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

CHEMBL1060019

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

Binding
Inhibition of pig kidney NEP by fluorimetry
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Neprilysin (CHEMBL6107)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Synthesis and enzymatic evaluation of novel partially fluorinated thiol dual ACE/NEP inhibitors.
Olimpieri F, Tambaro S, Fustero S, Lazzari P, Sanchez-Roselló M, Pani L, Volonterio A, Zanda M.
Bioorg Med Chem Lett (2009) 19 : 4715 -4719
PubMed 19596577 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.86 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10247 THIORPHAN -1.0 1 8.21
CHEMBL173287 1 7.39
CHEMBL367174 1 7.30
CHEMBL540674 1 7.10
CHEMBL551145 1 6.64
CHEMBL560685 1 6.52
CHEMBL560409 1 6.37
CHEMBL551622 1 6.24
CHEMBL558146 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10247 THIORPHAN IC50 = 6.2 nM 8.21
CHEMBL173287 IC50 = 41.0 nM 7.39
CHEMBL367174 IC50 = 50.0 nM 7.30
CHEMBL540674 IC50 = 80.0 nM 7.10
CHEMBL551145 IC50 = 230.0 nM 6.64
CHEMBL560685 IC50 = 300.0 nM 6.52
CHEMBL560409 IC50 = 430.0 nM 6.37
CHEMBL551622 IC50 = 580.0 nM 6.24
CHEMBL558146 IC50 = 1150.0 nM 5.94