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Assay Detail

CHEMBL4401048

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

Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Apelin receptor (CHEMBL1628481)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Plasma kallikrein cleaves and inactivates apelin-17: Palmitoyl- and PEG-extended apelin-17 analogs as metabolically stable blood pressure-lowering agents.
Fischer C, Lamer T, Wang W, McKinnie SMK, Iturrioz X, Llorens-Cortes C, Oudit GY, Vederas JC.
Eur J Med Chem (2019) 166 : 119 -124
PubMed 30690406 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.97 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3234446 1 8.72
CHEMBL4472749 1 8.60
CHEMBL4550078 1 8.59
CHEMBL4098390 1 8.39
CHEMBL4065973 1 8.31
CHEMBL4464954 1 8.20
CHEMBL4440817 1 7.95
CHEMBL4439951 1 6.75
CHEMBL4559795 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3234446 EC50 = 1.9 nM 8.72
CHEMBL4472749 EC50 = 2.5 nM 8.60
CHEMBL4550078 EC50 = 2.6 nM 8.59
CHEMBL4098390 EC50 = 4.1 nM 8.39
CHEMBL4065973 EC50 = 4.9 nM 8.31
CHEMBL4464954 EC50 = 6.3 nM 8.20
CHEMBL4440817 EC50 = 11.3 nM 7.95
CHEMBL4439951 EC50 = 176.0 nM 6.75
CHEMBL4559795 EC50 = 568.0 nM 6.25