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Assay Detail

CHEMBL4132610

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

Binding
Inhibition of recombinant human C-terminal His10-tagged APN (Lys69 to Lys967 residues) using Ala-AMC as substrate measured for 30 mins by fluorescence assay
11
Total Activities
11
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

Aminopeptidase N (CHEMBL1907)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Puromycin based inhibitors of aminopeptidases for the potential treatment of hematologic malignancies.
Singh R, Williams J, Vince R.
Eur J Med Chem (2017) 139 : 325 -336
PubMed 28803047 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.87 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4169814 1 6.57
CHEMBL4165328 1 6.55
CHEMBL3244800 1 6.38
CHEMBL2103847 TOSEDOSTAT 2.0 1 6.17
CHEMBL29292 UBENIMEX 2.0 1 6.10
CHEMBL3244799 1 5.96
CHEMBL4173240 1 5.50
CHEMBL4161892 1 5.25
CHEMBL469912 PUROMYCIN 2.0 1 4.39
CHEMBL4161496 1 -
CHEMBL4161744 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4169814 IC50 = 270.0 nM 6.57
CHEMBL4165328 IC50 = 280.0 nM 6.55
CHEMBL3244800 IC50 = 420.0 nM 6.38
CHEMBL2103847 TOSEDOSTAT IC50 = 680.0 nM 6.17
CHEMBL29292 UBENIMEX IC50 = 800.0 nM 6.10
CHEMBL3244799 IC50 = 1100.0 nM 5.96
CHEMBL4173240 IC50 = 3200.0 nM 5.50
CHEMBL4161892 IC50 = 5600.0 nM 5.25
CHEMBL469912 PUROMYCIN IC50 = 41000.0 nM 4.39
CHEMBL4161496 IC50 - -
CHEMBL4161744 IC50 - -