Target family: Glucagon receptor family (type: gpcr)
Target: GLP-1 receptor

Ligand: WB4-24 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.920000076293945 pA2
Reference (Journal): The non-peptide GLP-1 receptor agonist WB4-24 blocks inflammatory nociception by stimulating β-endorphin release from spinal microglia.
Published in: Br J Pharmacol

Ligand: tirzepatide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: EMA & FDA (2022)
Primary target: no
Median affinity: 8.369999885559082 pKi
Reference (Journal): LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept.
Published in: Mol Metab

Ligand: taspoglutide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.220000267028809 pEC50
Reference (Journal): Taspoglutide, an analog of human glucagon-like Peptide-1 with enhanced stability and in vivo potency.
Published in: Endocrinology

Ligand: T-0632 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4.699999809265137 pIC50
Reference (Journal): A small molecule ligand of the glucagon-like peptide 1 receptor targets its amino-terminal hormone binding domain.
Published in: J Biol Chem

Ligand: survodutide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.479999542236328 pEC50
Reference (Journal): BI 456906: Discovery and preclinical pharmacology of a novel GCGR/GLP-1R dual agonist with robust anti-obesity efficacy.
Published in: Mol Metab

Ligand: survodutide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.4399995803833 pEC50
Reference (Journal): BI 456906: Discovery and preclinical pharmacology of a novel GCGR/GLP-1R dual agonist with robust anti-obesity efficacy.
Published in: Mol Metab

Ligand: [125I]GLP-1-(7-37) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [125I]GLP-1-(7-36)-amide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pKd
Reference (Journal): Characterization of glucagon-like peptide-1 receptor beta-arrestin 2 interaction: a high-affinity receptor phenotype.
Published in: Mol Endocrinol

Ligand: [125I]exendin-(9-39) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKd
Reference (Journal): Characterization of glucagon-like peptide-1 receptor beta-arrestin 2 interaction: a high-affinity receptor phenotype.
Published in: Mol Endocrinol

Ligand: semaglutide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2017), EMA (2018)
Primary target: yes
Median affinity: 11.210000038146973 pEC50
Reference (Journal): Discovery of the Once-Weekly Glucagon-Like Peptide-1 (GLP-1) Analogue Semaglutide.
Published in: J Med Chem

Ligand: semaglutide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2017), EMA (2018)
Primary target: yes
Median affinity: 9.420000076293945 pIC50
Reference (Journal): Discovery of the Once-Weekly Glucagon-Like Peptide-1 (GLP-1) Analogue Semaglutide.
Published in: J Med Chem

Ligand: Peptide 5 [PMID: 28562585] (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi
Reference (Journal): Crystal structure of the GLP-1 receptor bound to a peptide agonist.
Published in: Nature

Ligand: Peptide 5 [PMID: 28562585] (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.800000190734863 pEC50
Reference (Journal): Crystal structure of the GLP-1 receptor bound to a peptide agonist.
Published in: Nature

Ligand: orforglipron (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.489999771118164 pKi
Reference (Journal): Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist.
Published in: Proc Natl Acad Sci U S A

Ligand: maridebart cafraglutide (Antibody)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.610000133514404 pEC50
Reference (Journal): A GIPR antagonist conjugated to GLP-1 analogues promotes weight loss with improved metabolic parameters in preclinical and phase 1 settings.
Published in: Nat Metab

Ligand: maridebart cafraglutide (Antibody)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.239999771118164 pEC50
Reference (Journal): A GIPR antagonist conjugated to GLP-1 analogues promotes weight loss with improved metabolic parameters in preclinical and phase 1 settings.
Published in: Nat Metab

Ligand: maridebart cafraglutide (Antibody)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.619999885559082 pEC50
Reference (Journal): A GIPR antagonist conjugated to GLP-1 analogues promotes weight loss with improved metabolic parameters in preclinical and phase 1 settings.
Published in: Nat Metab

Ligand: LSN3318839 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 7.849999904632568 pEC50
Reference (Journal): Discovery of an Orally Efficacious Positive Allosteric Modulator of the Glucagon-like Peptide-1 Receptor.
Published in: J Med Chem

Ligand: lixisenatide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: EMA (2013), FDA (2016)
Primary target: yes
Median affinity: 8.880000114440918 pKi
Reference (Journal): Pharmacological profile of lixisenatide: A new GLP-1 receptor agonist for the treatment of type 2 diabetes.
Published in: Regul Pept

Ligand: liraglutide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2009), FDA (2010)
Primary target: yes
Median affinity: 10.199999809265137 pEC50
Reference (Journal): Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administration.
Published in: J Med Chem

Ligand: glucagon-like peptide 1-(7-37) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Cloning and functional expression of the human glucagon-like peptide-1 (GLP-1) receptor.
Published in: Endocrinology

Ligand: glucagon-like peptide 1-(7-36) amide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Characterization of glucagon-like peptide-1 receptor beta-arrestin 2 interaction: a high-affinity receptor phenotype.
Published in: Mol Endocrinol