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Assay Detail

CHEMBL677316

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

Functional
Concentration for 50% inhibition of activity of rat kidney enkephalinase
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Feces
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Neprilysin (CHEMBL3369)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1H NMR configurational correlation for retro-inverso dipeptides: application to the determination of the absolute configuration of "enkephalinase" inhibitors. Relationships between stereochemistry and enzyme recognition.
Fournié-Zaluski MC, Lucas-Soroca E, Devin J, Roques BP.
J Med Chem (1986) 29 : 751 -757
PubMed 3517331 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.80 9.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL165980 1 9.39
CHEMBL51715 1 9.32
CHEMBL165922 1 9.27
CHEMBL165499 1 9.19
CHEMBL164955 1 9.12
CHEMBL165744 1 8.82
CHEMBL61512 (R)-THIORPHAN 1 8.80
CHEMBL298827 (S)-THIORPHAN 1 8.72
CHEMBL349404 1 8.64
CHEMBL45412 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL165980 IC50 = 0.41 nM 9.39
CHEMBL51715 IC50 = 0.48 nM 9.32
CHEMBL165922 IC50 = 0.54 nM 9.27
CHEMBL165499 IC50 = 0.65 nM 9.19
CHEMBL164955 IC50 = 0.75 nM 9.12
CHEMBL165744 IC50 = 1.5 nM 8.82
CHEMBL61512 (R)-THIORPHAN IC50 = 1.6 nM 8.80
CHEMBL298827 (S)-THIORPHAN IC50 = 1.9 nM 8.72
CHEMBL349404 IC50 = 2.3 nM 8.64
CHEMBL45412 IC50 = 210.0 nM 6.68