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Assay Detail

CHEMBL648764

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

Binding
In vitro binding affinity at Angiotensin II receptor, type 1 from rat liver membrane by [125I]- A II displacement.
17
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Dihydro-imidazolone derivatives as angiotensin II receptor antagonists: chiral effect on the activity
Perreaut P, Clement J, Muneaux C, Muneaux Y, Cazaubon C, Gougat J, Guiraudou P, Lacour C, Nisato D, Le Fur G, Breliere J
Bioorg Med Chem Lett (1994) 4 : 163 -168
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.39 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47428 1 8.48
CHEMBL47810 3 8.34
CHEMBL47669 1 8.14
CHEMBL47985 1 8.12
CHEMBL296492 1 7.92
CHEMBL45485 1 7.75
CHEMBL48062 1 7.72
CHEMBL290988 1 7.46
CHEMBL275437 1 7.28
CHEMBL296883 1 7.25
CHEMBL44268 1 7.10
CHEMBL297250 1 6.82
CHEMBL48392 1 6.64
CHEMBL46782 1 5.77
CHEMBL45493 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47428 IC50 = 3.3 nM 8.48
CHEMBL47810 IC50 = 4.6 nM 8.34
CHEMBL47810 IC50 = 5.2 nM 8.28
CHEMBL47669 IC50 = 7.3 nM 8.14
CHEMBL47985 IC50 = 7.6 nM 8.12
CHEMBL296492 IC50 = 12.0 nM 7.92
CHEMBL45485 IC50 = 18.0 nM 7.75
CHEMBL48062 IC50 = 19.0 nM 7.72
CHEMBL290988 IC50 = 35.0 nM 7.46
CHEMBL275437 IC50 = 52.0 nM 7.28
CHEMBL296883 IC50 = 56.0 nM 7.25
CHEMBL44268 IC50 = 80.0 nM 7.10
CHEMBL47810 IC50 = 110.0 nM 6.96
CHEMBL297250 IC50 = 150.0 nM 6.82
CHEMBL48392 IC50 = 230.0 nM 6.64
CHEMBL46782 IC50 = 1700.0 nM 5.77
CHEMBL45493 IC50 = 2100.0 nM 5.68