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Assay Detail

CHEMBL652358

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

Binding
In vitro binding affinity determined against angiotensin II AT1 receptor in rat adrenal cortex preparation
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Adrenal cortex
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

4,5-Dihydro-4-oxo-3H-imidazo[4,5-c]pyridines: potent arylacetic acid-derived AT1 antagonists with improved affinity for the AT2 receptor
Mederski WW, Dorsch D, Osswald M, Beier N, Lues I, Minck K, Schelling P, Ladstetter BJ
Bioorg Med Chem Lett (1995) 5 : 2665 -2670
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 8.21 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL89161 1 9.15
CHEMBL91465 1 8.54
CHEMBL328340 1 8.52
CHEMBL314603 1 8.51
CHEMBL88663 1 8.51
CHEMBL92479 1 8.44
CHEMBL313691 1 8.43
CHEMBL316063 1 8.40
CHEMBL315302 1 8.39
CHEMBL261981 1 8.38
CHEMBL329887 1 8.36
CHEMBL313142 1 8.25
CHEMBL420607 1 8.19
CHEMBL88170 1 8.19
CHEMBL328780 1 8.18
CHEMBL88600 1 8.15
CHEMBL328997 1 8.10
CHEMBL995 LOSARTAN POTASSIUM 4.0 1 8.09
CHEMBL314605 1 8.06
CHEMBL92206 1 8.05
CHEMBL315400 1 7.96
CHEMBL315401 1 7.96
CHEMBL90663 1 7.96
CHEMBL315483 1 7.85
CHEMBL329655 1 7.72
CHEMBL431592 1 7.68
CHEMBL265291 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL89161 IC50 = 0.7 nM 9.15
CHEMBL91465 IC50 = 2.9 nM 8.54
CHEMBL328340 IC50 = 3.0 nM 8.52
CHEMBL314603 IC50 = 3.1 nM 8.51
CHEMBL88663 IC50 = 3.1 nM 8.51
CHEMBL92479 IC50 = 3.6 nM 8.44
CHEMBL313691 IC50 = 3.7 nM 8.43
CHEMBL316063 IC50 = 4.0 nM 8.40
CHEMBL315302 IC50 = 4.1 nM 8.39
CHEMBL261981 IC50 = 4.2 nM 8.38
CHEMBL329887 IC50 = 4.4 nM 8.36
CHEMBL313142 IC50 = 5.6 nM 8.25
CHEMBL420607 IC50 = 6.5 nM 8.19
CHEMBL88170 IC50 = 6.5 nM 8.19
CHEMBL328780 IC50 = 6.6 nM 8.18
CHEMBL88600 IC50 = 7.1 nM 8.15
CHEMBL328997 IC50 = 8.0 nM 8.10
CHEMBL995 LOSARTAN POTASSIUM IC50 = 8.2 nM 8.09
CHEMBL314605 IC50 = 8.8 nM 8.06
CHEMBL92206 IC50 = 9.0 nM 8.05
CHEMBL315400 IC50 = 11.0 nM 7.96
CHEMBL315401 IC50 = 11.0 nM 7.96
CHEMBL90663 IC50 = 11.0 nM 7.96
CHEMBL315483 IC50 = 14.0 nM 7.85
CHEMBL329655 IC50 = 19.0 nM 7.72
CHEMBL431592 IC50 = 21.0 nM 7.68
CHEMBL265291 IC50 = 28.0 nM 7.55