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Assay Detail

CHEMBL652267

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

Binding
In vitro binding affinity against Angiotensin II receptor in rabbit aorta rings
19
Total Activities
16
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 Expert

Target

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

Publication

Substituted lactam biphenyltetrazoles as angiotensin II mediated antihypertensives
Murray W, Lalan P, Gill A, Lee D, Falotico R, Lewis J, Addo M, Wachter M
Bioorg Med Chem Lett (1994) 4 : 87 -92
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 19 8.13 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122891 1 9.00
CHEMBL48602 2 9.00
CHEMBL191 LOSARTAN 4.0 1 8.80
CHEMBL170196 1 8.50
CHEMBL49207 2 8.40
CHEMBL422912 1 8.40
CHEMBL51084 1 8.30
CHEMBL123208 2 8.20
CHEMBL425139 1 7.90
CHEMBL49192 1 7.90
CHEMBL48459 1 7.90
CHEMBL296731 1 7.80
CHEMBL122855 1 7.70
CHEMBL299151 1 7.50
CHEMBL49262 1 7.40
CHEMBL51622 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48602 Kd = 1.0 nM 9.00
CHEMBL122891 Kd = 1.0 nM 9.00
CHEMBL191 LOSARTAN Kd = 1.585 nM 8.80
CHEMBL48602 Kd = 2.512 nM 8.60
CHEMBL170196 Kd = 3.162 nM 8.50
CHEMBL49207 Kd = 3.981 nM 8.40
CHEMBL422912 Kd = 3.981 nM 8.40
CHEMBL51084 Kd = 5.012 nM 8.30
CHEMBL123208 Kd = 6.31 nM 8.20
CHEMBL49207 Kd = 7.943 nM 8.10
CHEMBL123208 Kd = 10.0 nM 8.00
CHEMBL425139 Kd = 12.59 nM 7.90
CHEMBL49192 Kd = 12.59 nM 7.90
CHEMBL48459 Kd = 12.59 nM 7.90
CHEMBL296731 Kd = 15.85 nM 7.80
CHEMBL122855 Kd = 19.95 nM 7.70
CHEMBL299151 Kd = 31.62 nM 7.50
CHEMBL49262 Kd = 39.81 nM 7.40
CHEMBL51622 Kd = 100.0 nM 7.00