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Assay Detail

CHEMBL647851

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

Binding
Compound was evaluated for inhibition of 125I[Sar1,Ile8] aII binding to rat midbrain membrane preparation Angiotensin II receptor, type 2
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Midbrain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

L-162,389: a potent orally active angiotensin II receptor antagonist with balanced affinity to both AT1 and AT2 receptor subtypes
Rivero R, Kevin N, Kivlighn S, Zingaro G, Chang R, Greenlee W
Bioorg Med Chem Lett (1996) 6 : 307 -310
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.09 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39959 1 8.42
CHEMBL449095 1 7.43
CHEMBL105199 1 7.06
CHEMBL318605 1 7.02
CHEMBL293511 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39959 IC50 = 3.8 nM 8.42
CHEMBL449095 IC50 = 37.0 nM 7.43
CHEMBL105199 IC50 = 87.0 nM 7.06
CHEMBL318605 IC50 = 95.0 nM 7.02
CHEMBL293511 IC50 = 2900.0 nM 5.54