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Assay Detail

CHEMBL648940

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

Binding
Compound was tested for inhibitory activity against angiotensin I converting enzyme
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Angiotensin-converting enzyme (CHEMBL2625)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis, and physicochemical properties of a novel, conformationally restricted 2,3-dihydro-1,3,4-thiadiazole-containing angiotensin converting enzyme inhibitor which is preferentially eliminated by the biliary route in rats.
Bennion C, Brown RC, Cook AR, Manners CN, Payling DW, Robinson DH.
J Med Chem (1991) 34 : 439 -447
PubMed 1992145 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 9.10 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL342372 UTIBAPRILAT 2.0 1 9.29
CHEMBL138409 1 9.22
CHEMBL139140 1 9.15
CHEMBL577 ENALAPRILAT ANHYDROUS 4.0 1 9.02
CHEMBL423916 1 8.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL342372 UTIBAPRILAT IC50 = 0.51 nM 9.29
CHEMBL138409 IC50 = 0.6 nM 9.22
CHEMBL139140 IC50 = 0.7 nM 9.15
CHEMBL577 ENALAPRILAT ANHYDROUS IC50 = 0.95 nM 9.02
CHEMBL423916 IC50 = 1.5 nM 8.82