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Assay Detail

CHEMBL647853

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

Binding
Inhibition of Angiotensin II receptor, type 2 in rat midbrain using [125I]-Sar1,Ile8 angiotensin II binding assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Type-2 angiotensin II receptor (CHEMBL257)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure-activity relationships of a novel series of non-peptide AT2-selective angiotensin II receptor antagonists
Wu M, Ikeler T, Ashton W, Chang R, Lotti V, Greenlee W
Bioorg Med Chem Lett (1993) 3 : 2023 -2028
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.97 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL60071 1 9.40
CHEMBL64861 1 9.22
CHEMBL293660 1 9.15
CHEMBL293625 1 8.96
CHEMBL63109 1 8.85
CHEMBL290829 1 8.82
CHEMBL64881 1 8.77
CHEMBL62422 1 8.57
CHEMBL59913 1 8.35
CHEMBL62744 1 8.15
CHEMBL62754 1 8.11
CHEMBL62806 1 8.00
CHEMBL292939 1 7.92
CHEMBL64280 1 7.82
CHEMBL291818 1 7.82
CHEMBL63046 1 7.82
CHEMBL60209 1 7.70
CHEMBL293195 1 7.64
CHEMBL299887 1 7.52
CHEMBL64575 1 7.46
CHEMBL293414 1 7.43
CHEMBL277567 1 7.40
CHEMBL59854 1 7.16
CHEMBL62157 1 7.09
CHEMBL64714 1 6.77
CHEMBL64674 1 6.75
CHEMBL303755 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL60071 IC50 = 0.4 nM 9.40
CHEMBL64861 IC50 = 0.6 nM 9.22
CHEMBL293660 IC50 = 0.7 nM 9.15
CHEMBL293625 IC50 = 1.1 nM 8.96
CHEMBL63109 IC50 = 1.4 nM 8.85
CHEMBL290829 IC50 = 1.5 nM 8.82
CHEMBL64881 IC50 = 1.7 nM 8.77
CHEMBL62422 IC50 = 2.7 nM 8.57
CHEMBL59913 IC50 = 4.5 nM 8.35
CHEMBL62744 IC50 = 7.0 nM 8.15
CHEMBL62754 IC50 = 7.8 nM 8.11
CHEMBL62806 IC50 = 10.0 nM 8.00
CHEMBL292939 IC50 = 12.0 nM 7.92
CHEMBL64280 IC50 = 15.0 nM 7.82
CHEMBL291818 IC50 = 15.0 nM 7.82
CHEMBL63046 IC50 = 15.0 nM 7.82
CHEMBL60209 IC50 = 20.0 nM 7.70
CHEMBL293195 IC50 = 23.0 nM 7.64
CHEMBL299887 IC50 = 30.0 nM 7.52
CHEMBL64575 IC50 = 35.0 nM 7.46
CHEMBL293414 IC50 = 37.0 nM 7.43
CHEMBL277567 IC50 = 40.0 nM 7.40
CHEMBL59854 IC50 = 70.0 nM 7.16
CHEMBL62157 IC50 = 82.0 nM 7.09
CHEMBL64714 IC50 = 170.0 nM 6.77
CHEMBL64674 IC50 = 180.0 nM 6.75
CHEMBL303755 IC50 = 230.0 nM 6.64