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Assay Detail

CHEMBL648853

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

Binding
In vitro binding affinity towards Angiotensin II type 1-AT1 receptor determined as its ability to displace 125I-Sarl,Ile8-AII from the receptor expressed in rabbit aorta membrane.
5
Total Activities
5
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

Angiotensin II receptor antagonists containing a phenylpyridine element.
Mantlo N, Chang RS, Siegl P
Bioorg Med Chem Lett (1993) 3 : 1693 -1696
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.17 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7550 L-158809 1 9.30
CHEMBL296725 1 9.00
CHEMBL47382 1 8.40
CHEMBL47459 1 7.22
CHEMBL410939 1 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7550 L-158809 IC50 = 0.5 nM 9.30
CHEMBL296725 IC50 = 1.0 nM 9.00
CHEMBL47382 IC50 = 4.0 nM 8.40
CHEMBL47459 IC50 = 60.0 nM 7.22
CHEMBL410939 IC50 = 116.0 nM 6.94