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Assay Detail

CHEMBL643790

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

Binding
In vitro binding affinity at Angiotensin II Type 2 receptor in rabbit uterus membrane by [125I]AII displacement.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Uterus
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Type-2 angiotensin II receptor (CHEMBL4607)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Balanced AT1 and AT2 angiotensin II antagonists. II. Potent 5 -hydroxyacid imidazolyl biphenyl sulfonylureas
Deprez P, Guillaume J, Corbier A, Fortin M, Vevert J, Heckmann B
Bioorg Med Chem Lett (1995) 5 : 2611 -2616
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.90 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432378 1 9.05
CHEMBL314506 1 8.96
CHEMBL314827 1 8.96
CHEMBL89053 1 8.96
CHEMBL81236 1 8.72
CHEMBL315327 1 8.70
CHEMBL88446 1 8.68
CHEMBL316021 1 8.41
CHEMBL275449 1 8.33
CHEMBL89052 1 8.30
CHEMBL86617 1 8.25
CHEMBL89463 1 8.10
CHEMBL315275 1 8.09
CHEMBL313073 1 8.04
CHEMBL315994 1 7.82
CHEMBL89769 1 7.42
CHEMBL328480 1 7.36
CHEMBL330744 1 6.92
CHEMBL80370 1 6.04
CHEMBL313005 1 5.46
CHEMBL330302 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432378 IC50 = 0.9 nM 9.05
CHEMBL314506 IC50 = 1.1 nM 8.96
CHEMBL314827 IC50 = 1.1 nM 8.96
CHEMBL89053 IC50 = 1.1 nM 8.96
CHEMBL81236 IC50 = 1.9 nM 8.72
CHEMBL315327 IC50 = 2.0 nM 8.70
CHEMBL88446 IC50 = 2.1 nM 8.68
CHEMBL316021 IC50 = 3.9 nM 8.41
CHEMBL275449 IC50 = 4.7 nM 8.33
CHEMBL89052 IC50 = 5.0 nM 8.30
CHEMBL86617 IC50 = 5.6 nM 8.25
CHEMBL89463 IC50 = 8.0 nM 8.10
CHEMBL315275 IC50 = 8.2 nM 8.09
CHEMBL313073 IC50 = 9.1 nM 8.04
CHEMBL315994 IC50 = 15.0 nM 7.82
CHEMBL89769 IC50 = 38.0 nM 7.42
CHEMBL328480 IC50 = 44.0 nM 7.36
CHEMBL330744 IC50 = 120.0 nM 6.92
CHEMBL80370 IC50 = 920.0 nM 6.04
CHEMBL313005 IC50 = 3500.0 nM 5.46
CHEMBL330302 IC50 = 3800.0 nM 5.42