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Assay Detail

CHEMBL5366266

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

Binding
Displacement of [125I]-GLP1 from GLP-1 receptor (unknown origin) expressed in CHO cells membrane pre-incubated for 10 mins followed by [125I]-GLP1 addition and measured after 180 mins by microbeta scintillation counting method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

6-Azaspiro[2.5]octanes as small molecule agonists of the human glucagon-like peptide-1 receptor.
Aspnes GE, Bagley SW, Coffey SB, Conn EL, Curto JM, Edmonds DJ, Genovino J, Griffith DA, Ingle G, Jiao W, Limberakis C, Mathiowetz AM, Piotrowski DW, Rose CR, Ruggeri RB, Wei L.
Bioorg Med Chem Lett (2023) 94 : 129454 -129454
PubMed 37591316 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.85 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5418836 1 8.39
CHEMBL5440900 1 8.24
CHEMBL4518483 DANUGLIPRON 2.0 1 7.89
CHEMBL5429544 1 7.85
CHEMBL5396298 1 7.82
CHEMBL5399359 1 7.82
CHEMBL5434776 1 7.72
CHEMBL5419346 1 7.50
CHEMBL5414345 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5418836 EC50 = 4.1 nM 8.39
CHEMBL5440900 EC50 = 5.8 nM 8.24
CHEMBL4518483 DANUGLIPRON EC50 = 13.0 nM 7.89
CHEMBL5429544 EC50 = 14.0 nM 7.85
CHEMBL5396298 EC50 = 15.0 nM 7.82
CHEMBL5399359 EC50 = 15.0 nM 7.82
CHEMBL5434776 EC50 = 19.0 nM 7.72
CHEMBL5419346 EC50 = 32.0 nM 7.50
CHEMBL5414345 EC50 = 35.0 nM 7.46