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Assay Detail

CHEMBL646975

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

Binding
Inhibition of [125l]-All binding to bovine adrenal cortex
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Tissue Adrenal cortex
Confidence 9 — Direct single protein target
Curated By Expert

Target

Type-1 angiotensin II receptor (CHEMBL3374)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Angiotensin II receptor antagonists: imidazoles and pyrroles bearing hydroxymethyl and carboxy substituents
Yanagisawa H, Amemiya Y, Kanazaki T, Fujimoto K, Shimoji Y, Fujimoto Y, Sada T, Mizuno M, Koike H
Bioorg Med Chem Lett (1994) 4 : 177 -182
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.38 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL907 CARBOXYLIC ACID METABOLITE 1 7.66
CHEMBL417366 1 7.24
CHEMBL299809 1 7.19
CHEMBL191 LOSARTAN 4.0 1 6.92
CHEMBL49170 1 6.89
CHEMBL50092 1 6.82
CHEMBL300186 1 6.50
CHEMBL274447 1 6.31
CHEMBL439743 1 6.08
CHEMBL53631 1 5.68
CHEMBL52601 1 5.57
CHEMBL50592 1 5.35
CHEMBL53322 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL907 CARBOXYLIC ACID METABOLITE IC50 = 22.0 nM 7.66
CHEMBL417366 IC50 = 58.0 nM 7.24
CHEMBL299809 IC50 = 65.0 nM 7.19
CHEMBL191 LOSARTAN IC50 = 120.0 nM 6.92
CHEMBL49170 IC50 = 130.0 nM 6.89
CHEMBL50092 IC50 = 150.0 nM 6.82
CHEMBL300186 IC50 = 320.0 nM 6.50
CHEMBL274447 IC50 = 490.0 nM 6.31
CHEMBL439743 IC50 = 840.0 nM 6.08
CHEMBL53631 IC50 = 2100.0 nM 5.68
CHEMBL52601 IC50 = 2700.0 nM 5.57
CHEMBL50592 IC50 = 4500.0 nM 5.35
CHEMBL53322 IC50 = 20000.0 nM 4.70