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Assay Detail

CHEMBL648849

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

Binding
Displacement of the specific binding ligand [125I]Sar1,Ile8-AII from Angiotensin II receptor, type 1 in rabbit aorta membrane.
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Type-1 angiotensin II receptor (CHEMBL3948)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Evaluation of heterocyclic acid equivalents as tetrazole replacements in imidazopyridine-based nonpeptide angiotensin II receptor antagonists
Kim D, Mantlo NB, Chang R, Kivlighn S, Greenlee W
Bioorg Med Chem Lett (1994) 4 : 41 -44
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.78 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7550 L-158809 1 9.52
CHEMBL344407 1 9.15
CHEMBL87842 1 8.42
CHEMBL424289 1 8.22
CHEMBL138358 1 8.19
CHEMBL441837 1 7.96
CHEMBL139739 1 7.24
CHEMBL337787 1 6.92
CHEMBL344388 1 6.26
CHEMBL136911 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7550 L-158809 IC50 = 0.3 nM 9.52
CHEMBL344407 IC50 = 0.7 nM 9.15
CHEMBL87842 IC50 = 3.8 nM 8.42
CHEMBL424289 IC50 = 6.0 nM 8.22
CHEMBL138358 IC50 = 6.5 nM 8.19
CHEMBL441837 IC50 = 11.0 nM 7.96
CHEMBL139739 IC50 = 57.0 nM 7.24
CHEMBL337787 IC50 = 120.0 nM 6.92
CHEMBL344388 IC50 = 550.0 nM 6.26
CHEMBL136911 IC50 = 1300.0 nM 5.89