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Assay Detail

CHEMBL752986

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

Binding
In vitro inhibitory activity against neutral endopeptidase (NEP) was determined
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neprilysin (CHEMBL1944)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual metalloprotease inhibitors. III. utilization of bicyclic and monocyclic diazepinone based mercaptoacetyls
Robl JA, Sun C, Simpkins LM, Ryono DE, Barrish JC, Karanewsky DS, Asaad MM, Schaeffer TR, Trippodo NC
Bioorg Med Chem Lett (1994) 4 : 2055 -2060
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.05 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL65545 1 8.52
CHEMBL299639 1 8.22
CHEMBL66481 1 7.80
CHEMBL66254 1 7.66
CHEMBL304881 1 7.26
CHEMBL305108 1 6.85
CHEMBL63001 1 6.32
CHEMBL417034 1 6.31
CHEMBL61566 1 5.83
CHEMBL62417 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL65545 IC50 = 3.0 nM 8.52
CHEMBL299639 IC50 = 6.0 nM 8.22
CHEMBL66481 IC50 = 16.0 nM 7.80
CHEMBL66254 IC50 = 22.0 nM 7.66
CHEMBL304881 IC50 = 55.0 nM 7.26
CHEMBL305108 IC50 = 140.0 nM 6.85
CHEMBL63001 IC50 = 484.0 nM 6.32
CHEMBL417034 IC50 = 486.0 nM 6.31
CHEMBL61566 IC50 = 1490.0 nM 5.83
CHEMBL62417 IC50 = 1922.0 nM 5.72