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Assay Detail

CHEMBL5168495

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Functional
Agonist activity at human GLP-1R expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins in absence of BETP by plate reader method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor.
Griffith DA, Edmonds DJ, Fortin JP, Kalgutkar AS, Kuzmiski JB, Loria PM, Saxena AR, Bagley SW, Buckeridge C, Curto JM, Derksen DR, Dias JM, Griffor MC, Han S, Jackson VM, Landis MS, Lettiere D, Limberakis C, Liu Y, Mathiowetz AM, Patel JC, Piotrowski DW, Price DA, Ruggeri RB, Tess DA.
J Med Chem (2022) 65 : 8208 -8226
PubMed 35647711 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.95 10.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414357 EXENATIDE 4.0 1 10.21
CHEMBL4084119 LIRAGLUTIDE 4.0 1 9.41
CHEMBL5191519 1 9.12
CHEMBL4518483 DANUGLIPRON 2.0 1 8.96
CHEMBL5182388 1 7.02
CHEMBL5209130 1 5.58
CHEMBL5208289 1 5.34
CHEMBL5206786 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414357 EXENATIDE EC50 = 0.061 nM 10.21
CHEMBL4084119 LIRAGLUTIDE EC50 = 0.39 nM 9.41
CHEMBL5191519 EC50 = 0.75 nM 9.12
CHEMBL4518483 DANUGLIPRON EC50 = 1.1 nM 8.96
CHEMBL5182388 EC50 = 95.0 nM 7.02
CHEMBL5209130 EC50 = 2600.0 nM 5.58
CHEMBL5208289 EC50 = 4600.0 nM 5.34
CHEMBL5206786 EC50 > 20000.0 nM -