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Assay Detail

CHEMBL5344102

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Functional
Agonist activity at N-terminal HA-tagged human GLP-1R expressed in HEK293 cells assessed as change in intracellular calcium level by Fluo-4 AM dye based calcium mobilization assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glucagon-like peptide 1 receptor (CHEMBL1784)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Novel 5,6-Dihydro-1,2,4-triazine Derivatives as Efficacious Glucagon-Like Peptide-1 Receptor Agonists.
Chen L, Yun Y, Guo S, Wang X, Xiong M, Zhao T, Xu T, Shen J, Xie X, Wang K.
J Med Chem (2023) 66 : 7988 -8010
PubMed 37286364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.58 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL410972 1 7.17
CHEMBL5408881 1 6.78
CHEMBL4518483 DANUGLIPRON 2.0 1 5.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL410972 EC50 = 67.0 nM 7.17
CHEMBL5408881 EC50 = 168.0 nM 6.78
CHEMBL4518483 DANUGLIPRON EC50 = 1610.0 nM 5.79