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Assay Detail

CHEMBL652721

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

Binding
Displacement of [125I]Sar1-Ile8-AII (without BSA) from type 1 Angiotensin II receptor of rabbit aorta
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Type-1 angiotensin II receptor (CHEMBL3948)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Quinazolinones 2: QSAR and in vivo characterization of AT1 selective AII antagonists
de Laszlo SE, Allen EE, Quagliato CS, Greenlee WJ, Patchett AA, Nachbar RB, Sieg PK, Chang RS, Kivlighn SD, Schorn TS, Faust KA, Chen T, Zingaro GJ, Lotti VJ
Bioorg Med Chem Lett (1993) 3 : 1299 -1304
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.67 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24322 1 10.00
CHEMBL25585 1 9.30
CHEMBL26614 1 9.24
CHEMBL287184 1 9.05
CHEMBL422756 1 8.96
CHEMBL26217 1 8.96
CHEMBL24861 1 8.80
CHEMBL280526 1 8.80
CHEMBL24661 1 8.40
CHEMBL25313 1 8.30
CHEMBL26548 1 8.12
CHEMBL281846 1 8.05
CHEMBL286260 1 7.92
CHEMBL24764 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24322 IC50 = 0.1 nM 10.00
CHEMBL25585 IC50 = 0.5 nM 9.30
CHEMBL26614 IC50 = 0.58 nM 9.24
CHEMBL287184 IC50 = 0.9 nM 9.05
CHEMBL422756 IC50 = 1.1 nM 8.96
CHEMBL26217 IC50 = 1.1 nM 8.96
CHEMBL24861 IC50 = 1.6 nM 8.80
CHEMBL280526 IC50 = 1.6 nM 8.80
CHEMBL24661 IC50 = 4.0 nM 8.40
CHEMBL25313 IC50 = 5.0 nM 8.30
CHEMBL26548 IC50 = 7.6 nM 8.12
CHEMBL281846 IC50 = 8.9 nM 8.05
CHEMBL286260 IC50 = 12.0 nM 7.92
CHEMBL24764 IC50 = 30.0 nM 7.52