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Assay Detail

CHEMBL652310

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

Binding
In vitro inhibition of [125I]AII specific binding towards Angiotensin II receptor in rat mesenteric 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-2 angiotensin II receptor (CHEMBL257)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1-(carboxybenzyl)imidazole-5-acrylic acids: potent and selective angiotensin II receptor antagonists.
Weinstock J, Keenan RM, Samanen J, Hempel J, Finkelstein JA, Franz RG, Gaitanopoulos DE, Girard GR, Gleason JG, Hill DT.
J Med Chem (1991) 34 : 1514 -1517
PubMed 2016730 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.44 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL813 EPROSARTAN 4.0 1 9.00
CHEMBL216061 1 8.89
CHEMBL40089 1 7.68
CHEMBL291086 1 7.51
CHEMBL289543 1 6.36
CHEMBL287762 1 6.21
CHEMBL36846 1 5.58
CHEMBL39349 1 5.22
CHEMBL291114 1 5.05
CHEMBL39345 1 4.92
CHEMBL25528 1 4.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL813 EPROSARTAN IC50 = 1.0 nM 9.00
CHEMBL216061 IC50 = 1.3 nM 8.89
CHEMBL40089 IC50 = 21.0 nM 7.68
CHEMBL291086 IC50 = 31.0 nM 7.51
CHEMBL289543 IC50 = 440.0 nM 6.36
CHEMBL287762 IC50 = 620.0 nM 6.21
CHEMBL36846 IC50 = 2600.0 nM 5.58
CHEMBL39349 IC50 = 6000.0 nM 5.22
CHEMBL291114 IC50 = 8900.0 nM 5.05
CHEMBL39345 IC50 = 12000.0 nM 4.92
CHEMBL25528 IC50 = 43000.0 nM 4.37