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Assay Detail

CHEMBL2060169

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

Binding
Displacement of [125I]AngII from type 1 angiotensin 2 receptor in 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 Autocuration

Target

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

Publication

Synthesis and biological evaluation of 4'-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists.
Bai R, Wei Z, Liu J, Xie W, Yao H, Wu X, Jiang J, Wang Q, Xu J.
Bioorg Med Chem (2012) 20 : 4661 -4667
PubMed 22750010 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.75 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2058372 1 8.07
CHEMBL2058371 1 8.04
CHEMBL2058373 1 8.01
CHEMBL2058370 1 8.00
CHEMBL2058374 1 8.00
CHEMBL2058375 1 7.98
CHEMBL2058376 1 7.96
CHEMBL2058377 1 7.92
CHEMBL2058369 1 7.80
CHEMBL2058368 1 7.55
CHEMBL2058367 1 7.35
CHEMBL2058366 1 7.04
CHEMBL191 LOSARTAN 4.0 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2058372 IC50 = 8.5 nM 8.07
CHEMBL2058371 IC50 = 9.1 nM 8.04
CHEMBL2058373 IC50 = 9.8 nM 8.01
CHEMBL2058370 IC50 = 9.9 nM 8.00
CHEMBL2058374 IC50 = 10.0 nM 8.00
CHEMBL2058375 IC50 = 10.5 nM 7.98
CHEMBL2058376 IC50 = 11.0 nM 7.96
CHEMBL2058377 IC50 = 12.0 nM 7.92
CHEMBL2058369 IC50 = 16.0 nM 7.80
CHEMBL2058368 IC50 = 28.0 nM 7.55
CHEMBL2058367 IC50 = 45.0 nM 7.35
CHEMBL2058366 IC50 = 92.0 nM 7.04
CHEMBL191 LOSARTAN IC50 = 95.0 nM 7.02