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Assay Detail

CHEMBL677314

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

Binding
In vitro inhibition of enkephalinase purified from rat kidney.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

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
IC50 17 7.46 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275637 1 9.00
CHEMBL16975 1 8.92
CHEMBL16779 1 8.85
CHEMBL16457 1 8.82
CHEMBL16046 1 8.70
CHEMBL10247 THIORPHAN -1.0 1 8.40
CHEMBL16622 1 8.00
CHEMBL17107 1 7.92
CHEMBL274994 1 7.52
CHEMBL17040 1 6.46
CHEMBL16791 1 6.22
CHEMBL17095 1 6.16
CHEMBL16568 1 6.12
CHEMBL16675 1 6.10
CHEMBL16467 1 6.10
CHEMBL17084 1 6.07
CHEMBL17059 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275637 IC50 = 1.0 nM 9.00
CHEMBL16975 IC50 = 1.2 nM 8.92
CHEMBL16779 IC50 = 1.4 nM 8.85
CHEMBL16457 IC50 = 1.5 nM 8.82
CHEMBL16046 IC50 = 2.0 nM 8.70
CHEMBL10247 THIORPHAN IC50 = 4.0 nM 8.40
CHEMBL16622 IC50 = 10.0 nM 8.00
CHEMBL17107 IC50 = 12.0 nM 7.92
CHEMBL274994 IC50 = 30.0 nM 7.52
CHEMBL17040 IC50 = 350.0 nM 6.46
CHEMBL16791 IC50 = 600.0 nM 6.22
CHEMBL17095 IC50 = 700.0 nM 6.16
CHEMBL16568 IC50 = 750.0 nM 6.12
CHEMBL16675 IC50 = 800.0 nM 6.10
CHEMBL16467 IC50 = 800.0 nM 6.10
CHEMBL17084 IC50 = 850.0 nM 6.07
CHEMBL17059 IC50 > 1.0 nM -