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Assay Detail

CHEMBL3757817

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

Binding
Displacement of 125I-labelled Sar1-Ile8-angiotensin-2 from human AT1 receptor
24
Total Activities
24
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

Synthesis and biological evaluation of 4-[(benzimidazol-1-yl) methyl]biphenyl-2-amides as dual angiotensin II and endothelin A receptor antagonists
Han X, Xue W, Hao L, Zhou Z
Medchemcomm (2015) 6 : 1479 -1483
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.10 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3752680 1 8.41
CHEMBL191 LOSARTAN 4.0 1 7.79
CHEMBL3753458 1 7.58
CHEMBL3752160 1 7.51
CHEMBL3751994 1 7.48
CHEMBL3752530 1 7.43
CHEMBL3752947 1 7.36
CHEMBL3751986 1 7.27
CHEMBL3753134 1 7.27
CHEMBL3754267 1 7.17
CHEMBL3753888 1 7.16
CHEMBL3752444 1 7.13
CHEMBL3752117 1 7.13
CHEMBL3753406 1 7.09
CHEMBL3752145 1 7.06
CHEMBL3753277 1 7.05
CHEMBL3754394 1 7.03
CHEMBL3753047 1 6.85
CHEMBL3752198 1 6.79
CHEMBL3751899 1 6.46
CHEMBL3754661 1 6.44
CHEMBL3754198 1 6.41
CHEMBL3754010 1 6.36
CHEMBL3753007 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3752680 IC50 = 3.9 nM 8.41
CHEMBL191 LOSARTAN IC50 = 16.2 nM 7.79
CHEMBL3753458 IC50 = 26.1 nM 7.58
CHEMBL3752160 IC50 = 30.7 nM 7.51
CHEMBL3751994 IC50 = 32.9 nM 7.48
CHEMBL3752530 IC50 = 36.9 nM 7.43
CHEMBL3752947 IC50 = 44.0 nM 7.36
CHEMBL3751986 IC50 = 53.5 nM 7.27
CHEMBL3753134 IC50 = 53.9 nM 7.27
CHEMBL3754267 IC50 = 67.5 nM 7.17
CHEMBL3753888 IC50 = 69.4 nM 7.16
CHEMBL3752444 IC50 = 73.7 nM 7.13
CHEMBL3752117 IC50 = 73.3 nM 7.13
CHEMBL3753406 IC50 = 82.0 nM 7.09
CHEMBL3752145 IC50 = 87.8 nM 7.06
CHEMBL3753277 IC50 = 90.0 nM 7.05
CHEMBL3754394 IC50 = 93.0 nM 7.03
CHEMBL3753047 IC50 = 140.0 nM 6.85
CHEMBL3752198 IC50 = 161.0 nM 6.79
CHEMBL3751899 IC50 = 347.0 nM 6.46
CHEMBL3754661 IC50 = 363.0 nM 6.44
CHEMBL3754198 IC50 = 390.0 nM 6.41
CHEMBL3754010 IC50 = 439.0 nM 6.36
CHEMBL3753007 IC50 = 549.8 nM 6.26