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Assay Detail

CHEMBL644743

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Binding
Compound was evaluated for inhibition of enkephalin degrading enzyme, aminopeptidase N(APN)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aminopeptidase N (CHEMBL1907)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Long lasting antinociceptive properties of enkephalin degrading enzyme (NEP and APN) inhibitor prodrugs.
Chen H, Noble F, Roques BP, Fournié-Zaluski MC.
J Med Chem (2001) 44 : 3523 -3530
PubMed 11585456 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.50 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL420321 1 8.54
CHEMBL117394 1 8.32
CHEMBL1160959 1 7.96
CHEMBL85320 KELATORPHAN 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL420321 Ki = 2.9 nM 8.54
CHEMBL117394 Ki = 4.8 nM 8.32
CHEMBL1160959 Ki = 11.0 nM 7.96
CHEMBL85320 KELATORPHAN Ki = 7000.0 nM 5.16