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Assay Detail

CHEMBL648850

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

Binding
Binding affinity evaluated by its ability to displace the specific binding ligand 125I-SAR1, Ile8-AII from Angiotensin II receptor, type 1 in rabbit aorta membrane
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Acidic phenols: a new class of potent nonpeptide angiotensin II receptor antagonists
Kim D, Mantlo NB, Tata J, Fitch K, Dhanoa D, Owens K, Levorse D, Siegl P, Chang R, Chen T, Scheck S, Zingaro G, Kivlighn S, Greenlee W
Bioorg Med Chem Lett (1994) 4 : 207 -212
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.14 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7550 L-158809 1 9.52
CHEMBL303147 1 8.30
CHEMBL291358 1 8.22
CHEMBL64983 1 8.10
CHEMBL293926 1 7.96
CHEMBL63144 1 7.80
CHEMBL303186 1 7.66
CHEMBL63879 1 7.60
CHEMBL67616 1 7.50
CHEMBL63280 1 7.29
CHEMBL293846 1 6.80
CHEMBL304655 1 6.60
CHEMBL292739 1 6.48
CHEMBL67309 1 6.39
CHEMBL68111 1 6.36
CHEMBL277614 1 6.11
CHEMBL304116 1 6.07
CHEMBL302869 1 5.96
CHEMBL66056 1 4.96
CHEMBL63250 1 -
CHEMBL63220 1 -
CHEMBL293925 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7550 L-158809 IC50 = 0.3 nM 9.52
CHEMBL303147 IC50 = 5.0 nM 8.30
CHEMBL291358 IC50 = 6.0 nM 8.22
CHEMBL64983 IC50 = 8.0 nM 8.10
CHEMBL293926 IC50 = 11.0 nM 7.96
CHEMBL63144 IC50 = 16.0 nM 7.80
CHEMBL303186 IC50 = 22.0 nM 7.66
CHEMBL63879 IC50 = 25.0 nM 7.60
CHEMBL67616 IC50 = 32.0 nM 7.50
CHEMBL63280 IC50 = 51.0 nM 7.29
CHEMBL293846 IC50 = 160.0 nM 6.80
CHEMBL304655 IC50 = 250.0 nM 6.60
CHEMBL292739 IC50 = 330.0 nM 6.48
CHEMBL67309 IC50 = 410.0 nM 6.39
CHEMBL68111 IC50 = 440.0 nM 6.36
CHEMBL277614 IC50 = 780.0 nM 6.11
CHEMBL304116 IC50 = 850.0 nM 6.07
CHEMBL302869 IC50 = 1100.0 nM 5.96
CHEMBL66056 IC50 = 11000.0 nM 4.96
CHEMBL63250 IC50 > 3000.0 nM -
CHEMBL63220 IC50 > 1000.0 nM -
CHEMBL293925 IC50 > 1200.0 nM -