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Assay Detail

CHEMBL1833759

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

Binding
Inhibition of neutral endopeptidase in human fibroblasts homogenates using glutaryl-Ala-Ala-Phe-4-methoxy-2-naphtylamide as substrate after 1 hrs by fluorimetric assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neprilysin (CHEMBL1944)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based design of dipeptide derivatives for the human neutral endopeptidase.
Misawa K, Suzuki Y, Takahashi S, Yoshimori A, Takasawa R, Shibuya Y, Tanuma S.
Bioorg Med Chem (2011) 19 : 5935 -5947
PubMed 21937235 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.51 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1829584 1 9.44
CHEMBL1829585 1 9.29
CHEMBL479579 PHOSPHORAMIDON 1 8.70
CHEMBL1829583 1 8.01
CHEMBL1829587 1 6.38
CHEMBL1829586 1 6.37
CHEMBL1829582 1 4.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1829584 IC50 = 0.36 nM 9.44
CHEMBL1829585 IC50 = 0.51 nM 9.29
CHEMBL479579 PHOSPHORAMIDON IC50 = 2.0 nM 8.70
CHEMBL1829583 IC50 = 9.7 nM 8.01
CHEMBL1829587 IC50 = 420.0 nM 6.38
CHEMBL1829586 IC50 = 430.0 nM 6.37
CHEMBL1829582 IC50 = 44000.0 nM 4.36