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Assay Detail

CHEMBL644417

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

Binding
Inhibitory activity against rabbit lung Angiotensin I converting enzyme with 5 mM hippuryl-histidyl-leucine as substrate
10
Total Activities
10
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

Angiotensin-converting enzyme inhibitors: perhydro-1,4-thiazepin-5-one derivatives.
Yanagisawa H, Ishihara S, Ando A, Kanazaki T, Miyamoto S, Koike H, Iijima Y, Oizumi K, Matsushita Y, Hata T.
J Med Chem (1987) 30 : 1984 -1991
PubMed 3669006 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.93 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL302181 1 8.55
CHEMBL300560 1 8.47
CHEMBL300841 TEMOCAPRILAT 2.0 1 8.44
CHEMBL59172 1 8.43
CHEMBL293765 1 8.39
CHEMBL577 ENALAPRILAT ANHYDROUS 4.0 1 8.24
CHEMBL61439 1 7.45
CHEMBL60108 1 7.19
CHEMBL292565 1 7.11
CHEMBL291810 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL302181 IC50 = 2.8 nM 8.55
CHEMBL300560 IC50 = 3.4 nM 8.47
CHEMBL300841 TEMOCAPRILAT IC50 = 3.6 nM 8.44
CHEMBL59172 IC50 = 3.7 nM 8.43
CHEMBL293765 IC50 = 4.1 nM 8.39
CHEMBL577 ENALAPRILAT ANHYDROUS IC50 = 5.7 nM 8.24
CHEMBL61439 IC50 = 35.5 nM 7.45
CHEMBL60108 IC50 = 64.7 nM 7.19
CHEMBL292565 IC50 = 78.2 nM 7.11
CHEMBL291810 IC50 = 86.9 nM 7.06