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Assay Detail

CHEMBL3586838

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

Binding
Inhibition of rabbit lung ACE assessed as hippuryl-histidyl-leucine hydrolysis after 30 mins by colorimetric method
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 Autocuration

Target

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

Publication

Design, synthesis and evaluation of novel 2-butyl-4-chloroimidazole derived peptidomimetics as Angiotensin Converting Enzyme (ACE) inhibitors.
Jallapally A, Addla D, Bagul P, Sridhar B, Banerjee SK, Kantevari S.
Bioorg Med Chem (2015) 23 : 3526 -3533
PubMed 25922179 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.56 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3585803 1 7.00
CHEMBL838 BENAZEPRIL 4.0 1 7.00
CHEMBL1592 QUINAPRIL 4.0 1 6.96
CHEMBL578 ENALAPRIL 4.0 1 6.91
CHEMBL1168 RAMIPRIL 4.0 1 6.60
CHEMBL1237 LISINOPRIL ANHYDROUS 4.0 1 6.50
CHEMBL3585794 1 6.28
CHEMBL3585792 1 6.19
CHEMBL3585802 1 6.18
CHEMBL3585799 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3585803 IC50 = 100.0 nM 7.00
CHEMBL838 BENAZEPRIL IC50 = 100.0 nM 7.00
CHEMBL1592 QUINAPRIL IC50 = 110.0 nM 6.96
CHEMBL578 ENALAPRIL IC50 = 123.0 nM 6.91
CHEMBL1168 RAMIPRIL IC50 = 253.0 nM 6.60
CHEMBL1237 LISINOPRIL ANHYDROUS IC50 = 318.0 nM 6.50
CHEMBL3585794 IC50 = 531.0 nM 6.28
CHEMBL3585792 IC50 = 647.0 nM 6.19
CHEMBL3585802 IC50 = 657.0 nM 6.18
CHEMBL3585799 IC50 = 1120.0 nM 5.95