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Assay Detail

CHEMBL752507

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Binding
In vitro inhibition of rat neutral endopeptidase
32
Total Activities
28
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

Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.
De Lombaert S, Blanchard L, Stamford LB, Tan J, Wallace EM, Satoh Y, Fitt J, Hoyer D, Simonsbergen D, Moliterni J, Marcopoulos N, Savage P, Chou M, Trapani AJ, Jeng AY.
J Med Chem (2000) 43 : 488 -504
PubMed 10669576 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 6.18 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290698 1 9.00
CHEMBL147157 1 8.57
CHEMBL10247 THIORPHAN -1.0 1 8.32
CHEMBL285619 1 8.30
CHEMBL413724 1 7.92
CHEMBL40028 1 7.85
CHEMBL479579 PHOSPHORAMIDON 1 7.52
CHEMBL357226 1 7.51
CHEMBL148056 1 6.94
CHEMBL147041 1 6.85
CHEMBL147964 2 6.68
CHEMBL147163 1 6.64
CHEMBL343904 1 6.35
CHEMBL359437 1 5.79
CHEMBL146936 1 5.64
CHEMBL147847 1 5.24
CHEMBL423751 2 5.19
CHEMBL289150 1 5.17
CHEMBL357251 1 4.86
CHEMBL358098 1 4.82
CHEMBL342962 1 4.75
CHEMBL342077 2 4.55
CHEMBL359024 2 4.32
CHEMBL148232 1 -
CHEMBL357441 1 -
CHEMBL358774 1 -
CHEMBL145943 1 -
CHEMBL147730 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290698 IC50 = 1.0 nM 9.00
CHEMBL147157 IC50 = 2.7 nM 8.57
CHEMBL10247 THIORPHAN IC50 = 4.8 nM 8.32
CHEMBL285619 IC50 = 5.0 nM 8.30
CHEMBL413724 IC50 = 12.0 nM 7.92
CHEMBL40028 IC50 = 14.0 nM 7.85
CHEMBL479579 PHOSPHORAMIDON IC50 = 30.0 nM 7.52
CHEMBL357226 IC50 = 31.0 nM 7.51
CHEMBL148056 IC50 = 114.0 nM 6.94
CHEMBL147041 IC50 = 140.0 nM 6.85
CHEMBL147964 IC50 = 210.0 nM 6.68
CHEMBL147163 IC50 = 230.0 nM 6.64
CHEMBL343904 IC50 = 450.0 nM 6.35
CHEMBL359437 IC50 = 1640.0 nM 5.79
CHEMBL146936 IC50 = 2300.0 nM 5.64
CHEMBL147847 IC50 = 5800.0 nM 5.24
CHEMBL423751 IC50 = 6400.0 nM 5.19
CHEMBL289150 IC50 = 6700.0 nM 5.17
CHEMBL147964 IC50 = 13000.0 nM 4.89
CHEMBL357251 IC50 = 13770.0 nM 4.86
CHEMBL358098 IC50 = 15000.0 nM 4.82
CHEMBL342962 IC50 = 18000.0 nM 4.75
CHEMBL423751 IC50 = 24000.0 nM 4.62
CHEMBL342077 IC50 = 28000.0 nM 4.55
CHEMBL342077 IC50 = 47000.0 nM 4.33
CHEMBL359024 IC50 = 48000.0 nM 4.32
CHEMBL359024 IC50 = 59000.0 nM 4.23
CHEMBL148232 IC50 > 16000.0 nM -
CHEMBL357441 IC50 > 10000.0 nM -
CHEMBL358774 IC50 > 10000.0 nM -
CHEMBL145943 IC50 > 100000.0 nM -
CHEMBL147730 IC50 > 10000.0 nM -