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Assay Detail

CHEMBL4703002

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

Functional
Activation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Chem-5
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Apelin receptor (CHEMBL1628481)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimizing PEG-Extended Apelin Analogues as Cardioprotective Drug Leads: Importance of the KFRR Motif and Aromatic Head Group for Improved Physiological Activity.
Fischer C,Lamer T,Fernandez K,Gheblawi M,Wang W,Pascoe C,Lambkin G,Iturrioz X,Llorens-Cortes C,Oudit GY,Vederas JC
J Med Chem (2020) 63 : 12073 -12082
PubMed 33001648 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 8.03 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4787992 1 8.72
CHEMBL4795982 1 8.62
CHEMBL4740668 1 8.62
CHEMBL4789383 1 8.60
CHEMBL4775988 1 8.54
CHEMBL4758442 1 8.46
CHEMBL4763310 1 8.31
CHEMBL4065973 1 8.31
CHEMBL4753692 1 8.27
CHEMBL4799454 1 8.21
CHEMBL4744011 1 8.21
CHEMBL4760648 1 8.11
CHEMBL4755954 1 8.09
CHEMBL4744024 1 7.77
CHEMBL4788623 1 7.59
CHEMBL4797426 1 7.40
CHEMBL4794535 1 7.31
CHEMBL4741692 1 7.27
CHEMBL4745212 1 7.13
CHEMBL4759447 1 7.05
CHEMBL4761000 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4787992 EC50 = 1.905 nM 8.72
CHEMBL4795982 EC50 = 2.399 nM 8.62
CHEMBL4740668 EC50 = 2.399 nM 8.62
CHEMBL4789383 EC50 = 2.512 nM 8.60
CHEMBL4775988 EC50 = 2.884 nM 8.54
CHEMBL4758442 EC50 = 3.467 nM 8.46
CHEMBL4763310 EC50 = 4.898 nM 8.31
CHEMBL4065973 EC50 = 4.898 nM 8.31
CHEMBL4753692 EC50 = 5.37 nM 8.27
CHEMBL4799454 EC50 = 6.166 nM 8.21
CHEMBL4744011 EC50 = 6.166 nM 8.21
CHEMBL4760648 EC50 = 7.762 nM 8.11
CHEMBL4755954 EC50 = 8.128 nM 8.09
CHEMBL4744024 EC50 = 16.98 nM 7.77
CHEMBL4788623 EC50 = 25.7 nM 7.59
CHEMBL4797426 EC50 = 39.81 nM 7.40
CHEMBL4794535 EC50 = 48.98 nM 7.31
CHEMBL4741692 EC50 = 53.7 nM 7.27
CHEMBL4745212 EC50 = 74.13 nM 7.13
CHEMBL4759447 EC50 = 89.13 nM 7.05
CHEMBL4761000 EC50 > 199.53 nM -