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Assay Detail

CHEMBL649712

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

Binding
Tested in vitro for binding affinity against Angiotensin II receptor, type 1 in rabbit aortic membrane
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

A new class of balanced AT1/AT2 angiotensin II antagonists: quinazolinone AII antagonists with acylsulfonamide and sulfonylcarbamate acidic functionalities
Glinka TW, de Laszlo SE, Siegl PK, Chang RS, Kivlighn SD, Schorn TS, Faust KA, Chen T, Zingaro GJ, Lotti VJ, Greenlee WJ
Bioorg Med Chem Lett (1994) 4 : 81 -86
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 9.30 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL353037 1 9.92
CHEMBL353800 1 9.82
CHEMBL352771 1 9.82
CHEMBL354779 1 9.77
CHEMBL169568 1 9.74
CHEMBL169221 1 9.74
CHEMBL352503 1 9.72
CHEMBL169967 1 9.68
CHEMBL74476 1 9.62
CHEMBL169488 1 9.62
CHEMBL168413 1 9.60
CHEMBL353615 1 9.60
CHEMBL169968 1 9.60
CHEMBL168490 1 9.59
CHEMBL352629 1 9.49
CHEMBL352947 1 9.48
CHEMBL352502 1 9.46
CHEMBL352458 1 9.44
CHEMBL169279 1 9.41
CHEMBL354080 1 9.37
CHEMBL353980 1 9.26
CHEMBL169009 1 9.07
CHEMBL168771 1 9.00
CHEMBL354298 1 8.96
CHEMBL168346 1 7.82
CHEMBL169798 1 7.80
CHEMBL169827 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL353037 IC50 = 0.12 nM 9.92
CHEMBL353800 IC50 = 0.15 nM 9.82
CHEMBL352771 IC50 = 0.15 nM 9.82
CHEMBL354779 IC50 = 0.17 nM 9.77
CHEMBL169568 IC50 = 0.18 nM 9.74
CHEMBL169221 IC50 = 0.18 nM 9.74
CHEMBL352503 IC50 = 0.19 nM 9.72
CHEMBL169967 IC50 = 0.21 nM 9.68
CHEMBL74476 IC50 = 0.24 nM 9.62
CHEMBL169488 IC50 = 0.24 nM 9.62
CHEMBL168413 IC50 = 0.25 nM 9.60
CHEMBL353615 IC50 = 0.25 nM 9.60
CHEMBL169968 IC50 = 0.25 nM 9.60
CHEMBL168490 IC50 = 0.26 nM 9.59
CHEMBL352629 IC50 = 0.32 nM 9.49
CHEMBL352947 IC50 = 0.33 nM 9.48
CHEMBL352502 IC50 = 0.35 nM 9.46
CHEMBL352458 IC50 = 0.36 nM 9.44
CHEMBL169279 IC50 = 0.39 nM 9.41
CHEMBL354080 IC50 = 0.43 nM 9.37
CHEMBL353980 IC50 = 0.55 nM 9.26
CHEMBL169009 IC50 = 0.86 nM 9.07
CHEMBL168771 IC50 = 0.99 nM 9.00
CHEMBL354298 IC50 = 1.1 nM 8.96
CHEMBL168346 IC50 = 15.0 nM 7.82
CHEMBL169798 IC50 = 16.0 nM 7.80
CHEMBL169827 IC50 = 180.0 nM 6.75