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Assay Detail

CHEMBL770909

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

Functional
Antagonistic activity through inhibition of A II induced contractions on rabbit aortic strips
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 1 — Organism
Curated By Expert

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

Publication

A new series of imidazolones: highly specific and potent nonpeptide AT1 angiotensin II receptor antagonists.
Bernhart CA, Perreaut PM, Ferrari BP, Muneaux YA, Assens JL, Clément J, Haudricourt F, Muneaux CF, Taillades JE, Vignal MA.
J Med Chem (1993) 36 : 3371 -3380
PubMed 8230127 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 6.71 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL938 SARALASIN 4.0 1 8.64
CHEMBL1513 IRBESARTAN 4.0 1 8.40
CHEMBL325201 1 7.92
CHEMBL324452 1 7.64
CHEMBL191 LOSARTAN 4.0 1 7.60
CHEMBL419583 1 7.57
CHEMBL116170 1 7.42
CHEMBL114656 1 7.41
CHEMBL113674 1 7.38
CHEMBL327018 1 7.28
CHEMBL114267 1 7.28
CHEMBL439968 1 7.20
CHEMBL114720 1 7.16
CHEMBL114710 1 7.10
CHEMBL44268 1 6.96
CHEMBL114687 1 6.96
CHEMBL290988 1 6.92
CHEMBL115984 1 6.89
CHEMBL325445 1 6.70
CHEMBL115193 1 6.70
CHEMBL114983 1 6.62
CHEMBL113039 1 6.60
CHEMBL296883 1 6.57
CHEMBL325684 1 6.47
CHEMBL323244 1 6.47
CHEMBL324245 1 6.46
CHEMBL112343 1 6.38
CHEMBL115492 1 6.32
CHEMBL324785 1 6.22
CHEMBL114771 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL938 SARALASIN IC50 = 2.3 nM 8.64
CHEMBL1513 IRBESARTAN IC50 = 4.0 nM 8.40
CHEMBL325201 IC50 = 12.0 nM 7.92
CHEMBL324452 IC50 = 23.0 nM 7.64
CHEMBL191 LOSARTAN IC50 = 25.0 nM 7.60
CHEMBL419583 IC50 = 27.0 nM 7.57
CHEMBL116170 IC50 = 38.0 nM 7.42
CHEMBL114656 IC50 = 39.0 nM 7.41
CHEMBL113674 IC50 = 42.0 nM 7.38
CHEMBL327018 IC50 = 52.0 nM 7.28
CHEMBL114267 IC50 = 52.0 nM 7.28
CHEMBL439968 IC50 = 63.0 nM 7.20
CHEMBL114720 IC50 = 70.0 nM 7.16
CHEMBL114710 IC50 = 80.0 nM 7.10
CHEMBL114687 IC50 = 110.0 nM 6.96
CHEMBL44268 IC50 = 110.0 nM 6.96
CHEMBL290988 IC50 = 120.0 nM 6.92
CHEMBL115984 IC50 = 130.0 nM 6.89
CHEMBL325445 IC50 = 200.0 nM 6.70
CHEMBL115193 IC50 = 200.0 nM 6.70
CHEMBL114983 IC50 = 240.0 nM 6.62
CHEMBL113039 IC50 = 250.0 nM 6.60
CHEMBL296883 IC50 = 270.0 nM 6.57
CHEMBL325684 IC50 = 340.0 nM 6.47
CHEMBL323244 IC50 = 340.0 nM 6.47
CHEMBL324245 IC50 = 350.0 nM 6.46
CHEMBL112343 IC50 = 420.0 nM 6.38
CHEMBL115492 IC50 = 480.0 nM 6.32
CHEMBL324785 IC50 = 600.0 nM 6.22
CHEMBL114771 IC50 = 1600.0 nM 5.80
CHEMBL115771 IC50 = 3900.0 nM 5.41
CHEMBL46782 IC50 = 4000.0 nM 5.40
CHEMBL325751 IC50 = 4000.0 nM 5.40
CHEMBL45493 IC50 = 5100.0 nM 5.29
CHEMBL423325 IC50 = 5300.0 nM 5.28
CHEMBL324888 IC50 = 5400.0 nM 5.27
CHEMBL113701 IC50 = 5900.0 nM 5.23
CHEMBL115835 IC50 > 10000.0 nM -
CHEMBL410724 IC50 > 10000.0 nM -
CHEMBL325502 IC50 > 10000.0 nM -
CHEMBL332051 IC50 > 10000.0 nM -