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Assay Detail

CHEMBL647116

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

Binding
Inhibitory potency against angiotensin converting enzyme by displacement of [3H]trandolaprilate binding in mouse lung
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Angiotensin-converting enzyme (CHEMBL2994)
Type SINGLE PROTEIN
Organism Mus musculus

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 22 7.88 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273853 1 8.44
CHEMBL275690 1 8.40
CHEMBL11806 1 8.40
CHEMBL11616 1 8.37
CHEMBL11607 1 8.35
CHEMBL276008 1 8.30
CHEMBL6915 1 8.27
CHEMBL273724 1 8.16
CHEMBL11537 1 8.15
CHEMBL11227 1 8.10
CHEMBL11620 1 8.02
CHEMBL11297 1 8.00
CHEMBL273672 1 7.92
CHEMBL11344 1 7.85
CHEMBL273898 1 7.72
CHEMBL2051773 1 7.70
CHEMBL11495 1 7.60
CHEMBL273748 1 7.50
CHEMBL11236 1 7.37
CHEMBL275980 1 7.00
CHEMBL267766 1 6.96
CHEMBL416522 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273853 IC50 = 3.6 nM 8.44
CHEMBL275690 IC50 = 4.0 nM 8.40
CHEMBL11806 IC50 = 4.0 nM 8.40
CHEMBL11616 IC50 = 4.3 nM 8.37
CHEMBL11607 IC50 = 4.5 nM 8.35
CHEMBL276008 IC50 = 5.0 nM 8.30
CHEMBL6915 IC50 = 5.4 nM 8.27
CHEMBL273724 IC50 = 6.9 nM 8.16
CHEMBL11537 IC50 = 7.0 nM 8.15
CHEMBL11227 IC50 = 7.9 nM 8.10
CHEMBL11620 IC50 = 9.5 nM 8.02
CHEMBL11297 IC50 = 10.0 nM 8.00
CHEMBL273672 IC50 = 12.0 nM 7.92
CHEMBL11344 IC50 = 14.0 nM 7.85
CHEMBL273898 IC50 = 19.0 nM 7.72
CHEMBL2051773 IC50 = 20.0 nM 7.70
CHEMBL11495 IC50 = 25.0 nM 7.60
CHEMBL273748 IC50 = 32.0 nM 7.50
CHEMBL11236 IC50 = 43.0 nM 7.37
CHEMBL275980 IC50 = 100.0 nM 7.00
CHEMBL267766 IC50 = 110.0 nM 6.96
CHEMBL416522 IC50 = 210.0 nM 6.68