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Assay Detail

CHEMBL755112

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Binding
Tested for inhibitory potency against neutral endopeptidase (NEP)
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Neprilysin (CHEMBL3768)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

New thiol inhibitors of neutral endopeptidase EC 3.4.24.11: synthesis and enzyme active-site recognition.
Gomez-Monterrey I, Beaumont A, Nemecek P, Roques BP, Fournie-Zaluski MC.
J Med Chem (1994) 37 : 1865 -1873
PubMed 8021926 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.80 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55286 1 8.44
CHEMBL47289 1 7.75
CHEMBL54601 1 7.36
CHEMBL54942 1 6.89
CHEMBL301703 1 6.82
CHEMBL293794 1 6.72
CHEMBL55583 1 6.66
CHEMBL55103 1 6.66
CHEMBL53141 1 6.60
CHEMBL54823 1 6.58
CHEMBL55721 1 6.57
CHEMBL54477 1 6.54
CHEMBL55520 1 6.50
CHEMBL54457 1 6.50
CHEMBL55613 1 6.46
CHEMBL54796 1 6.46
CHEMBL53621 1 6.44
CHEMBL53678 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55286 IC50 = 3.6 nM 8.44
CHEMBL47289 IC50 = 18.0 nM 7.75
CHEMBL54601 IC50 = 44.0 nM 7.36
CHEMBL54942 IC50 = 130.0 nM 6.89
CHEMBL301703 IC50 = 150.0 nM 6.82
CHEMBL293794 IC50 = 190.0 nM 6.72
CHEMBL55583 IC50 = 220.0 nM 6.66
CHEMBL55103 IC50 = 220.0 nM 6.66
CHEMBL53141 IC50 = 250.0 nM 6.60
CHEMBL54823 IC50 = 260.0 nM 6.58
CHEMBL55721 IC50 = 270.0 nM 6.57
CHEMBL54477 IC50 = 290.0 nM 6.54
CHEMBL55520 IC50 = 320.0 nM 6.50
CHEMBL54457 IC50 = 320.0 nM 6.50
CHEMBL55613 IC50 = 350.0 nM 6.46
CHEMBL54796 IC50 = 350.0 nM 6.46
CHEMBL53621 IC50 = 360.0 nM 6.44
CHEMBL53678 IC50 = 380.0 nM 6.42