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Assay Detail

CHEMBL747371

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

Binding
Evaluation of in vitro inhibitory activity against Neutral endopeptidase
23
Total Activities
23
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

New alpha-thiol dipeptide dual inhibitors of angiotensin-I converting enzyme and neutral endopeptidase EC 3.4.24.11.
Fink CA, Qiao Y, Berry CJ, Sakane Y, Ghai RD, Trapani AJ.
J Med Chem (1995) 38 : 5023 -5030
PubMed 8544178 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.30 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL358592 1 8.92
CHEMBL356123 1 8.82
CHEMBL320610 1 8.82
CHEMBL149364 1 8.74
CHEMBL146652 1 8.70
CHEMBL424497 1 8.68
CHEMBL343691 1 8.66
CHEMBL148911 1 8.59
CHEMBL147702 1 8.52
CHEMBL356343 1 8.52
CHEMBL356084 1 8.51
CHEMBL144549 1 8.30
CHEMBL435421 1 8.28
CHEMBL10247 THIORPHAN -1.0 1 8.27
CHEMBL147899 1 8.19
CHEMBL342321 1 8.06
CHEMBL144543 1 8.04
CHEMBL148368 1 7.82
CHEMBL342993 1 7.82
CHEMBL64081 1 7.80
CHEMBL147595 1 7.60
CHEMBL479579 PHOSPHORAMIDON 1 7.58
CHEMBL358338 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL358592 IC50 = 1.2 nM 8.92
CHEMBL356123 IC50 = 1.5 nM 8.82
CHEMBL320610 IC50 = 1.5 nM 8.82
CHEMBL149364 IC50 = 1.8 nM 8.74
CHEMBL146652 IC50 = 2.0 nM 8.70
CHEMBL424497 IC50 = 2.1 nM 8.68
CHEMBL343691 IC50 = 2.2 nM 8.66
CHEMBL148911 IC50 = 2.6 nM 8.59
CHEMBL147702 IC50 = 3.0 nM 8.52
CHEMBL356343 IC50 = 3.0 nM 8.52
CHEMBL356084 IC50 = 3.1 nM 8.51
CHEMBL144549 IC50 = 5.0 nM 8.30
CHEMBL435421 IC50 = 5.2 nM 8.28
CHEMBL10247 THIORPHAN IC50 = 5.4 nM 8.27
CHEMBL147899 IC50 = 6.4 nM 8.19
CHEMBL342321 IC50 = 8.7 nM 8.06
CHEMBL144543 IC50 = 9.2 nM 8.04
CHEMBL148368 IC50 = 15.0 nM 7.82
CHEMBL342993 IC50 = 15.0 nM 7.82
CHEMBL64081 IC50 = 16.0 nM 7.80
CHEMBL147595 IC50 = 25.0 nM 7.60
CHEMBL479579 PHOSPHORAMIDON IC50 = 26.0 nM 7.58
CHEMBL358338 IC50 = 28.0 nM 7.55