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Assay Detail

CHEMBL647791

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

Binding
Specific binding inhibition of [125I]AII to Angiotensin II receptor, type 1 in rat liver membrane
ChEMBL ↗
53
Total Activities
53
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

Sulfonylureas and sulfonylcarbamates as new non-tetrazole angiotensin II receptor antagonists. Discovery of a highly potent orally active (imidazolylbiphenylyl)sulfonylurea (HR 720).
Deprez P, Guillaume J, Becker R, Corbier A, Didierlaurent S, Fortin M, Frechet D, Hamon G, Heckmann B, Heitsch H.
J Med Chem (1995) 38 : 2357 -2377
PubMed 7608902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 53 9.01 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL80177 — — 1 10.10
CHEMBL76870 — — 1 10.05
CHEMBL311312 — — 1 10.00
CHEMBL309313 — — 1 10.00
CHEMBL309602 — — 1 9.70
CHEMBL63998 — — 1 9.70
CHEMBL80700 — — 1 9.70
CHEMBL78866 — — 1 9.70
CHEMBL445365 — — 1 9.70
CHEMBL311827 — — 1 9.70
CHEMBL308135 — — 1 9.70
CHEMBL77308 — — 1 9.70
CHEMBL309845 — — 1 9.52
CHEMBL312386 — — 1 9.52
CHEMBL305638 — — 1 9.52
CHEMBL76525 — — 1 9.52
CHEMBL76538 — — 1 9.52
CHEMBL76948 — — 1 9.40
CHEMBL80971 — — 1 9.40
CHEMBL80370 — — 1 9.32
CHEMBL306157 — — 1 9.30
CHEMBL80622 — — 1 9.22
CHEMBL305604 — — 1 9.22
CHEMBL432158 — — 1 9.10
CHEMBL76799 — — 1 9.10
CHEMBL77138 — — 1 9.10
CHEMBL77360 — — 1 9.10
CHEMBL311189 — — 1 9.05
CHEMBL80900 — — 1 9.05
CHEMBL311847 — — 1 9.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL80177 — IC50 = 0.08 nM 10.10
CHEMBL76870 — IC50 = 0.09 nM 10.05
CHEMBL309313 — IC50 = 0.1 nM 10.00
CHEMBL311312 — IC50 = 0.1 nM 10.00
CHEMBL309602 — IC50 = 0.2 nM 9.70
CHEMBL63998 — IC50 = 0.2 nM 9.70
CHEMBL80700 — IC50 = 0.2 nM 9.70
CHEMBL78866 — IC50 = 0.2 nM 9.70
CHEMBL445365 — IC50 = 0.2 nM 9.70
CHEMBL311827 — IC50 = 0.2 nM 9.70
CHEMBL308135 — IC50 = 0.2 nM 9.70
CHEMBL77308 — IC50 = 0.2 nM 9.70
CHEMBL76525 — IC50 = 0.3 nM 9.52
CHEMBL312386 — IC50 = 0.3 nM 9.52
CHEMBL309845 — IC50 = 0.3 nM 9.52
CHEMBL305638 — IC50 = 0.3 nM 9.52
CHEMBL76538 — IC50 = 0.3 nM 9.52
CHEMBL76948 — IC50 = 0.4 nM 9.40
CHEMBL80971 — IC50 = 0.4 nM 9.40
CHEMBL80370 — IC50 = 0.48 nM 9.32
CHEMBL306157 — IC50 = 0.5 nM 9.30
CHEMBL80622 — IC50 = 0.6 nM 9.22
CHEMBL305604 — IC50 = 0.6 nM 9.22
CHEMBL77360 — IC50 = 0.8 nM 9.10
CHEMBL77138 — IC50 = 0.8 nM 9.10
CHEMBL432158 — IC50 = 0.8 nM 9.10
CHEMBL76799 — IC50 = 0.8 nM 9.10
CHEMBL311189 — IC50 = 0.9 nM 9.05
CHEMBL80900 — IC50 = 0.9 nM 9.05
CHEMBL311847 — IC50 = 0.9 nM 9.05
CHEMBL76613 — IC50 = 1.0 nM 9.00
CHEMBL306778 — IC50 = 1.0 nM 9.00
CHEMBL306085 — IC50 = 1.0 nM 9.00
CHEMBL443069 — IC50 = 1.1 nM 8.96
CHEMBL80908 — IC50 = 1.1 nM 8.96
CHEMBL310267 — IC50 = 1.3 nM 8.89
CHEMBL78169 — IC50 = 1.5 nM 8.82
CHEMBL413491 — IC50 = 1.7 nM 8.77
CHEMBL80181 — IC50 = 1.8 nM 8.74
CHEMBL310610 — IC50 = 1.9 nM 8.72
CHEMBL441990 — IC50 = 2.1 nM 8.68
CHEMBL78445 — IC50 = 2.1 nM 8.68
CHEMBL76760 — IC50 = 2.6 nM 8.59
CHEMBL306180 — IC50 = 3.1 nM 8.51
CHEMBL80212 — IC50 = 3.2 nM 8.49
CHEMBL79106 — IC50 = 4.5 nM 8.35
CHEMBL80901 — IC50 = 4.7 nM 8.33
CHEMBL75921 — IC50 = 7.7 nM 8.11
CHEMBL76675 — IC50 = 15.0 nM 7.82
CHEMBL79108 — IC50 = 36.0 nM 7.44