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Assay Detail

CHEMBL755096

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

Binding
In vivo inhibitory potency against neutral endopeptidase by displacement of [3H]HACBOGly binding in mouse kidney
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Neprilysin (CHEMBL1944)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New dual inhibitors of neutral endopeptidase and angiotensin-converting enzyme: rational design, bioavailability, and pharmacological responses in experimental hypertension.
Fournié-Zaluski MC, Coric P, Turcaud S, Rousselet N, Gonzalez W, Barbe B, Pham I, Jullian N, Michel JB, Roques BP.
J Med Chem (1994) 37 : 1070 -1083
PubMed 8164250 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 8.31 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273748 1 8.89
CHEMBL11495 1 8.70
CHEMBL11620 1 8.70
CHEMBL11297 1 8.70
CHEMBL2051773 1 8.70
CHEMBL267766 1 8.62
CHEMBL11616 1 8.60
CHEMBL11537 1 8.51
CHEMBL273898 1 8.46
CHEMBL276008 1 8.46
CHEMBL11236 1 8.40
CHEMBL275690 1 8.40
CHEMBL11607 1 8.28
CHEMBL273724 1 8.23
CHEMBL6915 1 8.20
CHEMBL11227 1 8.05
CHEMBL416522 1 7.96
CHEMBL275980 1 7.82
CHEMBL273672 1 7.80
CHEMBL11806 1 7.80
CHEMBL11344 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273748 IC50 = 1.3 nM 8.89
CHEMBL11495 IC50 = 2.0 nM 8.70
CHEMBL11620 IC50 = 2.0 nM 8.70
CHEMBL11297 IC50 = 2.0 nM 8.70
CHEMBL2051773 IC50 = 2.0 nM 8.70
CHEMBL267766 IC50 = 2.4 nM 8.62
CHEMBL11616 IC50 = 2.5 nM 8.60
CHEMBL11537 IC50 = 3.1 nM 8.51
CHEMBL273898 IC50 = 3.5 nM 8.46
CHEMBL276008 IC50 = 3.5 nM 8.46
CHEMBL11236 IC50 = 4.0 nM 8.40
CHEMBL275690 IC50 = 4.0 nM 8.40
CHEMBL11607 IC50 = 5.2 nM 8.28
CHEMBL273724 IC50 = 5.9 nM 8.23
CHEMBL6915 IC50 = 6.3 nM 8.20
CHEMBL11227 IC50 = 9.0 nM 8.05
CHEMBL416522 IC50 = 11.0 nM 7.96
CHEMBL275980 IC50 = 15.0 nM 7.82
CHEMBL273672 IC50 = 16.0 nM 7.80
CHEMBL11806 IC50 = 16.0 nM 7.80
CHEMBL11344 IC50 = 65.0 nM 7.19