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Assay Detail

CHEMBL751022

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

Binding
Inhibition of neutral endopeptidase (NEP) 24.11
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Neprilysin (CHEMBL3369)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

-Mercaptoacyl dipeptides that inhibit angiotensin converting enzyme and neutral endopeptidase 24.11
Bhagwat SS, Fink CA, Gude C, Chan K, Qiao Y, Sakane Y, Berry C, Ghai RD
Bioorg Med Chem Lett (1995) 5 : 735 -738
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.79 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL358338 1 7.55
CHEMBL163182 1 7.48
CHEMBL161879 1 7.37
CHEMBL351878 1 7.23
CHEMBL163454 1 7.00
CHEMBL165888 1 6.93
CHEMBL163468 1 6.65
CHEMBL349594 1 6.42
CHEMBL163621 1 6.30
CHEMBL166083 1 6.23
CHEMBL350414 1 6.18
CHEMBL423635 1 6.15
CHEMBL350378 1 -
CHEMBL351318 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL358338 IC50 = 28.0 nM 7.55
CHEMBL163182 IC50 = 33.0 nM 7.48
CHEMBL161879 IC50 = 43.0 nM 7.37
CHEMBL351878 IC50 = 59.0 nM 7.23
CHEMBL163454 IC50 = 100.0 nM 7.00
CHEMBL165888 IC50 = 117.0 nM 6.93
CHEMBL163468 IC50 = 222.0 nM 6.65
CHEMBL349594 IC50 = 385.0 nM 6.42
CHEMBL163621 IC50 = 500.0 nM 6.30
CHEMBL166083 IC50 = 583.0 nM 6.23
CHEMBL350414 IC50 = 654.0 nM 6.18
CHEMBL423635 IC50 = 705.0 nM 6.15
CHEMBL350378 IC50 > 1000.0 nM -
CHEMBL351318 IC50 > 1000.0 nM -