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Assay Detail

CHEMBL652260

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

Binding
Displacement of angiotensin II from angiotensin II receptor of rabbit aorta
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

4,5,6,7-Tetrahdryo-8-oxo-cycloheptimidazoles: a new class of potent non-peptide angiiotensin II receptor antagonists
Yanagisawa T, Ueyama N, Kawai T, Sonegawa M, Baba H, Mochizuki S, Kozakai K, Tomiyama T
Bioorg Med Chem Lett (1993) 3 : 1559 -1564
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 14 8.16 10.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41194 PRATOSARTAN 2.0 1 10.04
CHEMBL40340 1 9.66
CHEMBL40286 1 9.36
CHEMBL41826 1 9.04
CHEMBL17196 1 8.32
CHEMBL287841 1 8.31
CHEMBL43360 1 8.13
CHEMBL288506 1 7.80
CHEMBL41828 1 7.69
CHEMBL41448 1 7.41
CHEMBL39642 1 7.33
CHEMBL290917 1 7.23
CHEMBL291087 1 7.04
CHEMBL40549 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41194 PRATOSARTAN Kd = 0.0912 nM 10.04
CHEMBL40340 Kd = 0.2188 nM 9.66
CHEMBL40286 Kd = 0.4365 nM 9.36
CHEMBL41826 Kd = 0.912 nM 9.04
CHEMBL17196 Kd = 4.786 nM 8.32
CHEMBL287841 Kd = 4.898 nM 8.31
CHEMBL43360 Kd = 7.413 nM 8.13
CHEMBL288506 Kd = 15.85 nM 7.80
CHEMBL41828 Kd = 20.42 nM 7.69
CHEMBL41448 Kd = 38.9 nM 7.41
CHEMBL39642 Kd = 46.77 nM 7.33
CHEMBL290917 Kd = 58.88 nM 7.23
CHEMBL291087 Kd = 91.2 nM 7.04
CHEMBL40549 Kd = 144.54 nM 6.84