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Assay Detail

CHEMBL648759

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

Binding
In vitro inhibition of specific binding of [125I]AII to Angiotensin II receptor, type 1 from rat liver membrane
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Liver
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Type-1 angiotensin II receptor B (CHEMBL263)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Cyclopentanespiro-3H-dihydro-pyrimidinones as Angiotensin II AT1 receptor antagonists
Bernhart C, Hundricourt F, Assens J, Gougat J, Lacour C, Roccon A, Cazaubon C, Breliere J, Le Fur G, Nisato D
Bioorg Med Chem Lett (1994) 4 : 157 -162
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.81 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42200 1 9.00
CHEMBL1513 IRBESARTAN 4.0 1 8.89
CHEMBL40251 1 8.66
CHEMBL40250 1 7.28
CHEMBL295646 1 7.15
CHEMBL295181 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42200 IC50 = 1.0 nM 9.00
CHEMBL1513 IRBESARTAN IC50 = 1.3 nM 8.89
CHEMBL40251 IC50 = 2.2 nM 8.66
CHEMBL40250 IC50 = 53.0 nM 7.28
CHEMBL295646 IC50 = 71.0 nM 7.15
CHEMBL295181 IC50 = 1300.0 nM 5.89