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Assay Detail

CHEMBL3830508

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

Binding
Displacement of [125I-Sar1-Ile8]Ang2 from human AT1 receptor expressed in HEK293 cell membrane incubated for 1 hr by gamma counting method
10
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Type-1 angiotensin II receptor (CHEMBL227)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploring new scaffolds for angiotensin II receptor antagonism.
Kritsi E, Matsoukas MT, Potamitis C, Karageorgos V, Detsi A, Magafa V, Liapakis G, Mavromoustakos T, Zoumpoulakis P.
Bioorg Med Chem (2016) 24 : 4444 -4451
PubMed 27480029 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.47 8.49
Inhibition 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191 LOSARTAN 4.0 1 8.49
CHEMBL1332729 3 6.70
CHEMBL1374011 2 5.68
CHEMBL1474431 2 5.66
CHEMBL1716544 2 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191 LOSARTAN IC50 = 3.236 nM 8.49
CHEMBL1332729 IC50 = 199.53 nM 6.70
CHEMBL1332729 IC50 = 199.0 nM 6.70
CHEMBL1374011 IC50 = 2089.3 nM 5.68
CHEMBL1474431 IC50 = 2187.76 nM 5.66
CHEMBL1716544 IC50 = 2570.4 nM 5.59
CHEMBL1332729 Inhibition - % -
CHEMBL1716544 Inhibition - % -
CHEMBL1374011 Inhibition - % -
CHEMBL1474431 Inhibition - % -