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Assay Detail

CHEMBL647289

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

Binding
Displacement of [1251][Sar1,IIe8]AII from rabbit aorta Angiotensin II receptor, type 1
13
Total Activities
13
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 Intermediate

Target

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

Publication

(Dipropylphenoxy)phenylacetic acids: a new generation of nonpeptide angiotensin II receptor antagonists.
Dhanoa DS, Bagley SW, Chang RS, Lotti VJ, Chen TB, Kivlighn SD, Zingaro GJ, Siegl PK, Chakravarty PK, Patchett AA.
J Med Chem (1993) 36 : 3738 -3742
PubMed 8246245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.65 9.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340367 1 9.33
CHEMBL123084 1 9.28
CHEMBL7550 L-158809 1 9.27
CHEMBL122224 1 9.13
CHEMBL122017 1 9.12
CHEMBL122212 1 9.05
CHEMBL121891 1 8.92
CHEMBL332239 1 8.55
CHEMBL124541 1 8.40
CHEMBL331797 1 8.28
CHEMBL122367 1 8.17
CHEMBL123562 1 7.72
CHEMBL191 LOSARTAN 4.0 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340367 IC50 = 0.47 nM 9.33
CHEMBL123084 IC50 = 0.53 nM 9.28
CHEMBL7550 L-158809 IC50 = 0.54 nM 9.27
CHEMBL122224 IC50 = 0.74 nM 9.13
CHEMBL122017 IC50 = 0.75 nM 9.12
CHEMBL122212 IC50 = 0.9 nM 9.05
CHEMBL121891 IC50 = 1.2 nM 8.92
CHEMBL332239 IC50 = 2.8 nM 8.55
CHEMBL124541 IC50 = 4.0 nM 8.40
CHEMBL331797 IC50 = 5.2 nM 8.28
CHEMBL122367 IC50 = 6.8 nM 8.17
CHEMBL123562 IC50 = 19.0 nM 7.72
CHEMBL191 LOSARTAN IC50 = 54.0 nM 7.27