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Assay Detail

CHEMBL4775348

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Binding
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Galpha(i1)-RlucII(91) assessed as induction of dissociation of Galpha(i1) from G-beta-gamma subunits incubated for 5 mins by BRET assay
23
Total Activities
23
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

Structure-Activity Relationship and Bioactivity of Short Analogues of ELABELA as Agonists of the Apelin Receptor.
Trân K,Murza A,Sainsily X,Delile E,Couvineau P,Côté J,Coquerel D,Peloquin M,Auger-Messier M,Bouvier M,Lesur O,Sarret P,Marsault É
J Med Chem (2021) 64 : 602 -615
PubMed 33350824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 8.29 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4791583 1 8.96
CHEMBL3184840 1 8.96
CHEMBL4797921 1 8.92
CHEMBL4777690 1 8.64
CHEMBL4789289 1 8.62
CHEMBL4790636 1 8.55
CHEMBL4781348 1 8.42
CHEMBL4791473 1 8.40
CHEMBL4793361 1 8.35
CHEMBL4788480 1 8.34
CHEMBL4795339 1 8.29
CHEMBL4796315 1 8.28
CHEMBL4791398 1 8.24
CHEMBL4787249 1 8.24
CHEMBL4792840 1 8.19
CHEMBL4797169 1 8.16
CHEMBL4785339 1 8.15
CHEMBL4788436 1 8.10
CHEMBL4779171 1 7.96
CHEMBL4795334 1 7.85
CHEMBL4794333 1 7.77
CHEMBL4780010 1 7.72
CHEMBL4778604 1 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4791583 EC50 = 1.1 nM 8.96
CHEMBL3184840 EC50 = 1.1 nM 8.96
CHEMBL4797921 EC50 = 1.2 nM 8.92
CHEMBL4777690 EC50 = 2.3 nM 8.64
CHEMBL4789289 EC50 = 2.4 nM 8.62
CHEMBL4790636 EC50 = 2.8 nM 8.55
CHEMBL4781348 EC50 = 3.8 nM 8.42
CHEMBL4791473 EC50 = 4.0 nM 8.40
CHEMBL4793361 EC50 = 4.5 nM 8.35
CHEMBL4788480 EC50 = 4.6 nM 8.34
CHEMBL4795339 EC50 = 5.1 nM 8.29
CHEMBL4796315 EC50 = 5.3 nM 8.28
CHEMBL4791398 EC50 = 5.8 nM 8.24
CHEMBL4787249 EC50 = 5.8 nM 8.24
CHEMBL4792840 EC50 = 6.4 nM 8.19
CHEMBL4797169 EC50 = 6.9 nM 8.16
CHEMBL4785339 EC50 = 7.0 nM 8.15
CHEMBL4788436 EC50 = 8.0 nM 8.10
CHEMBL4779171 EC50 = 11.0 nM 7.96
CHEMBL4795334 EC50 = 14.0 nM 7.85
CHEMBL4794333 EC50 = 17.0 nM 7.77
CHEMBL4780010 EC50 = 19.0 nM 7.72
CHEMBL4778604 EC50 = 23.0 nM 7.64