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Assay Detail

CHEMBL646972

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

Binding
Ability to displace [125I]- labelled [Sar1,Ileu8] from angiotensin II receptor of bovine adrenal cortex membranes
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Adrenal cortex
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Type-1 angiotensin II receptor (CHEMBL3374)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Substituted piperidin-2-one biphenyltetrazoles as angiotensin II antagonists
Murray W, Lalan P, Gill A, Addo M, Lewis J, Lee D, Rampulla R, Wachter M, Hsi J, Underwood D
Bioorg Med Chem Lett (1992) 2 : 1775 -1779
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.56 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49207 1 7.70
CHEMBL51084 1 7.40
CHEMBL48459 1 7.05
CHEMBL50906 1 6.92
CHEMBL296731 1 6.92
CHEMBL51622 1 6.75
CHEMBL413098 1 6.70
CHEMBL418269 1 6.68
CHEMBL48602 1 6.60
CHEMBL51001 1 6.50
CHEMBL295369 1 6.48
CHEMBL191 LOSARTAN 4.0 1 6.38
CHEMBL299151 1 6.33
CHEMBL49192 1 6.27
CHEMBL51078 1 6.17
CHEMBL52046 1 5.51
CHEMBL49262 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49207 IC50 = 20.0 nM 7.70
CHEMBL51084 IC50 = 40.0 nM 7.40
CHEMBL48459 IC50 = 90.0 nM 7.05
CHEMBL50906 IC50 = 120.0 nM 6.92
CHEMBL296731 IC50 = 120.0 nM 6.92
CHEMBL51622 IC50 = 180.0 nM 6.75
CHEMBL413098 IC50 = 200.0 nM 6.70
CHEMBL418269 IC50 = 210.0 nM 6.68
CHEMBL48602 IC50 = 250.0 nM 6.60
CHEMBL51001 IC50 = 320.0 nM 6.50
CHEMBL295369 IC50 = 330.0 nM 6.48
CHEMBL191 LOSARTAN IC50 = 420.0 nM 6.38
CHEMBL299151 IC50 = 470.0 nM 6.33
CHEMBL49192 IC50 = 540.0 nM 6.27
CHEMBL51078 IC50 = 680.0 nM 6.17
CHEMBL52046 IC50 = 3100.0 nM 5.51
CHEMBL49262 IC50 = 5800.0 nM 5.24