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Assay Detail

CHEMBL1670936

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

Binding
Inhibition of human aminopeptidase N by Dixon plot analysis
9
Total Activities
9
Compounds Tested
2
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

Amino-benzosuberone: a novel warhead for selective inhibition of human aminopeptidase-N/CD13.
Albrecht S, Al-Lakkis-Wehbe M, Orsini A, Defoin A, Pale P, Salomon E, Tarnus C, Weibel JM.
Bioorg Med Chem (2011) 19 : 1434 -1449
PubMed 21292493 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.46 5.46
Ki 4 5.31 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1668623 1 6.30
CHEMBL1668626 1 6.00
CHEMBL29292 UBENIMEX 2.0 1 5.46
CHEMBL1668624 1 4.70
CHEMBL1668630 1 4.22
CHEMBL1668625 1 -
CHEMBL1668627 2-AMINOCYCLOHEPTANONE HYDROCHLORIDE 1 -
CHEMBL1668628 1 -
CHEMBL1668629 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1668623 Ki = 500.0 nM 6.30
CHEMBL1668626 Ki = 1000.0 nM 6.00
CHEMBL29292 UBENIMEX IC50 = 3500.0 nM 5.46
CHEMBL1668624 Ki = 20000.0 nM 4.70
CHEMBL1668630 Ki = 60000.0 nM 4.22
CHEMBL1668625 IC50 > 1000000.0 nM -
CHEMBL1668627 2-AMINOCYCLOHEPTANONE HYDROCHLORIDE IC50 = 310000.0 nM -
CHEMBL1668628 IC50 = 110000.0 nM -
CHEMBL1668629 IC50 = 300000.0 nM -