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Assay Detail

CHEMBL653122

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

Binding
Angiotensin II receptor antagonist activity was determined by 50% inhibition of specific binding of [3H]angiotensin II (2 nM) to rat adrenal cortical microsomes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Angiotensin II receptor (CHEMBL2094112)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

The preparation of (perfluoroalkyl)imidazoles as nonpeptide angiotensin II receptor antagonists
Carini DJ, Chiu AT, Wong PC, Johnson AL, Wexler RR, Timmermans PB
Bioorg Med Chem Lett (1993) 3 : 895 -898
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.49 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL170944 1 8.92
CHEMBL408403 ANGIOTENSIN II 4.0 1 8.70
CHEMBL171524 1 8.19
CHEMBL170208 1 7.89
CHEMBL995 LOSARTAN POTASSIUM 4.0 1 7.72
CHEMBL170281 1 7.32
CHEMBL173654 1 7.13
CHEMBL172765 1 6.89
CHEMBL352593 1 6.54
CHEMBL171136 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL170944 IC50 = 1.2 nM 8.92
CHEMBL408403 ANGIOTENSIN II IC50 = 2.0 nM 8.70
CHEMBL171524 IC50 = 6.4 nM 8.19
CHEMBL170208 IC50 = 13.0 nM 7.89
CHEMBL995 LOSARTAN POTASSIUM IC50 = 19.0 nM 7.72
CHEMBL170281 IC50 = 48.0 nM 7.32
CHEMBL173654 IC50 = 74.0 nM 7.13
CHEMBL172765 IC50 = 130.0 nM 6.89
CHEMBL352593 IC50 = 290.0 nM 6.54
CHEMBL171136 IC50 = 2500.0 nM 5.60