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Assay Detail

CHEMBL652348

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

Binding
Binding affinity against AT1 receptor of rat adrenal cortical membranes
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Intermediate

Target

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

Publication

Non-peptide angiotensin II receptor antagonists: synthesis and biological activity of a series of novel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridine derivatives.
Mederski WW, Dorsch D, Bokel HH, Beier N, Lues I, Schelling P.
J Med Chem (1994) 37 : 1632 -1645
PubMed 8201597 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 8.57 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL295854 1 9.44
CHEMBL295928 1 9.22
CHEMBL288246 1 9.15
CHEMBL43535 1 9.15
CHEMBL418625 1 9.15
CHEMBL42775 1 9.10
CHEMBL291043 1 9.00
CHEMBL46822 1 8.96
CHEMBL43424 1 8.92
CHEMBL43500 1 8.89
CHEMBL297358 1 8.89
CHEMBL289291 1 8.85
CHEMBL42397 1 8.77
CHEMBL289507 1 8.72
CHEMBL298417 1 8.72
CHEMBL7550 L-158809 1 8.68
CHEMBL290248 1 8.66
CHEMBL296472 1 8.66
CHEMBL295456 1 8.64
CHEMBL429008 1 8.62
CHEMBL298464 1 8.49
CHEMBL45195 1 8.47
CHEMBL43171 1 8.46
CHEMBL45102 1 8.42
CHEMBL44925 1 8.38
CHEMBL430570 1 8.38
CHEMBL47187 1 8.37
CHEMBL295966 1 8.34
CHEMBL290907 1 8.34
CHEMBL42287 1 8.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL295854 IC50 = 0.36 nM 9.44
CHEMBL295928 IC50 = 0.6 nM 9.22
CHEMBL43535 IC50 = 0.7 nM 9.15
CHEMBL418625 IC50 = 0.7 nM 9.15
CHEMBL288246 IC50 = 0.7 nM 9.15
CHEMBL42775 IC50 = 0.8 nM 9.10
CHEMBL291043 IC50 = 1.0 nM 9.00
CHEMBL46822 IC50 = 1.1 nM 8.96
CHEMBL43424 IC50 = 1.2 nM 8.92
CHEMBL43500 IC50 = 1.3 nM 8.89
CHEMBL297358 IC50 = 1.3 nM 8.89
CHEMBL289291 IC50 = 1.4 nM 8.85
CHEMBL42397 IC50 = 1.7 nM 8.77
CHEMBL289507 IC50 = 1.9 nM 8.72
CHEMBL298417 IC50 = 1.9 nM 8.72
CHEMBL7550 L-158809 IC50 = 2.1 nM 8.68
CHEMBL290248 IC50 = 2.2 nM 8.66
CHEMBL296472 IC50 = 2.2 nM 8.66
CHEMBL295456 IC50 = 2.3 nM 8.64
CHEMBL429008 IC50 = 2.4 nM 8.62
CHEMBL298464 IC50 = 3.2 nM 8.49
CHEMBL45195 IC50 = 3.4 nM 8.47
CHEMBL43171 IC50 = 3.5 nM 8.46
CHEMBL45102 IC50 = 3.8 nM 8.42
CHEMBL44925 IC50 = 4.2 nM 8.38
CHEMBL430570 IC50 = 4.2 nM 8.38
CHEMBL47187 IC50 = 4.3 nM 8.37
CHEMBL295966 IC50 = 4.6 nM 8.34
CHEMBL290907 IC50 = 4.6 nM 8.34
CHEMBL42287 IC50 = 5.6 nM 8.25
CHEMBL295929 IC50 = 5.7 nM 8.24
CHEMBL42101 IC50 = 5.7 nM 8.24
CHEMBL42184 IC50 = 6.0 nM 8.22
CHEMBL907 CARBOXYLIC ACID METABOLITE IC50 = 7.5 nM 8.12
CHEMBL995 LOSARTAN POTASSIUM IC50 = 8.2 nM 8.09
CHEMBL288705 IC50 = 16.8 nM 7.78
CHEMBL289448 IC50 = 30.0 nM 7.52
CHEMBL42631 IC50 = 56.0 nM 7.25