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Assay Detail

CHEMBL643770

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

Binding
In vitro inhibitory activity against Angiotensin I converting enzyme (ACE) isolated from rabbit lung extract using hippuryl-L-histidyl-L-leucine (HHL) as the substrate
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Angiotensin-converting enzyme (CHEMBL4074)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Vasopeptidase inhibitors: incorporation of geminal and spirocyclic substituted azepinones in mercaptoacyl dipeptides.
Robl JA, Sulsky R, Sieber-McMaster E, Ryono DE, Cimarusti MP, Simpkins LM, Karanewsky DS, Chao S, Asaad MM, Seymour AA, Fox M, Smith PL, Trippodo NC.
J Med Chem (1999) 42 : 305 -311
PubMed 9925736 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.94 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289556 OMAPATRILAT 2.0 1 8.30
CHEMBL319237 1 8.22
CHEMBL104054 1 8.09
CHEMBL430484 1 8.02
CHEMBL107747 GEMOPATRILAT 2.0 1 7.92
CHEMBL318096 1 7.80
CHEMBL299169 1 7.66
CHEMBL107275 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289556 OMAPATRILAT IC50 = 5.0 nM 8.30
CHEMBL319237 IC50 = 6.0 nM 8.22
CHEMBL104054 IC50 = 8.2 nM 8.09
CHEMBL430484 IC50 = 9.6 nM 8.02
CHEMBL107747 GEMOPATRILAT IC50 = 12.0 nM 7.92
CHEMBL318096 IC50 = 16.0 nM 7.80
CHEMBL299169 IC50 = 22.0 nM 7.66
CHEMBL107275 IC50 = 29.0 nM 7.54