Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL652723

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

Binding
Ability to displace [125I]Sar1-Ile8-AII from angiotensin II receptor, type 1 in rabbit aorta in presence of 0.2% bovine serum albumin (BSA) was determined in vitro
31
Total Activities
31
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 31 8.09 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25585 1 9.12
CHEMBL25315 1 9.08
CHEMBL25056 1 9.00
CHEMBL287184 1 9.00
CHEMBL24724 1 8.89
CHEMBL24053 1 8.70
CHEMBL281846 1 8.70
CHEMBL26548 1 8.52
CHEMBL24861 1 8.47
CHEMBL422756 1 8.40
CHEMBL23994 1 8.40
CHEMBL282236 1 8.37
CHEMBL25000 1 8.30
CHEMBL24240 1 8.30
CHEMBL24661 1 8.30
CHEMBL279515 1 8.22
CHEMBL280526 1 8.19
CHEMBL282746 1 8.15
CHEMBL26217 1 8.10
CHEMBL277182 1 8.05
CHEMBL24688 1 7.89
CHEMBL284764 1 7.70
CHEMBL25075 1 7.58
CHEMBL26514 1 7.57
CHEMBL24488 1 7.55
CHEMBL422932 1 7.54
CHEMBL284455 1 7.48
CHEMBL24111 1 7.30
CHEMBL287253 1 7.04
CHEMBL25767 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25585 IC50 = 0.75 nM 9.12
CHEMBL25315 IC50 = 0.83 nM 9.08
CHEMBL25056 IC50 = 1.0 nM 9.00
CHEMBL287184 IC50 = 1.0 nM 9.00
CHEMBL24724 IC50 = 1.3 nM 8.89
CHEMBL24053 IC50 = 2.0 nM 8.70
CHEMBL281846 IC50 = 2.0 nM 8.70
CHEMBL26548 IC50 = 3.0 nM 8.52
CHEMBL24861 IC50 = 3.4 nM 8.47
CHEMBL422756 IC50 = 4.0 nM 8.40
CHEMBL23994 IC50 = 4.0 nM 8.40
CHEMBL282236 IC50 = 4.3 nM 8.37
CHEMBL25000 IC50 = 5.0 nM 8.30
CHEMBL24240 IC50 = 5.0 nM 8.30
CHEMBL24661 IC50 = 5.0 nM 8.30
CHEMBL279515 IC50 = 6.0 nM 8.22
CHEMBL280526 IC50 = 6.4 nM 8.19
CHEMBL282746 IC50 = 7.0 nM 8.15
CHEMBL26217 IC50 = 8.0 nM 8.10
CHEMBL277182 IC50 = 9.0 nM 8.05
CHEMBL24688 IC50 = 13.0 nM 7.89
CHEMBL284764 IC50 = 20.0 nM 7.70
CHEMBL25075 IC50 = 26.0 nM 7.58
CHEMBL26514 IC50 = 27.0 nM 7.57
CHEMBL24488 IC50 = 28.0 nM 7.55
CHEMBL422932 IC50 = 29.0 nM 7.54
CHEMBL284455 IC50 = 33.0 nM 7.48
CHEMBL24111 IC50 = 50.0 nM 7.30
CHEMBL287253 IC50 = 92.0 nM 7.04
CHEMBL25767 IC50 = 120.0 nM 6.92
CHEMBL284469 IC50 = 940.0 nM 6.03