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Assay Detail

CHEMBL4703004

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

Binding
Displacement of [125I]-pyr-1-apelin-13 from EGFP-tagged wild-type rat apelin receptor expressed in CHO cell membranes by gamma counting method
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Apelin receptor (CHEMBL2398)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
IC50 25 9.00 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4787992 1 10.30
CHEMBL4751860 1 9.70
CHEMBL4764067 1 9.66
CHEMBL4786278 1 9.53
CHEMBL4795982 1 9.52
CHEMBL4750105 1 9.52
CHEMBL4789383 1 9.26
CHEMBL4065973 1 9.22
CHEMBL4744011 1 9.00
CHEMBL4753692 1 9.00
CHEMBL4740668 1 9.00
CHEMBL4759447 1 8.89
CHEMBL4797426 1 8.85
CHEMBL4758442 1 8.82
CHEMBL4788623 1 8.77
CHEMBL4775988 1 8.77
CHEMBL4755954 1 8.77
CHEMBL4799454 1 8.72
CHEMBL4761000 1 8.72
CHEMBL4745212 1 8.66
CHEMBL4763310 1 8.62
CHEMBL4744024 1 8.60
CHEMBL4794535 1 8.52
CHEMBL4741692 1 8.48
CHEMBL4760648 1 8.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4787992 IC50 = 0.05012 nM 10.30
CHEMBL4751860 IC50 = 0.1995 nM 9.70
CHEMBL4764067 IC50 = 0.2188 nM 9.66
CHEMBL4786278 IC50 = 0.2951 nM 9.53
CHEMBL4795982 IC50 = 0.302 nM 9.52
CHEMBL4750105 IC50 = 0.302 nM 9.52
CHEMBL4789383 IC50 = 0.5495 nM 9.26
CHEMBL4065973 IC50 = 0.6026 nM 9.22
CHEMBL4744011 IC50 = 1.0 nM 9.00
CHEMBL4753692 IC50 = 1.0 nM 9.00
CHEMBL4740668 IC50 = 1.0 nM 9.00
CHEMBL4759447 IC50 = 1.288 nM 8.89
CHEMBL4797426 IC50 = 1.413 nM 8.85
CHEMBL4758442 IC50 = 1.514 nM 8.82
CHEMBL4788623 IC50 = 1.698 nM 8.77
CHEMBL4775988 IC50 = 1.698 nM 8.77
CHEMBL4755954 IC50 = 1.698 nM 8.77
CHEMBL4799454 IC50 = 1.905 nM 8.72
CHEMBL4761000 IC50 = 1.905 nM 8.72
CHEMBL4745212 IC50 = 2.188 nM 8.66
CHEMBL4763310 IC50 = 2.399 nM 8.62
CHEMBL4744024 IC50 = 2.512 nM 8.60
CHEMBL4794535 IC50 = 3.02 nM 8.52
CHEMBL4741692 IC50 = 3.311 nM 8.48
CHEMBL4760648 IC50 = 6.31 nM 8.20