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Assay Detail

CHEMBL5168501

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

Functional
Agonist activity at human GLP-1R expressed in PathHunter CHO-K1 GLP1R beta-arrestin-2 cell assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins in presence of BETP by PathHunter assay
3
Total Activities
3
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 3 5.46 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5208289 1 5.82
CHEMBL5182388 1 5.55
CHEMBL5209130 1 5.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5208289 EC50 = 1500.0 nM 5.82
CHEMBL5182388 EC50 = 2800.0 nM 5.55
CHEMBL5209130 EC50 = 9600.0 nM 5.02