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

CHEMBL677318

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

Binding
Inhibition of enkephalinase activity in synaptic membranes prepared from rat striatum
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neprilysin (CHEMBL3369)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Enkephalinase inhibitors. 1. 2,4-Dibenzylglutaric acid derivatives.
Ksander GM, Diefenbacher CG, Yuan AM, Clark F, Sakane Y, Ghai RD.
J Med Chem (1989) 32 : 2519 -2526
PubMed 2585440 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.49 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL479579 PHOSPHORAMIDON 1 9.22
CHEMBL10247 THIORPHAN -1.0 1 8.52
CHEMBL85397 1 8.40
CHEMBL83778 1 8.40
CHEMBL85159 1 8.30
CHEMBL85560 1 8.22
CHEMBL295104 1 8.10
CHEMBL314855 1 8.05
CHEMBL83326 1 7.92
CHEMBL47289 1 7.75
CHEMBL430436 1 7.70
CHEMBL315312 1 7.60
CHEMBL311093 1 7.54
CHEMBL82732 1 7.42
CHEMBL84930 1 7.40
CHEMBL421724 1 7.13
CHEMBL85324 1 7.05
CHEMBL84195 1 6.10
CHEMBL313766 1 6.00
CHEMBL84865 1 6.00
CHEMBL84370 1 6.00
CHEMBL84258 1 6.00
CHEMBL86222 1 -
CHEMBL84924 1 -
CHEMBL2114199 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL479579 PHOSPHORAMIDON IC50 = 0.6 nM 9.22
CHEMBL10247 THIORPHAN IC50 = 3.0 nM 8.52
CHEMBL85397 IC50 = 4.0 nM 8.40
CHEMBL83778 IC50 = 4.0 nM 8.40
CHEMBL85159 IC50 = 5.0 nM 8.30
CHEMBL85560 IC50 = 6.0 nM 8.22
CHEMBL295104 IC50 = 8.0 nM 8.10
CHEMBL314855 IC50 = 9.0 nM 8.05
CHEMBL83326 IC50 = 12.0 nM 7.92
CHEMBL47289 IC50 = 18.0 nM 7.75
CHEMBL430436 IC50 = 20.0 nM 7.70
CHEMBL315312 IC50 = 25.0 nM 7.60
CHEMBL311093 IC50 = 29.0 nM 7.54
CHEMBL82732 IC50 = 38.0 nM 7.42
CHEMBL84930 IC50 = 40.0 nM 7.40
CHEMBL421724 IC50 = 74.0 nM 7.13
CHEMBL85324 IC50 = 90.0 nM 7.05
CHEMBL84195 IC50 = 800.0 nM 6.10
CHEMBL313766 IC50 = 1000.0 nM 6.00
CHEMBL84865 IC50 = 1000.0 nM 6.00
CHEMBL84370 IC50 = 1000.0 nM 6.00
CHEMBL84258 IC50 = 1000.0 nM 6.00
CHEMBL86222 IC50 > 1000.0 nM -
CHEMBL84924 IC50 > 1000.0 nM -
CHEMBL2114199 IC50 > 1000.0 nM -