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Assay Detail

CHEMBL884033

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

Binding
Tested for inhibitory concentration against AT1 receptor binding affinity in rat liver
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Angiotensin II receptor (AT-1) type-1 (CHEMBL2094250)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Nonpeptide angiotensin II receptor antagonists. 2. Design, synthesis, and structure-activity relationships of 2-alkyl-4-(1H-pyrrol-1-yl)-1H-imidazole derivatives: profile of 2-propyl-1-[[2'-(1H-tetrazol-5-yl)-[1,1' -biphenyl]-4-yl]-methyl]-4-[2-(trifluoroacetyl)-1H-pyrrol-1-yl]-1H- imidazole-5-carboxylic acid (CI-996).
Sircar I, Hodges JC, Quin J, Bunker AM, Winters RT, Edmunds JJ, Kostlan CR, Connolly C, Kesten SJ, Hamby JM.
J Med Chem (1993) 36 : 2253 -2265
PubMed 8360871 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.52 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL907 CARBOXYLIC ACID METABOLITE 1 8.80
CHEMBL443269 1 8.47
CHEMBL191 LOSARTAN 4.0 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL907 CARBOXYLIC ACID METABOLITE IC50 = 1.6 nM 8.80
CHEMBL443269 IC50 = 3.4 nM 8.47
CHEMBL191 LOSARTAN IC50 = 5.0 nM 8.30