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Assay Detail

CHEMBL648954

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

Binding
Displacement of [125-I]-labeled angiotensin II from Angiotensin II receptor, type 1 of rat uterine membranes
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Discovery of nonpeptide potent conformationally restricted angiotensin II receptor antagonists
Huang H, Chamberlain TS, Olins GM, Corpus VM, Chen ST, McMahon EG, Palomo MA, Blaine EH, Manning RE
Bioorg Med Chem Lett (1994) 4 : 2591 -2596
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.10 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL87778 1 8.30
CHEMBL86764 1 6.30
CHEMBL327614 2 5.80
CHEMBL86558 1 4.35
CHEMBL313239 1 -
CHEMBL89998 1 -
CHEMBL313448 1 -
CHEMBL89246 1 -
CHEMBL315924 1 -
CHEMBL87356 1 -
CHEMBL87378 1 -
CHEMBL313945 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL87778 IC50 = 5.0 nM 8.30
CHEMBL86764 IC50 = 500.0 nM 6.30
CHEMBL327614 IC50 = 1600.0 nM 5.80
CHEMBL327614 IC50 = 1800.0 nM 5.75
CHEMBL86558 IC50 = 45000.0 nM 4.35
CHEMBL313239 IC50 > 10000.0 nM -
CHEMBL89998 IC50 > 10000.0 nM -
CHEMBL313448 IC50 > 10000.0 nM -
CHEMBL89246 IC50 > 10000.0 nM -
CHEMBL315924 IC50 > 10000.0 nM -
CHEMBL87356 IC50 > 10000.0 nM -
CHEMBL87378 IC50 > 10000.0 nM -
CHEMBL313945 IC50 > 10000.0 nM -