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Assay Detail

CHEMBL647855

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

Functional
In vitro antagonist activity against angiotensin II type 2 (AT2) receptor in rat midbrain using [125I]- Sar, Ile AII.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Type-2 angiotensin II receptor (CHEMBL257)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Non-peptide angiotensin II receptor antagonists. 2. Design, synthesis, and biological activity of N-substituted (phenylamino)phenylacetic acids and acyl sulfonamides.
Dhanoa DS, Bagley SW, Chang RS, Lotti VJ, Chen TB, Kivlighn SD, Zingaro GJ, Siegl PK, Patchett AA, Greenlee WJ.
J Med Chem (1993) 36 : 4239 -4249
PubMed 8277506 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 5.52 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL337007 1 6.70
CHEMBL335722 1 6.38
CHEMBL135089 1 6.31
CHEMBL336738 1 6.25
CHEMBL336808 1 6.18
CHEMBL135346 1 6.13
CHEMBL135929 1 5.80
CHEMBL134491 1 5.68
CHEMBL134286 1 5.66
CHEMBL337006 1 5.54
CHEMBL135345 1 5.47
CHEMBL336773 1 5.37
CHEMBL335066 1 5.32
CHEMBL135819 1 5.22
CHEMBL335289 1 5.07
CHEMBL337663 1 5.06
CHEMBL135704 1 4.96
CHEMBL424643 1 4.96
CHEMBL334832 1 4.96
CHEMBL132807 1 4.92
CHEMBL424465 1 4.72
CHEMBL335514 1 4.68
CHEMBL7550 L-158809 1 -
CHEMBL136028 1 -
CHEMBL335276 1 -
CHEMBL136034 1 -
CHEMBL191 LOSARTAN 4.0 1 -
CHEMBL337217 1 -
CHEMBL134754 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL337007 IC50 = 200.0 nM 6.70
CHEMBL335722 IC50 = 420.0 nM 6.38
CHEMBL135089 IC50 = 490.0 nM 6.31
CHEMBL336738 IC50 = 560.0 nM 6.25
CHEMBL336808 IC50 = 660.0 nM 6.18
CHEMBL135346 IC50 = 740.0 nM 6.13
CHEMBL135929 IC50 = 1600.0 nM 5.80
CHEMBL134491 IC50 = 2100.0 nM 5.68
CHEMBL134286 IC50 = 2200.0 nM 5.66
CHEMBL337006 IC50 = 2900.0 nM 5.54
CHEMBL135345 IC50 = 3400.0 nM 5.47
CHEMBL336773 IC50 = 4300.0 nM 5.37
CHEMBL335066 IC50 = 4800.0 nM 5.32
CHEMBL135819 IC50 = 6000.0 nM 5.22
CHEMBL335289 IC50 = 8600.0 nM 5.07
CHEMBL337663 IC50 = 8800.0 nM 5.06
CHEMBL135704 IC50 = 11000.0 nM 4.96
CHEMBL424643 IC50 = 11000.0 nM 4.96
CHEMBL334832 IC50 = 11000.0 nM 4.96
CHEMBL132807 IC50 = 12000.0 nM 4.92
CHEMBL424465 IC50 = 19000.0 nM 4.72
CHEMBL335514 IC50 = 21000.0 nM 4.68
CHEMBL7550 L-158809 IC50 > 10000.0 nM -
CHEMBL136028 IC50 > 300.0 nM -
CHEMBL335276 IC50 > 10000.0 nM -
CHEMBL136034 IC50 > 110000.0 nM -
CHEMBL191 LOSARTAN IC50 > 30000.0 nM -
CHEMBL337217 IC50 > 30000.0 nM -
CHEMBL134754 IC50 > 10000.0 nM -