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Assay Detail

CHEMBL4480339

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

Binding
Inhibition of recombinant human aromatase using 7-methoxy-trifluoromethylcoumarin as substrate incubated for 30 mins by fluorescence microplate reader analysis
28
Total Activities
14
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

Synthesis and aromatase inhibitory evaluation of 4-N-nitrophenyl substituted amino-4H-1,2,4-triazole derivatives.
Song Z, Liu Y, Dai Z, Liu W, Zhao K, Zhang T, Hu Y, Zhang X, Dai Y.
Bioorg Med Chem (2016) 24 : 4723 -4730
PubMed 27567077 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.62 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1444 LETROZOLE 4.0 2 8.66
CHEMBL4574913 2 8.04
CHEMBL4575939 2 7.92
CHEMBL4560281 2 7.84
CHEMBL4556775 2 7.76
CHEMBL4514474 2 7.76
CHEMBL4563511 2 7.71
CHEMBL4592407 2 7.52
CHEMBL4536893 2 7.40
CHEMBL4526798 2 7.36
CHEMBL4568674 2 7.24
CHEMBL4564168 2 7.23
CHEMBL4546916 2 7.14
CHEMBL4547558 2 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1444 LETROZOLE IC50 = 2.178 nM 8.66
CHEMBL1444 LETROZOLE IC50 = 2.18 nM 8.66
CHEMBL4574913 IC50 = 9.02 nM 8.04
CHEMBL4574913 IC50 = 9.016 nM 8.04
CHEMBL4575939 IC50 = 12.12 nM 7.92
CHEMBL4575939 IC50 = 12.11 nM 7.92
CHEMBL4560281 IC50 = 14.53 nM 7.84
CHEMBL4560281 IC50 = 14.52 nM 7.84
CHEMBL4556775 IC50 = 17.42 nM 7.76
CHEMBL4514474 IC50 = 17.38 nM 7.76
CHEMBL4556775 IC50 = 17.42 nM 7.76
CHEMBL4514474 IC50 = 17.38 nM 7.76
CHEMBL4563511 IC50 = 19.66 nM 7.71
CHEMBL4563511 IC50 = 19.68 nM 7.71
CHEMBL4592407 IC50 = 30.2 nM 7.52
CHEMBL4592407 IC50 = 30.19 nM 7.52
CHEMBL4536893 IC50 = 39.81 nM 7.40
CHEMBL4536893 IC50 = 39.77 nM 7.40
CHEMBL4526798 IC50 = 43.55 nM 7.36
CHEMBL4526798 IC50 = 43.57 nM 7.36
CHEMBL4568674 IC50 = 57.54 nM 7.24
CHEMBL4568674 IC50 = 57.58 nM 7.24
CHEMBL4564168 IC50 = 58.88 nM 7.23
CHEMBL4564168 IC50 = 58.85 nM 7.23
CHEMBL4546916 IC50 = 73.11 nM 7.14
CHEMBL4546916 IC50 = 73.17 nM 7.14
CHEMBL4547558 IC50 = 90.78 nM 7.04
CHEMBL4547558 IC50 = 90.73 nM 7.04