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Assay Detail

CHEMBL652868

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

Binding
In vitro ability to inhibit the binding of radioligand 125I[Sar1,IIe8]AII to AT1 receptor from rabbit aorta
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Potent triazolinone-based angiotensin II receptor antagonists with equivalent affinity for both the AT1 and AT2 subtypes
Chang L, Ashton W, Flanagan K, Rivero R, Chen T, O'Malley S, Zingaro G, Kivlighn S, Siegl P, Lotti V, Chang R, Greenlee W
Bioorg Med Chem Lett (1994) 4 : 2787 -2792
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 9.27 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265797 1 10.28
CHEMBL316300 1 9.96
CHEMBL329679 1 9.82
CHEMBL96075 1 9.80
CHEMBL93907 1 9.77
CHEMBL319730 1 9.60
CHEMBL276674 1 9.54
CHEMBL92533 1 9.51
CHEMBL292150 1 9.35
CHEMBL313868 1 9.21
CHEMBL323506 1 9.08
CHEMBL321531 1 9.05
CHEMBL94793 1 9.00
CHEMBL316299 1 8.89
CHEMBL321313 1 8.85
CHEMBL302102 1 8.77
CHEMBL96314 1 8.41
CHEMBL96554 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265797 IC50 = 0.052 nM 10.28
CHEMBL316300 IC50 = 0.11 nM 9.96
CHEMBL329679 IC50 = 0.15 nM 9.82
CHEMBL96075 IC50 = 0.16 nM 9.80
CHEMBL93907 IC50 = 0.17 nM 9.77
CHEMBL319730 IC50 = 0.25 nM 9.60
CHEMBL276674 IC50 = 0.29 nM 9.54
CHEMBL92533 IC50 = 0.31 nM 9.51
CHEMBL292150 IC50 = 0.45 nM 9.35
CHEMBL313868 IC50 = 0.62 nM 9.21
CHEMBL323506 IC50 = 0.84 nM 9.08
CHEMBL321531 IC50 = 0.9 nM 9.05
CHEMBL94793 IC50 = 1.0 nM 9.00
CHEMBL316299 IC50 = 1.3 nM 8.89
CHEMBL321313 IC50 = 1.4 nM 8.85
CHEMBL302102 IC50 = 1.7 nM 8.77
CHEMBL96314 IC50 = 3.9 nM 8.41
CHEMBL96554 IC50 = 10.0 nM 8.00