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Assay Detail

CHEMBL747373

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

Binding
In vitro inhibition of Neutral endopeptidase (NEP) enzyme
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neprilysin (CHEMBL3369)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N-Phosphonomethyl dipeptides and their phosphonate prodrugs, a new generation of neutral endopeptidase (NEP, EC 3.4.24.11) inhibitors.
De Lombaert S, Erion MD, Tan J, Blanchard L, el-Chehabi L, Ghai RD, Sakane Y, Berry C, Trapani AJ.
J Med Chem (1994) 37 : 498 -511
PubMed 8120868 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.46 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285038 1 8.72
CHEMBL341868 1 8.70
CHEMBL146594 1 8.52
CHEMBL148521 1 8.40
CHEMBL10247 THIORPHAN -1.0 1 8.32
CHEMBL357903 1 8.30
CHEMBL149646 1 8.00
CHEMBL145937 1 7.96
CHEMBL146631 1 7.85
CHEMBL479579 PHOSPHORAMIDON 1 7.57
CHEMBL342768 1 6.92
CHEMBL149131 1 6.68
CHEMBL358631 1 6.62
CHEMBL145916 1 6.52
CHEMBL148564 1 6.00
CHEMBL147400 1 5.94
CHEMBL2112023 1 5.75
CHEMBL357607 1 -
CHEMBL423937 1 -
CHEMBL359254 1 -
CHEMBL150209 1 -
CHEMBL177646 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285038 IC50 = 1.9 nM 8.72
CHEMBL341868 IC50 = 2.0 nM 8.70
CHEMBL146594 IC50 = 3.0 nM 8.52
CHEMBL148521 IC50 = 4.0 nM 8.40
CHEMBL10247 THIORPHAN IC50 = 4.8 nM 8.32
CHEMBL357903 IC50 = 5.0 nM 8.30
CHEMBL149646 IC50 = 10.0 nM 8.00
CHEMBL145937 IC50 = 11.0 nM 7.96
CHEMBL146631 IC50 = 14.0 nM 7.85
CHEMBL479579 PHOSPHORAMIDON IC50 = 27.0 nM 7.57
CHEMBL342768 IC50 = 120.0 nM 6.92
CHEMBL149131 IC50 = 207.0 nM 6.68
CHEMBL358631 IC50 = 238.0 nM 6.62
CHEMBL145916 IC50 = 301.0 nM 6.52
CHEMBL148564 IC50 = 1000.0 nM 6.00
CHEMBL147400 IC50 = 1150.0 nM 5.94
CHEMBL2112023 IC50 = 1800.0 nM 5.75
CHEMBL357607 IC50 > 1000.0 nM -
CHEMBL423937 IC50 > 1000.0 nM -
CHEMBL359254 IC50 > 1000.0 nM -
CHEMBL150209 IC50 > 1000.0 nM -
CHEMBL177646 IC50 > 1000.0 nM -