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Assay Detail

CHEMBL646401

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

Binding
Inhibition of [3H]Leu-enkephalin binding to Aminopeptidase N from hog kidney
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Aminopeptidase N (CHEMBL2590)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Potent and systemically active aminopeptidase N inhibitors designed from active-site investigation.
Fournié-Zaluski MC, Coric P, Turcaud S, Bruetschy L, Lucas E, Noble F, Roques BP.
J Med Chem (1992) 35 : 1259 -1266
PubMed 1348542 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.74 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1159812 1 7.96
CHEMBL1159809 1 7.70
CHEMBL1159811 1 7.70
CHEMBL1159810 1 7.68
CHEMBL1159806 1 7.66
CHEMBL1159805 1 7.40
CHEMBL1159815 1 7.25
CHEMBL1159814 1 7.05
CHEMBL1159813 1 6.89
CHEMBL1159807 1 5.40
CHEMBL26989 1 4.12
CHEMBL1159816 1 4.10
CHEMBL26845 1 -
CHEMBL1159808 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1159812 IC50 = 11.0 nM 7.96
CHEMBL1159809 IC50 = 20.0 nM 7.70
CHEMBL1159811 IC50 = 20.0 nM 7.70
CHEMBL1159810 IC50 = 21.0 nM 7.68
CHEMBL1159806 IC50 = 22.0 nM 7.66
CHEMBL1159805 IC50 = 40.0 nM 7.40
CHEMBL1159815 IC50 = 56.0 nM 7.25
CHEMBL1159814 IC50 = 90.0 nM 7.05
CHEMBL1159813 IC50 = 130.0 nM 6.89
CHEMBL1159807 IC50 = 4000.0 nM 5.40
CHEMBL26989 IC50 = 75000.0 nM 4.12
CHEMBL1159816 IC50 = 80000.0 nM 4.10
CHEMBL26845 IC50 = 500000.0 nM -
CHEMBL1159808 IC50 = 160000.0 nM -