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Assay Detail

CHEMBL648955

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

Binding
Binding affinity towards Angiotensin II receptor, type 1 in rat liver membrane using [125I]-angiotensin II (0.1 nM)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Angiotensin II receptor (AT-1) type-1 (CHEMBL2094250)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Development of tetrazole bioisosteres in angiotensin II antagonists
Ferrari B, Taillades J, Perreaut P, Bernhart C, Gougat J, Guiraudou P, Cazaubon C, Roccon A, Nisato D, Le Fur G, Breliere J
Bioorg Med Chem Lett (1994) 4 : 45 -50
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.03 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL357878 1 9.15
CHEMBL1513 IRBESARTAN 4.0 1 8.89
CHEMBL343261 1 8.85
CHEMBL148434 1 8.77
CHEMBL47810 1 8.28
CHEMBL907 CARBOXYLIC ACID METABOLITE 1 7.85
CHEMBL144089 1 7.60
CHEMBL147598 1 7.22
CHEMBL148137 1 7.00
CHEMBL148379 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL357878 IC50 = 0.7 nM 9.15
CHEMBL1513 IRBESARTAN IC50 = 1.3 nM 8.89
CHEMBL343261 IC50 = 1.4 nM 8.85
CHEMBL148434 IC50 = 1.7 nM 8.77
CHEMBL47810 IC50 = 5.2 nM 8.28
CHEMBL907 CARBOXYLIC ACID METABOLITE IC50 = 14.0 nM 7.85
CHEMBL144089 IC50 = 25.0 nM 7.60
CHEMBL147598 IC50 = 60.0 nM 7.22
CHEMBL148137 IC50 = 100.0 nM 7.00
CHEMBL148379 IC50 = 230.0 nM 6.64