMBL2111917 1 6.16
CHEMBL3349856 1 6.07
CHEMBL1630267 1 6.03
CHEMBL2112739 1 6.00
CHEMBL1630266 1 5.85
CHEMBL1630273 1 5.17
CHEMBL1630911 1 5.16
CHEMBL2112738 1 4.96
CHEMBL1629804 1 -
CHEMBL1630275 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1630274 IC50 = 31.0 nM 7.51
CHEMBL1629805 IC50 = 49.0 nM 7.31
CHEMBL1630261 IC50 = 50.0 nM 7.30
CHEMBL1629806 IC50 = 190.0 nM 6.72
CHEMBL3349864 IC50 = 280.0 nM 6.55
CHEMBL2311169 IC50 = 660.0 nM 6.18
CHEMBL2111917 IC50 = 700.0 nM 6.16
CHEMBL3349856 IC50 = 860.0 nM 6.07
CHEMBL1630267 IC50 = 940.0 nM 6.03
CHEMBL2112739 IC50 = 1000.0 nM 6.00
CHEMBL1630266 IC50 = 1400.0 nM 5.85
CHEMBL1630273 IC50 = 6800.0 nM 5.17
CHEMBL1630911 IC50 = 6900.0 nM 5.16
CHEMBL2112738 IC50 = 11000.0 nM 4.96
CHEMBL1629804 IC50 = 60.0 nM -
CHEMBL1630275 IC50 = 150000.0 nM -