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Assay Detail

CHEMBL754363

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

Binding
Inhibition of neutral endopeptidase 24.11(NEP)
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Neprilysin (CHEMBL1944)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent non-peptidic dual inhibitors of endothelin-converting enzyme and neutral endopeptidase 24.11
De Lombaert S, Stamford LB, Blanchard L, Tan J, Hoyer D, Diefenbacher CG, Wei D, Wallace EM, Moskal MA, Savage P, Jeng AY
Bioorg Med Chem Lett (1997) 7 : 1059 -1064
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.51 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL268473 1 9.22
CHEMBL276690 1 9.15
CHEMBL276872 1 9.13
CHEMBL290698 1 9.05
CHEMBL268761 1 8.84
CHEMBL273489 1 8.60
CHEMBL10251 1 8.32
CHEMBL10247 THIORPHAN -1.0 1 8.32
CHEMBL415967 CGS-314447 1 8.16
CHEMBL9963 1 8.06
CHEMBL418704 1 7.77
CHEMBL479579 PHOSPHORAMIDON 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL268473 IC50 = 0.6 nM 9.22
CHEMBL276690 IC50 = 0.7 nM 9.15
CHEMBL276872 IC50 = 0.74 nM 9.13
CHEMBL290698 IC50 = 0.9 nM 9.05
CHEMBL268761 IC50 = 1.46 nM 8.84
CHEMBL273489 IC50 = 2.5 nM 8.60
CHEMBL10251 IC50 = 4.8 nM 8.32
CHEMBL10247 THIORPHAN IC50 = 4.8 nM 8.32
CHEMBL415967 CGS-314447 IC50 = 6.9 nM 8.16
CHEMBL9963 IC50 = 8.8 nM 8.06
CHEMBL418704 IC50 = 17.0 nM 7.77
CHEMBL479579 PHOSPHORAMIDON IC50 = 30.0 nM 7.52