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Assay Detail

CHEMBL652725

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

Binding
Inhibition of [125I]-Sar1-Ile8-Ang II binding to Angiotensin II receptor type 1 from rabbit aorta
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

The design, binding affinity prediction and synthesis of macrocyclic angiotensin II AT1 and AT2 receptor antagonists
de Laszlo SE, Glinka TW, Greenlee WJ, Ball R, Nachbar RB, Prendergast K
Bioorg Med Chem Lett (1996) 6 : 923 -928
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.59 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL367569 1 9.52
CHEMBL173643 1 9.40
CHEMBL176473 1 9.05
CHEMBL168771 1 9.00
CHEMBL408798 1 8.89
CHEMBL302102 1 8.82
CHEMBL408799 1 8.82
CHEMBL368149 1 8.41
CHEMBL173455 1 8.06
CHEMBL367095 1 7.96
CHEMBL172376 1 7.64
CHEMBL174080 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL367569 IC50 = 0.3 nM 9.52
CHEMBL173643 IC50 = 0.4 nM 9.40
CHEMBL176473 IC50 = 0.9 nM 9.05
CHEMBL168771 IC50 = 1.0 nM 9.00
CHEMBL408798 IC50 = 1.3 nM 8.89
CHEMBL302102 IC50 = 1.5 nM 8.82
CHEMBL408799 IC50 = 1.5 nM 8.82
CHEMBL368149 IC50 = 3.9 nM 8.41
CHEMBL173455 IC50 = 8.8 nM 8.06
CHEMBL367095 IC50 = 11.0 nM 7.96
CHEMBL172376 IC50 = 23.0 nM 7.64
CHEMBL174080 IC50 = 30.0 nM 7.52