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Assay Detail

CHEMBL652349

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

Binding
Inhibition of [125-I]-labeled angiotensin II binding to AT1 receptor in rat uterine membranes
11
Total Activities
11
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 11 7.32 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL315219 1 7.96
CHEMBL316392 1 7.82
CHEMBL86935 1 7.20
CHEMBL313239 1 6.92
CHEMBL88014 1 6.72
CHEMBL263967 1 -
CHEMBL314799 1 -
CHEMBL191 LOSARTAN 4.0 1 -
CHEMBL313945 1 -
CHEMBL314861 1 -
CHEMBL84849 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL315219 IC50 = 11.0 nM 7.96
CHEMBL316392 IC50 = 15.0 nM 7.82
CHEMBL86935 IC50 = 63.0 nM 7.20
CHEMBL313239 IC50 = 120.0 nM 6.92
CHEMBL88014 IC50 = 190.0 nM 6.72
CHEMBL263967 IC50 > 10000.0 nM -
CHEMBL314799 IC50 > 10000.0 nM -
CHEMBL191 LOSARTAN IC50 > 10000.0 nM -
CHEMBL313945 IC50 > 10000.0 nM -
CHEMBL314861 IC50 > 10000.0 nM -
CHEMBL84849 IC50 > 10000.0 nM -