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Assay Detail

CHEMBL644583

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

Binding
Binding affinity against Angiotensin II receptor, type 1 using [125I]Sar-Ile8-AII in rat liver membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Angiotensin II receptor (AT-1) type-1 (CHEMBL2094250)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

A conformationally restrained series of AT1-selective angiotensin II antagonists
Carpino PA, Sneddon SF, Paul da Silva J, George T. M, Albert L. R, Michael R. B
Bioorg Med Chem Lett (1994) 4 : 93 -98
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.82 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL174546 1 9.70
CHEMBL7550 L-158809 1 9.70
CHEMBL178380 1 7.96
CHEMBL176099 1 7.85
CHEMBL414836 1 7.52
CHEMBL427130 1 7.16
CHEMBL174600 1 6.92
CHEMBL367683 1 6.92
CHEMBL176370 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL174546 IC50 = 0.2 nM 9.70
CHEMBL7550 L-158809 IC50 = 0.2 nM 9.70
CHEMBL178380 IC50 = 11.0 nM 7.96
CHEMBL176099 IC50 = 14.0 nM 7.85
CHEMBL414836 IC50 = 30.0 nM 7.52
CHEMBL427130 IC50 = 70.0 nM 7.16
CHEMBL174600 IC50 = 120.0 nM 6.92
CHEMBL367683 IC50 = 120.0 nM 6.92
CHEMBL176370 IC50 = 220.0 nM 6.66