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Assay Detail

CHEMBL650302

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

Binding
Compound was tested for in vitro inhibition of specific binding of [I-125]AII to Angiotensin II receptor, type 1 in guinea pig adrenal membrane preparation
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Type-1 angiotensin II receptor (CHEMBL1671613)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

The synthesis and biological activity of tetrahydroquinoline angiotensin II antagonists containing a substituted biphenyltetrazole group
Thomas AP, Roberts DA, Thomason DA
Bioorg Med Chem Lett (1994) 4 : 2615 -2620
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.50 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418226 1 8.30
CHEMBL314982 1 8.05
CHEMBL191 LOSARTAN 4.0 1 7.75
CHEMBL86604 1 7.54
CHEMBL89614 1 7.27
CHEMBL86495 1 7.17
CHEMBL84792 1 7.03
CHEMBL87034 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418226 IC50 = 5.0 nM 8.30
CHEMBL314982 IC50 = 9.0 nM 8.05
CHEMBL191 LOSARTAN IC50 = 18.0 nM 7.75
CHEMBL86604 IC50 = 29.0 nM 7.54
CHEMBL89614 IC50 = 54.0 nM 7.27
CHEMBL86495 IC50 = 67.0 nM 7.17
CHEMBL84792 IC50 = 93.0 nM 7.03
CHEMBL87034 IC50 = 140.0 nM 6.85