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Assay Detail

CHEMBL4132608

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

Binding
Inhibition of recombinant human N-terminal His6-MBP-tagged PSA expressed in Escherichia coli BL21 STAR (DE3) using 4-Ala-MNA as substrate measured for 30 mins by thefluorescence 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

Puromycin-sensitive aminopeptidase (CHEMBL2264)
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 5.62 8.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3244800 1 8.13
CHEMBL2103847 TOSEDOSTAT 2.0 1 6.58
CHEMBL3244799 1 6.03
CHEMBL4165328 1 5.85
CHEMBL29292 UBENIMEX 2.0 1 5.46
CHEMBL4161892 1 5.32
CHEMBL4161496 1 5.30
CHEMBL469912 PUROMYCIN 2.0 1 5.01
CHEMBL4173240 1 4.28
CHEMBL4161744 1 4.28
CHEMBL4169814 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3244800 IC50 = 7.4 nM 8.13
CHEMBL2103847 TOSEDOSTAT IC50 = 260.0 nM 6.58
CHEMBL3244799 IC50 = 940.0 nM 6.03
CHEMBL4165328 IC50 = 1400.0 nM 5.85
CHEMBL29292 UBENIMEX IC50 = 3500.0 nM 5.46
CHEMBL4161892 IC50 = 4800.0 nM 5.32
CHEMBL4161496 IC50 = 5000.0 nM 5.30
CHEMBL469912 PUROMYCIN IC50 = 9700.0 nM 5.01
CHEMBL4173240 IC50 = 53000.0 nM 4.28
CHEMBL4161744 IC50 = 53000.0 nM 4.28
CHEMBL4169814 IC50 > 100000.0 nM -