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Assay Detail

CHEMBL2061970

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

Binding
Displacement of [125I]Sar1Ile8-Ang2 from angiotensin AT1 receptor after 180 mins by gamma counting
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Type-1 angiotensin II receptor (CHEMBL227)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological activity of 6-substituted carbamoyl benzimidazoles as new nonpeptidic angiotensin II AT₁ receptor antagonists.
Zhang J, Wang JL, Zhou ZM, Li ZH, Xue WZ, Xu D, Hao LP, Han XF, Fei F, Liu T, Liang AH.
Bioorg Med Chem (2012) 20 : 4208 -4216
PubMed 22727371 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.72 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2058860 1 9.05
CHEMBL1017 TELMISARTAN 4.0 1 9.00
CHEMBL2058859 1 8.89
CHEMBL2058861 1 8.59
CHEMBL2058864 1 8.43
CHEMBL191 LOSARTAN 4.0 1 7.79
CHEMBL2058855 1 7.71
CHEMBL2058862 1 7.65
CHEMBL2058865 1 7.42
CHEMBL2058856 1 7.11
CHEMBL2058863 1 7.11
CHEMBL2058858 1 7.01
CHEMBL2058857 1 6.93
CHEMBL2058866 1 6.68
CHEMBL2058588 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2058860 IC50 = 0.9 nM 9.05
CHEMBL1017 TELMISARTAN IC50 = 1.0 nM 9.00
CHEMBL2058859 IC50 = 1.3 nM 8.89
CHEMBL2058861 IC50 = 2.6 nM 8.59
CHEMBL2058864 IC50 = 3.7 nM 8.43
CHEMBL191 LOSARTAN IC50 = 16.2 nM 7.79
CHEMBL2058855 IC50 = 19.7 nM 7.71
CHEMBL2058862 IC50 = 22.5 nM 7.65
CHEMBL2058865 IC50 = 37.6 nM 7.42
CHEMBL2058856 IC50 = 78.3 nM 7.11
CHEMBL2058863 IC50 = 78.0 nM 7.11
CHEMBL2058858 IC50 = 96.8 nM 7.01
CHEMBL2058857 IC50 = 118.5 nM 6.93
CHEMBL2058866 IC50 = 209.0 nM 6.68
CHEMBL2058588 IC50 = 410.0 nM 6.39