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Assay Detail

CHEMBL3421350

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

Binding
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-2 recruitment subunit dissociation incubated for 30 mins by BRET assay
2
Total Activities
2
Compounds Tested
1
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

Apelin receptor (CHEMBL1628481)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

C-Terminal modifications of apelin-13 significantly change ligand binding, receptor signaling, and hypotensive action.
Murza A, Besserer-Offroy É, Côté J, Bérubé P, Longpré JM, Dumaine R, Lesur O, Auger-Messier M, Leduc R, Sarret P, Marsault É.
J Med Chem (2015) 58 : 2431 -2440
PubMed 25668242 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.72 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3417384 1 7.89
CHEMBL3184840 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3417384 EC50 = 13.0 nM 7.89
CHEMBL3184840 EC50 = 29.0 nM 7.54