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Assay Detail

CHEMBL646967

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

Binding
Inhibitory concentration was evaluated by inhibiting 50% of Angiotensin I Converting Enzyme activity using 50 uM N-Cbz-Phe-His-Leu as substrate
9
Total Activities
9
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 (CHEMBL1808)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploration of neutral endopeptidase active site by a series of new thiol-containing inhibitors.
Gomez-Monterrey I, Turcaud S, Lucas E, Bruetschy L, Roques BP, Fournié-Zaluski MC.
J Med Chem (1993) 36 : 87 -94
PubMed 8421293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.37 6.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL171850 1 6.15
CHEMBL175110 1 5.80
CHEMBL173919 1 5.40
CHEMBL54601 1 5.40
CHEMBL172787 1 5.35
CHEMBL174237 1 5.30
CHEMBL173287 1 5.00
CHEMBL2110258 1 5.00
CHEMBL55286 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL171850 IC50 = 710.0 nM 6.15
CHEMBL175110 IC50 = 1600.0 nM 5.80
CHEMBL173919 IC50 = 4000.0 nM 5.40
CHEMBL54601 IC50 = 4000.0 nM 5.40
CHEMBL172787 IC50 = 4500.0 nM 5.35
CHEMBL174237 IC50 = 5000.0 nM 5.30
CHEMBL173287 IC50 = 10000.0 nM 5.00
CHEMBL2110258 IC50 = 10000.0 nM 5.00
CHEMBL55286 IC50 = 12000.0 nM 4.92