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Assay Detail

CHEMBL645588

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

Binding
In vitro inhibitory concentration against Aromatase was determined using [1-beta,2beta-3H]testosterone as radioligand
14
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.
Bayer H, Batzl C, Hartmann RW, Mannschreck A.
J Med Chem (1991) 34 : 2685 -2691
PubMed 1895288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.65 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93828 3 6.77
CHEMBL92488 1 6.16
CHEMBL90427 1 5.66
CHEMBL313774 1 5.52
CHEMBL88233 1 5.48
CHEMBL92065 1 5.37
CHEMBL90077 1 5.31
CHEMBL91818 1 5.21
CHEMBL93666 3 5.10
CHEMBL91992 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93828 IC50 = 170.0 nM 6.77
CHEMBL93828 IC50 = 200.0 nM 6.70
CHEMBL93828 IC50 = 210.0 nM 6.68
CHEMBL92488 IC50 = 690.0 nM 6.16
CHEMBL90427 IC50 = 2200.0 nM 5.66
CHEMBL313774 IC50 = 3000.0 nM 5.52
CHEMBL88233 IC50 = 3300.0 nM 5.48
CHEMBL92065 IC50 = 4300.0 nM 5.37
CHEMBL90077 IC50 = 4900.0 nM 5.31
CHEMBL91818 IC50 = 6200.0 nM 5.21
CHEMBL93666 IC50 = 7900.0 nM 5.10
CHEMBL91992 IC50 = 8600.0 nM 5.07
CHEMBL93666 IC50 = 8500.0 nM 5.07
CHEMBL93666 IC50 = 9600.0 nM 5.02