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Assay Detail

CHEMBL649491

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

Binding
Inhibition of [125I]AII binding to guinea pig adrenal membrane
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Angiotensin II receptor (CHEMBL2094256)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

New nonpeptide angiostensin II receptor antagonists. Synthesis, biological properties and structure-activity relationships of 3-substituted 2,6-dialkyl-4-(biphenyll)methylaminopyridine derivatives.
Bradbury R, Edwards M, Fisher E, Girdwood J, Major J, Oldham A, Patel M, Pearce R, Revill J, Ratcliffe A
Bioorg Med Chem Lett (1994) 4 : 139 -144
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.08 8.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33459 1 8.58
CHEMBL33811 1 8.46
CHEMBL32649 1 8.42
CHEMBL418226 1 8.30
CHEMBL33226 1 8.21
CHEMBL34044 1 8.18
CHEMBL32648 1 8.12
CHEMBL191 LOSARTAN 4.0 1 8.10
CHEMBL285176 1 8.10
CHEMBL285560 1 7.85
CHEMBL33403 1 7.60
CHEMBL287230 1 7.58
CHEMBL284536 1 7.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33459 IC50 = 2.64 nM 8.58
CHEMBL33811 IC50 = 3.48 nM 8.46
CHEMBL32649 IC50 = 3.83 nM 8.42
CHEMBL418226 IC50 = 5.0 nM 8.30
CHEMBL33226 IC50 = 6.21 nM 8.21
CHEMBL34044 IC50 = 6.65 nM 8.18
CHEMBL32648 IC50 = 7.58 nM 8.12
CHEMBL191 LOSARTAN IC50 = 8.0 nM 8.10
CHEMBL285176 IC50 = 8.03 nM 8.10
CHEMBL285560 IC50 = 14.0 nM 7.85
CHEMBL33403 IC50 = 24.9 nM 7.60
CHEMBL287230 IC50 = 26.4 nM 7.58
CHEMBL284536 IC50 = 31.0 nM 7.51