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Assay Detail

CHEMBL5153399

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

Binding
Displacement of [125I]Sar1,I1e8-AII from AT1 receptor in rabbit aorta membrane
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.
Li G, Cheng Y, Han C, Song C, Huang N, Du Y.
RSC Med Chem (2022) 13 : 1300 -1321
PubMed 36439976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.71 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93226 1 9.46
CHEMBL332897 1 9.26
CHEMBL191 LOSARTAN 4.0 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93226 IC50 = 0.35 nM 9.46
CHEMBL332897 IC50 = 0.55 nM 9.26
CHEMBL191 LOSARTAN IC50 = 40.0 nM 7.40