Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1780284

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

Binding
Inhibition of neutral endopeptidase
13
Total Activities
13
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

Synthesis and evaluation of heteroarylalanine diacids as potent and selective neutral endopeptidase inhibitors.
Glossop MS, Bazin RJ, Dack KN, Fox DN, MacDonald GA, Mills M, Owen DR, Phillips C, Reeves KA, Ringer TJ, Strang RS, Watson CA.
Bioorg Med Chem Lett (2011) 21 : 3404 -3406
PubMed 21515054 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.48 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1778532 1 9.52
CHEMBL1778534 1 9.52
CHEMBL42583 SAMPATRILAT 2.0 1 9.22
CHEMBL1778530 1 9.22
CHEMBL1778536 1 8.72
CHEMBL1778531 1 8.32
CHEMBL1778533 1 8.30
CHEMBL1778535 1 8.22
CHEMBL1778529 1 8.15
CHEMBL434492 CANDOXATRILAT 2.0 1 8.11
CHEMBL1778528 1 7.70
CHEMBL1778527 1 7.66
CHEMBL1778526 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1778532 IC50 = 0.3 nM 9.52
CHEMBL1778534 IC50 = 0.3 nM 9.52
CHEMBL42583 SAMPATRILAT IC50 = 0.6 nM 9.22
CHEMBL1778530 IC50 = 0.6 nM 9.22
CHEMBL1778536 IC50 = 1.9 nM 8.72
CHEMBL1778531 IC50 = 4.8 nM 8.32
CHEMBL1778533 IC50 = 5.0 nM 8.30
CHEMBL1778535 IC50 = 6.0 nM 8.22
CHEMBL1778529 IC50 = 7.0 nM 8.15
CHEMBL434492 CANDOXATRILAT IC50 = 7.8 nM 8.11
CHEMBL1778528 IC50 = 20.0 nM 7.70
CHEMBL1778527 IC50 = 22.0 nM 7.66
CHEMBL1778526 IC50 = 28.0 nM 7.55