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Assay Detail

CHEMBL4023909

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

Binding
Induction of human HA-tagged APJ receptor internalization expressed in HEK293 cells after 30 mins by ELISA
3
Total Activities
3
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

A Systematic Exploration of Macrocyclization in Apelin-13: Impact on Binding, Signaling, Stability, and Cardiovascular Effects.
Trân K, Murza A, Sainsily X, Coquerel D, Côté J, Belleville K, Haroune L, Longpré JM, Dumaine R, Salvail D, Lesur O, Auger-Messier M, Sarret P, Marsault É.
J Med Chem (2018) 61 : 2266 -2277
PubMed 29461833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.10 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3184840 1 7.62
CHEMBL4094033 1 7.35
CHEMBL4076755 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3184840 EC50 = 24.0 nM 7.62
CHEMBL4094033 EC50 = 45.0 nM 7.35
CHEMBL4076755 EC50 = 469.0 nM 6.33