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Assay Detail

CHEMBL677322

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

Binding
50% inhibitory activity against enkephalinase purified from rat kidney with [3H]D-Ala2-Leu-enkephalin (20 nM) as substrate.
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neprilysin (CHEMBL3369)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New bidentates as full inhibitors of enkephalin-degrading enzymes: synthesis and analgesic properties.
Fournié-Zaluski MC, Coulaud A, Bouboutou R, Chaillet P, Devin J, Waksman G, Costentin J, Roques BP.
J Med Chem (1985) 28 : 1158 -1169
PubMed 3897541 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.76 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85320 KELATORPHAN 1 8.77
CHEMBL2079630 1 8.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85320 KELATORPHAN Ki = 1.7 nM 8.77
CHEMBL2079630 Ki = 1.8 nM 8.74