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Assay Detail

CHEMBL876751

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

Binding
Concentration required for 50% inhibition of binding against Angiotensin II receptor, type 1 in rat adrenal cortex
16
Total Activities
16
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

(6-oxo-3-pyridazinyl)-benzimidazoles as potent angiotensin II receptor antagonists
Dorsch D, Mederski WW, Beier N, Lues I, Minck K, Schelling P
Bioorg Med Chem Lett (1994) 4 : 1297 -1302
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.47 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2079789 1 8.80
CHEMBL2079788 1 8.77
CHEMBL24266 1 8.74
CHEMBL24224 1 8.74
CHEMBL2079792 1 8.55
CHEMBL2079790 1 8.54
CHEMBL284704 1 8.49
CHEMBL2079785 1 8.47
CHEMBL2079786 1 8.44
CHEMBL2079791 1 8.44
CHEMBL26389 1 8.36
CHEMBL2079787 1 8.33
CHEMBL26437 1 8.30
CHEMBL25989 1 8.20
CHEMBL284703 1 8.19
CHEMBL191 LOSARTAN 4.0 1 8.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2079789 IC50 = 1.6 nM 8.80
CHEMBL2079788 IC50 = 1.7 nM 8.77
CHEMBL24266 IC50 = 1.8 nM 8.74
CHEMBL24224 IC50 = 1.8 nM 8.74
CHEMBL2079792 IC50 = 2.8 nM 8.55
CHEMBL2079790 IC50 = 2.9 nM 8.54
CHEMBL284704 IC50 = 3.2 nM 8.49
CHEMBL2079785 IC50 = 3.4 nM 8.47
CHEMBL2079786 IC50 = 3.6 nM 8.44
CHEMBL2079791 IC50 = 3.6 nM 8.44
CHEMBL26389 IC50 = 4.4 nM 8.36
CHEMBL2079787 IC50 = 4.7 nM 8.33
CHEMBL26437 IC50 = 5.0 nM 8.30
CHEMBL25989 IC50 = 6.3 nM 8.20
CHEMBL284703 IC50 = 6.5 nM 8.19
CHEMBL191 LOSARTAN IC50 = 8.2 nM 8.09