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Assay Detail

CHEMBL2176197

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

Binding
Inhibition of human recombinant NEP using Mca-RPPGFSAFK(Dnp)-OH as substrate incubated for 15 mins prior to substrate addition measured after 20 to 30 mins by fluorimetric analysis
9
Total Activities
7
Compounds Tested
2
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

Novel β-amino acid derivatives as inhibitors of cathepsin A.
Ruf S, Buning C, Schreuder H, Horstick G, Linz W, Olpp T, Pernerstorfer J, Hiss K, Kroll K, Kannt A, Kohlmann M, Linz D, Hübschle T, Rütten H, Wirth K, Schmidt T, Sadowski T.
J Med Chem (2012) 55 : 7636 -7649
PubMed 22861813 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.60 6.52
Inhibition 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3145333 1 6.52
CHEMBL2171396 1 5.72
CHEMBL2171398 1 4.57
CHEMBL2171393 2 -
CHEMBL2171392 2 -
CHEMBL3145346 1 -
CHEMBL3145341 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3145333 IC50 = 300.0 nM 6.52
CHEMBL2171396 IC50 = 1900.0 nM 5.72
CHEMBL2171398 IC50 = 27000.0 nM 4.57
CHEMBL2171393 IC50 > 1000.0 nM -
CHEMBL2171392 IC50 > 1000.0 nM -
CHEMBL3145346 IC50 < 60.0 nM -
CHEMBL2171393 Inhibition - % -
CHEMBL2171392 Inhibition - % -
CHEMBL3145341 Inhibition - % -