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Assay Detail

CHEMBL652357

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

Binding
Concentration required for 50% inhibition of [125I]- AII binding to rat liver membrane preparation (AT1)
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Liver
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Balanced AT1 and AT2 angiotensin II antagonists. III. potent and orally active 5--ketosulfoxide imidazolyl biphenyl sulfonylureas
Deprez P, Guillaume J, Corbier A, Vevert J, Fortin M, Heckmann B
Bioorg Med Chem Lett (1995) 5 : 2617 -2622
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 9.86 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL313598 1 10.70
CHEMBL87244 2 10.52
CHEMBL89032 1 10.40
CHEMBL315236 1 10.40
CHEMBL431853 1 10.22
CHEMBL84908 1 10.15
CHEMBL91046 1 10.10
CHEMBL86538 1 10.10
CHEMBL264304 1 10.10
CHEMBL87091 1 10.05
CHEMBL433010 1 10.05
CHEMBL328985 1 10.00
CHEMBL84795 1 10.00
CHEMBL327927 1 9.70
CHEMBL327297 1 9.70
CHEMBL91047 1 9.52
CHEMBL312990 1 9.52
CHEMBL85075 1 9.52
CHEMBL316402 1 9.46
CHEMBL80370 1 9.30
CHEMBL89772 1 8.74
CHEMBL315275 1 8.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL313598 IC50 = 0.02 nM 10.70
CHEMBL87244 IC50 = 0.03 nM 10.52
CHEMBL89032 IC50 = 0.04 nM 10.40
CHEMBL315236 IC50 = 0.04 nM 10.40
CHEMBL431853 IC50 = 0.06 nM 10.22
CHEMBL84908 IC50 = 0.07 nM 10.15
CHEMBL87244 IC50 = 0.07 nM 10.15
CHEMBL91046 IC50 = 0.08 nM 10.10
CHEMBL86538 IC50 = 0.08 nM 10.10
CHEMBL264304 IC50 = 0.08 nM 10.10
CHEMBL433010 IC50 = 0.09 nM 10.05
CHEMBL87091 IC50 = 0.09 nM 10.05
CHEMBL84795 IC50 = 0.1 nM 10.00
CHEMBL328985 IC50 = 0.1 nM 10.00
CHEMBL327927 IC50 = 0.2 nM 9.70
CHEMBL327297 IC50 = 0.2 nM 9.70
CHEMBL91047 IC50 = 0.3 nM 9.52
CHEMBL312990 IC50 = 0.3 nM 9.52
CHEMBL85075 IC50 = 0.3 nM 9.52
CHEMBL316402 IC50 = 0.35 nM 9.46
CHEMBL80370 IC50 = 0.5 nM 9.30
CHEMBL89772 IC50 = 1.8 nM 8.74
CHEMBL315275 IC50 = 3.8 nM 8.42