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Assay Detail

CHEMBL751029

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

Binding
Inhibitory activity against neutral endopeptidase (NEP)prepared from microsomal fractions of rat small intestine
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neprilysin (CHEMBL3369)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Aminophosphonate endothelin converting enzyme inhibitors: potency-enhancing and selectivity-improving modifications of phosphoramidon
Fukami T, Hayama T, Amano Y, Nakamura Y, Arai Y, Matsuyama K, Yano M, Ishikawa K
Bioorg Med Chem Lett (1994) 4 : 1257 -1262
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.89 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL479579 PHOSPHORAMIDON 1 8.38
CHEMBL281333 1 7.62
CHEMBL282663 1 6.89
CHEMBL277199 1 6.89
CHEMBL25269 1 6.85
CHEMBL279255 1 6.26
CHEMBL283758 1 6.25
CHEMBL277195 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL479579 PHOSPHORAMIDON IC50 = 4.2 nM 8.38
CHEMBL281333 IC50 = 24.0 nM 7.62
CHEMBL282663 IC50 = 130.0 nM 6.89
CHEMBL277199 IC50 = 130.0 nM 6.89
CHEMBL25269 IC50 = 140.0 nM 6.85
CHEMBL279255 IC50 = 550.0 nM 6.26
CHEMBL283758 IC50 = 560.0 nM 6.25
CHEMBL277195 IC50 = 1100.0 nM 5.96