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Assay Detail

CHEMBL646467

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

Binding
Inhibitory activity against rabbit kidney aminopeptidase using 10 nM of [3H]Leu-enkephalin as substrate
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aminopeptidase N (CHEMBL2590)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

New bidentates as full inhibitors of enkephalin-degrading enzymes: synthesis and analgesic properties.
Fournié-Zaluski MC, Coulaud A, Bouboutou R, Chaillet P, Devin J, Waksman G, Costentin J, Roques BP.
J Med Chem (1985) 28 : 1158 -1169
PubMed 3897541 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.47 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17107 1 9.00
CHEMBL16779 1 8.70
CHEMBL16457 1 8.60
CHEMBL29292 UBENIMEX 2.0 1 8.30
CHEMBL16046 1 8.15
CHEMBL16622 1 8.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17107 IC50 = 1.0 nM 9.00
CHEMBL16779 IC50 = 2.0 nM 8.70
CHEMBL16457 IC50 = 2.5 nM 8.60
CHEMBL29292 UBENIMEX IC50 = 5.0 nM 8.30
CHEMBL16046 IC50 = 7.1 nM 8.15
CHEMBL16622 IC50 = 8.5 nM 8.07