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Assay Detail

CHEMBL3739215

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

Binding
Displacement of 125I-labeled Sar1-Ile8-angiotensin II from human AT1 receptor incubated for 2 hrs by gamma counting analysis
33
Total Activities
33
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 4-[(benzimidazol-1-yl)methyl]biphenyl-2-sulphonamides as dual angiotensin II and endothelin A receptor antagonists
Hao L, Xue W, Han X, He X, Zhang J, Zhou Z
Medchemcomm (2015) 6 : 715 -718
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 7.38 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12233 1 8.89
CHEMBL12106 1 8.70
CHEMBL12013 1 8.70
CHEMBL11706 BMS-248360 1 8.22
CHEMBL3736242 1 8.15
CHEMBL275545 1 8.10
CHEMBL3735574 1 8.10
CHEMBL3734968 1 7.89
CHEMBL3735155 1 7.80
CHEMBL12333 1 7.68
CHEMBL417429 1 7.62
CHEMBL3735931 1 7.55
CHEMBL11528 1 7.52
CHEMBL3736037 1 7.51
CHEMBL3734870 1 7.43
CHEMBL3736248 1 7.38
CHEMBL3735236 1 7.33
CHEMBL3736262 1 7.30
CHEMBL3735151 1 7.25
CHEMBL3736414 1 7.12
CHEMBL3734835 1 7.09
CHEMBL3734955 1 7.04
CHEMBL3735302 1 7.03
CHEMBL3736507 1 7.02
CHEMBL3735265 1 6.82
CHEMBL3734829 1 6.80
CHEMBL3735036 1 6.70
CHEMBL3734849 1 6.66
CHEMBL3736310 1 6.47
CHEMBL3735797 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12233 IC50 = 1.3 nM 8.89
CHEMBL12106 IC50 = 2.0 nM 8.70
CHEMBL12013 IC50 = 2.0 nM 8.70
CHEMBL11706 BMS-248360 IC50 = 6.0 nM 8.22
CHEMBL3736242 IC50 = 7.0 nM 8.15
CHEMBL275545 IC50 = 8.0 nM 8.10
CHEMBL3735574 IC50 = 8.0 nM 8.10
CHEMBL3734968 IC50 = 13.0 nM 7.89
CHEMBL3735155 IC50 = 16.0 nM 7.80
CHEMBL12333 IC50 = 21.0 nM 7.68
CHEMBL417429 IC50 = 24.0 nM 7.62
CHEMBL3735931 IC50 = 28.0 nM 7.55
CHEMBL11528 IC50 = 30.0 nM 7.52
CHEMBL3736037 IC50 = 31.0 nM 7.51
CHEMBL3734870 IC50 = 37.0 nM 7.43
CHEMBL3736248 IC50 = 42.0 nM 7.38
CHEMBL3735236 IC50 = 47.0 nM 7.33
CHEMBL3736262 IC50 = 50.0 nM 7.30
CHEMBL3735151 IC50 = 56.0 nM 7.25
CHEMBL3736414 IC50 = 76.0 nM 7.12
CHEMBL3734835 IC50 = 81.0 nM 7.09
CHEMBL3734955 IC50 = 92.0 nM 7.04
CHEMBL3735302 IC50 = 94.0 nM 7.03
CHEMBL3736507 IC50 = 95.0 nM 7.02
CHEMBL3735265 IC50 = 152.0 nM 6.82
CHEMBL3734829 IC50 = 160.0 nM 6.80
CHEMBL3735036 IC50 = 201.0 nM 6.70
CHEMBL3734849 IC50 = 217.0 nM 6.66
CHEMBL3736310 IC50 = 341.0 nM 6.47
CHEMBL3735797 IC50 = 373.0 nM 6.43
CHEMBL3736225 IC50 = 385.0 nM 6.42
CHEMBL3735300 IC50 = 419.0 nM 6.38
CHEMBL3735311 IC50 = 465.0 nM 6.33