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Assay Detail

CHEMBL1828368

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

Binding
Inhibition of aromatase using 7-methoxy-4-trifluoromethyl coumarin as substrate after 30 mins by fluorescence-based colorimetric analysis
68
Total Activities
68
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship of 1- and 2-substituted-1,2,3-triazole letrozole-based analogues as aromatase inhibitors.
Doiron J, Soultan AH, Richard R, Touré MM, Picot N, Richard R, Cuperlović-Culf M, Robichaud GA, Touaibia M.
Eur J Med Chem (2011) 46 : 4010 -4024
PubMed 21703734 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 68 5.37 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29482 1 8.40
CHEMBL349822 1 8.15
CHEMBL224789 1 8.10
CHEMBL1444 LETROZOLE 4.0 1 8.10
CHEMBL336638 1 7.70
CHEMBL1824769 1 7.00
CHEMBL14192 BENZYLIMIDAZOLE 1 6.82
CHEMBL1825020 1 6.82
CHEMBL1825024 1 5.96
CHEMBL1825045 1 5.87
CHEMBL1825047 1 5.64
CHEMBL1825036 1 5.63
CHEMBL1825046 1 5.56
CHEMBL1825027 1 5.51
CHEMBL1825030 1 5.47
CHEMBL1825032 1 5.41
CHEMBL1825021 1 5.39
CHEMBL1825035 1 5.38
CHEMBL1825025 1 5.36
CHEMBL1824755 1 5.34
CHEMBL1824742 1 5.33
CHEMBL1824750 1 5.33
CHEMBL1825044 1 5.30
CHEMBL1824743 1 5.29
CHEMBL1825026 1 5.28
CHEMBL1825034 1 5.25
CHEMBL1825031 1 5.21
CHEMBL1825041 1 5.19
CHEMBL1825039 1 5.13
CHEMBL1824751 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29482 IC50 = 4.0 nM 8.40
CHEMBL349822 IC50 = 7.0 nM 8.15
CHEMBL1444 LETROZOLE IC50 = 8.0 nM 8.10
CHEMBL224789 IC50 = 8.0 nM 8.10
CHEMBL336638 IC50 = 20.0 nM 7.70
CHEMBL1824769 IC50 = 100.0 nM 7.00
CHEMBL14192 BENZYLIMIDAZOLE IC50 = 150.0 nM 6.82
CHEMBL1825020 IC50 = 150.0 nM 6.82
CHEMBL1825024 IC50 = 1100.0 nM 5.96
CHEMBL1825045 IC50 = 1360.0 nM 5.87
CHEMBL1825047 IC50 = 2270.0 nM 5.64
CHEMBL1825036 IC50 = 2340.0 nM 5.63
CHEMBL1825046 IC50 = 2780.0 nM 5.56
CHEMBL1825027 IC50 = 3070.0 nM 5.51
CHEMBL1825030 IC50 = 3380.0 nM 5.47
CHEMBL1825032 IC50 = 3910.0 nM 5.41
CHEMBL1825021 IC50 = 4110.0 nM 5.39
CHEMBL1825035 IC50 = 4170.0 nM 5.38
CHEMBL1825025 IC50 = 4370.0 nM 5.36
CHEMBL1824755 IC50 = 4580.0 nM 5.34
CHEMBL1824742 IC50 = 4700.0 nM 5.33
CHEMBL1824750 IC50 = 4640.0 nM 5.33
CHEMBL1825044 IC50 = 5040.0 nM 5.30
CHEMBL1824743 IC50 = 5070.0 nM 5.29
CHEMBL1825026 IC50 = 5260.0 nM 5.28
CHEMBL1825034 IC50 = 5620.0 nM 5.25
CHEMBL1825031 IC50 = 6090.0 nM 5.21
CHEMBL1825041 IC50 = 6400.0 nM 5.19
CHEMBL1825039 IC50 = 7470.0 nM 5.13
CHEMBL1824751 IC50 = 7730.0 nM 5.11
CHEMBL1825042 IC50 = 7980.0 nM 5.10
CHEMBL1825028 IC50 = 7880.0 nM 5.10
CHEMBL1825033 IC50 = 9160.0 nM 5.04
CHEMBL1825040 IC50 = 9530.0 nM 5.02
CHEMBL1825043 IC50 = 9770.0 nM 5.01
CHEMBL1824747 IC50 = 10330.0 nM 4.99
CHEMBL272339 IC50 = 10600.0 nM 4.97
CHEMBL1824744 IC50 = 10600.0 nM 4.97
CHEMBL1825029 IC50 = 10700.0 nM 4.97
CHEMBL1825049 IC50 = 10700.0 nM 4.97
CHEMBL1824752 IC50 = 10950.0 nM 4.96
CHEMBL1824748 IC50 = 10970.0 nM 4.96
CHEMBL1824756 IC50 = 10960.0 nM 4.96
CHEMBL1825037 IC50 = 11570.0 nM 4.94
CHEMBL1824765 IC50 = 11610.0 nM 4.93
CHEMBL1825018 IC50 = 11880.0 nM 4.92
CHEMBL1825023 IC50 = 12010.0 nM 4.92
CHEMBL1824753 IC50 = 12160.0 nM 4.92
CHEMBL1825017 IC50 = 12200.0 nM 4.91
CHEMBL1825038 IC50 = 12630.0 nM 4.90