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Assay Detail

CHEMBL643765

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Binding
In vitro activity against angiotensin I converting enzyme especially against Hip-His-Leu residues
9
Total Activities
9
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

Configuration and preferential solid-state conformations of perindoprilat (S-9780). Comparison with the crystal structures of other ACE inhibitors and conclusions related to structure-activity relationships.
Pascard C, Guilhem J, Vincent M, Rémond G, Portevin B, Laubie M.
J Med Chem (1991) 34 : 663 -669
PubMed 1995891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.54 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL577 ENALAPRILAT ANHYDROUS 4.0 1 8.92
CHEMBL347863 1 8.82
CHEMBL161170 1 8.82
CHEMBL2371228 1 8.72
CHEMBL162360 1 7.64
CHEMBL161660 1 6.70
CHEMBL2371229 1 6.64
CHEMBL349119 1 5.96
CHEMBL348537 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL577 ENALAPRILAT ANHYDROUS IC50 = 1.2 nM 8.92
CHEMBL347863 IC50 = 1.5 nM 8.82
CHEMBL161170 IC50 = 1.5 nM 8.82
CHEMBL2371228 IC50 = 1.9 nM 8.72
CHEMBL162360 IC50 = 23.0 nM 7.64
CHEMBL161660 IC50 = 200.0 nM 6.70
CHEMBL2371229 IC50 = 230.0 nM 6.64
CHEMBL349119 IC50 = 1100.0 nM 5.96
CHEMBL348537 IC50 = 2500.0 nM 5.60