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Assay Detail

CHEMBL1011778

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

Binding
Inhibition of human aromatase-mediated conversion of [1beta3H]androstenedione to estrone by Lineweaver-Burke plot in presence of NADPH
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Neves MA, Dinis TC, Colombo G, Sá e Melo ML.
J Med Chem (2009) 52 : 143 -150
PubMed 19072235 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.99 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL513615 1 8.72
CHEMBL1444 LETROZOLE 4.0 1 8.66
CHEMBL459503 1 8.25
CHEMBL459502 1 8.19
CHEMBL522733 1 7.88
CHEMBL509750 1 7.82
CHEMBL495567 1 7.59
CHEMBL495565 1 7.48
CHEMBL496777 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL513615 Ki = 1.9 nM 8.72
CHEMBL1444 LETROZOLE Ki = 2.2 nM 8.66
CHEMBL459503 Ki = 5.6 nM 8.25
CHEMBL459502 Ki = 6.5 nM 8.19
CHEMBL522733 Ki = 13.1 nM 7.88
CHEMBL509750 Ki = 15.1 nM 7.82
CHEMBL495567 Ki = 25.5 nM 7.59
CHEMBL495565 Ki = 33.4 nM 7.48
CHEMBL496777 Ki = 52.7 nM 7.28