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Assay Detail

CHEMBL662434

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

Binding
Inhibition of Human placental Cytochrome P450 19A1
14
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

Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.
Hartmann RW, Bayer H, Grün G, Sergejew T, Bartz U, Mitrenga M.
J Med Chem (1995) 38 : 2103 -2111
PubMed 7783141 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.24 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294361 3 7.52
CHEMBL304583 1 7.18
CHEMBL67842 1 7.16
CHEMBL304903 1 6.73
CHEMBL304222 1 6.48
CHEMBL66867 1 6.43
CHEMBL419619 3 6.04
CHEMBL66673 1 5.47
CHEMBL63336 1 5.37
CHEMBL65590 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294361 IC50 = 30.0 nM 7.52
CHEMBL294361 IC50 = 61.0 nM 7.21
CHEMBL304583 IC50 = 66.0 nM 7.18
CHEMBL67842 IC50 = 69.0 nM 7.16
CHEMBL304903 IC50 = 185.0 nM 6.73
CHEMBL304222 IC50 = 330.0 nM 6.48
CHEMBL66867 IC50 = 370.0 nM 6.43
CHEMBL419619 IC50 = 920.0 nM 6.04
CHEMBL419619 IC50 = 1400.0 nM 5.85
CHEMBL419619 IC50 = 2800.0 nM 5.55
CHEMBL66673 IC50 = 3350.0 nM 5.47
CHEMBL63336 IC50 = 4300.0 nM 5.37
CHEMBL65590 IC50 = 5000.0 nM 5.30
CHEMBL294361 IC50 = 10000.0 nM 5.00