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Assay Detail

CHEMBL772962

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

Functional
In vitro antagonist activity was determined by the ability to antagonize the contractile response to angiotensin II in the isolated rabbit aortic strips
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

Publication

Synthesis and biological evaluation of new arylthiophene analogs of DuP 753
Estenne G, Dodey P, Renaut P, Leclerc G
Bioorg Med Chem Lett (1995) 5 : 15 -18
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.53 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191 LOSARTAN 4.0 1 8.21
CHEMBL274447 1 6.92
CHEMBL300882 1 6.48
CHEMBL50204 1 6.48
CHEMBL409552 1 5.70
CHEMBL50135 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191 LOSARTAN IC50 = 6.1 nM 8.21
CHEMBL274447 IC50 = 120.0 nM 6.92
CHEMBL300882 IC50 = 328.0 nM 6.48
CHEMBL50204 IC50 = 330.0 nM 6.48
CHEMBL409552 IC50 = 2000.0 nM 5.70
CHEMBL50135 IC50 = 4160.0 nM 5.38