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Assay Detail

CHEMBL648566

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

Binding
Tested for inhibition of Angiotensin II receptor, type 1 in the absence of bovine serum albumin (BSA)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Type-1 angiotensin II receptor (CHEMBL227)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Valsartan, a potent, orally active angiotensin II antagonist developed from the structurally new amino acid series
Buhlmayer P, Furet P, Criscione L, de Gasparo M, Whitebread S, Schmidlin T, Lattmann R, Wood J
Bioorg Med Chem Lett (1994) 4 : 29 -34
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.32 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1069 VALSARTAN 4.0 1 8.57
CHEMBL116298 1 8.22
CHEMBL191 LOSARTAN 4.0 1 8.10
CHEMBL112523 1 7.62
CHEMBL115783 1 7.52
CHEMBL326349 1 7.22
CHEMBL117941 1 7.22
CHEMBL114653 1 6.70
CHEMBL323911 1 6.57
CHEMBL115622 1 6.52
CHEMBL326140 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1069 VALSARTAN IC50 = 2.7 nM 8.57
CHEMBL116298 IC50 = 6.0 nM 8.22
CHEMBL191 LOSARTAN IC50 = 8.0 nM 8.10
CHEMBL112523 IC50 = 24.0 nM 7.62
CHEMBL115783 IC50 = 30.0 nM 7.52
CHEMBL326349 IC50 = 60.0 nM 7.22
CHEMBL117941 IC50 = 60.0 nM 7.22
CHEMBL114653 IC50 = 200.0 nM 6.70
CHEMBL323911 IC50 = 270.0 nM 6.57
CHEMBL115622 IC50 = 300.0 nM 6.52
CHEMBL326140 IC50 = 600.0 nM 6.22