Assay Detail

CHEMBL5168512

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 by pathHunter assay

ChEMBL ↗

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Target

Glucagon-like peptide 1 receptor (CHEMBL1784) ↗

Open DB target context

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Glucagon-like peptide 1 receptor (CHEMBL1784) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Glucagon-like peptide 1 receptor

CHEMBL1784

Anchored from Assay target.

Protein identity Glucagon-like peptide 1 receptor

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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	4	7.07	8.05

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL414357	EXENATIDE	4.0	1	8.05
CHEMBL4084119	LIRAGLUTIDE	4.0	1	7.70
CHEMBL4518483	DANUGLIPRON	2.0	1	6.31
CHEMBL5191519	—	—	1	6.21

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL414357	EXENATIDE	EC50	=	9.0	nM	8.05
CHEMBL4084119	LIRAGLUTIDE	EC50	=	20.0	nM	7.70
CHEMBL4518483	DANUGLIPRON	EC50	=	490.0	nM	6.31
CHEMBL5191519	—	EC50	=	610.0	nM	6.21