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Assay Detail

CHEMBL1949358

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Functional
Antagonist activity at angiotensin 2 AT1 receptor in Japanese White rabbits thoracic aorta assessed as inhibition of KCl-indcuced contraction after 60 mins
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Thoracic aorta
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Type-1 angiotensin II receptor (CHEMBL3948)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Design, synthesis and biological evaluation of 6-substituted aminocarbonyl benzimidazole derivatives as nonpeptidic angiotensin II AT1 receptor antagonists.
Wang JL, Zhang J, Zhou ZM, Li ZH, Xue WZ, Xu D, Hao LP, Han XF, Fei F, Liu T, Liang AH.
Eur J Med Chem (2012) 49 : 183 -190
PubMed 22309912 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 8.22 8.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1945010 1 8.50
CHEMBL1947131 1 8.32
CHEMBL1947129 1 8.16
CHEMBL191 LOSARTAN 4.0 1 7.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1945010 Kd = 3.162 nM 8.50
CHEMBL1947131 Kd = 4.786 nM 8.32
CHEMBL1947129 Kd = 6.918 nM 8.16
CHEMBL191 LOSARTAN Kd = 12.59 nM 7.90