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Assay Detail

CHEMBL3258305

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

Binding
Competitive antagonist at angiotensin 2 receptor in rabbit aorta assessed as rightward shift in angiotensin-2 dose response curve for myotropic activity
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis of angiotensin II antagonists by incorporating alpha-methylalanine or O-methylthreonine residues in angiotension II analogues.
Khosla MC, Muñoz-Ramírez H, Hall MM, Khairallah PA, Bumpus FM.
J Med Chem (1977) 20 : 1051 -1055
PubMed 894674 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 8.78 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2370903 1 9.50
CHEMBL3248820 1 9.50
CHEMBL404594 1 9.17
CHEMBL2371400 1 8.79
CHEMBL2371388 1 8.78
CHEMBL3248823 1 8.76
CHEMBL3248821 1 8.70
CHEMBL312754 1 8.61
CHEMBL3248822 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2370903 Kd = 0.3162 nM 9.50
CHEMBL3248820 Kd = 0.3162 nM 9.50
CHEMBL404594 Kd = 0.6761 nM 9.17
CHEMBL2371400 Kd = 1.622 nM 8.79
CHEMBL2371388 Kd = 1.66 nM 8.78
CHEMBL3248823 Kd = 1.738 nM 8.76
CHEMBL3248821 Kd = 1.995 nM 8.70
CHEMBL312754 Kd = 2.455 nM 8.61
CHEMBL3248822 Kd = 60.26 nM 7.22