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Assay Detail

CHEMBL647850

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

Binding
Binding affinity towards Angiotensin II receptor, type 2 in rat isolated adrenal medullary microsomes
23
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Adrenal medulla
Subcellular Microsome
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

A novel series of selective, non-peptide inhibitors of angiotensin II binding to the AT2 site.
VanAtten MK, Ensinger CL, Chiu AT, McCall DE, Nguyen TT, Wexler RR, Timmermans PB.
J Med Chem (1993) 36 : 3985 -3992
PubMed 8258820 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.67 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL128527 1 7.52
CHEMBL336991 1 7.40
CHEMBL340778 1 7.40
CHEMBL128066 1 7.40
CHEMBL292277 1 7.40
CHEMBL340467 1 7.22
CHEMBL340902 3 7.16
CHEMBL339706 1 7.16
CHEMBL339485 1 7.05
CHEMBL338709 1 7.00
CHEMBL131940 1 6.70
CHEMBL128594 1 6.52
CHEMBL128065 1 6.52
CHEMBL340187 1 6.40
CHEMBL340933 1 6.22
CHEMBL419979 1 5.70
CHEMBL419974 1 5.70
CHEMBL128416 1 5.60
CHEMBL127844 1 5.30
CHEMBL340018 1 5.16
CHEMBL128233 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL128527 IC50 = 30.0 nM 7.52
CHEMBL336991 IC50 = 40.0 nM 7.40
CHEMBL340778 IC50 = 40.0 nM 7.40
CHEMBL128066 IC50 = 40.0 nM 7.40
CHEMBL292277 IC50 = 40.0 nM 7.40
CHEMBL340467 IC50 = 60.0 nM 7.22
CHEMBL340902 IC50 = 70.0 nM 7.16
CHEMBL339706 IC50 = 70.0 nM 7.16
CHEMBL340902 IC50 = 80.0 nM 7.10
CHEMBL339485 IC50 = 90.0 nM 7.05
CHEMBL340902 IC50 = 90.0 nM 7.05
CHEMBL338709 IC50 = 100.0 nM 7.00
CHEMBL131940 IC50 = 200.0 nM 6.70
CHEMBL128594 IC50 = 300.0 nM 6.52
CHEMBL128065 IC50 = 300.0 nM 6.52
CHEMBL340187 IC50 = 400.0 nM 6.40
CHEMBL340933 IC50 = 600.0 nM 6.22
CHEMBL419974 IC50 = 2000.0 nM 5.70
CHEMBL419979 IC50 = 2000.0 nM 5.70
CHEMBL128416 IC50 = 2500.0 nM 5.60
CHEMBL127844 IC50 = 5000.0 nM 5.30
CHEMBL340018 IC50 = 7000.0 nM 5.16
CHEMBL128233 IC50 > 10000.0 nM -