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Assay Detail

CHEMBL1949357

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

Binding
Displacement of [125I]Sar1 Ile8-Ang 2 from angiotensin 2 AT2 receptor after 180 mins by gamma counting
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Type-2 angiotensin II receptor (CHEMBL4607)
Type SINGLE PROTEIN
Organism Homo sapiens

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
IC50 12 6.34 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1017 TELMISARTAN 4.0 1 9.48
CHEMBL1947129 1 5.96
CHEMBL1945009 1 5.92
CHEMBL1945149 1 5.89
CHEMBL1945010 1 5.85
CHEMBL1945008 1 5.82
CHEMBL1947131 1 5.44
CHEMBL1947130 1 -
CHEMBL1945006 1 -
CHEMBL1945007 1 -
CHEMBL1945148 1 -
CHEMBL191 LOSARTAN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1017 TELMISARTAN IC50 = 0.33 nM 9.48
CHEMBL1947129 IC50 = 1100.0 nM 5.96
CHEMBL1945009 IC50 = 1200.0 nM 5.92
CHEMBL1945149 IC50 = 1300.0 nM 5.89
CHEMBL1945010 IC50 = 1400.0 nM 5.85
CHEMBL1945008 IC50 = 1500.0 nM 5.82
CHEMBL1947131 IC50 = 3600.0 nM 5.44
CHEMBL1947130 IC50 > 10000.0 nM -
CHEMBL1945006 IC50 > 10000.0 nM -
CHEMBL1945007 IC50 > 10000.0 nM -
CHEMBL1945148 IC50 - -
CHEMBL191 LOSARTAN IC50 > 10000.0 nM -