Target family: Glucagon receptor family (type: gpcr)
Target: glucagon receptor

Ligand: survodutide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.279999732971191 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]glucagon (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: RVT-1502 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): LGD‐6972, a potent, orally‐bioavailable, small molecule glucagon receptor antagonist for the treatment of type 2 diabetes
Published in: Diabetes

Ligand: NNC 92-1687 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi
Reference (Journal): Discovery and structure-activity relationship of the first non-peptide competitive human glucagon receptor antagonists.
Published in: J Med Chem

Ligand: NNC1702 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.269999980926514 pIC50
Reference (Journal): Structure of the glucagon receptor in complex with a glucagon analogue.
Published in: Nature

Ligand: NNC0640 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 7.159999847412109 pIC50
Reference (Journal): Structure of the full-length glucagon class B G-protein-coupled receptor.
Published in: Nature

Ligand: MK-0893 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: yes
Median affinity: 8.180000305175781 pIC50
Reference (Journal): Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes.
Published in: J Med Chem

Ligand: L-168,049 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor.
Published in: J Biol Chem

Ligand: hGCGR antagonist (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.1 pIC50
Reference (Journal): A novel glucagon receptor antagonist inhibits glucagon-mediated biological effects.
Published in: Diabetes

Ligand: hGCGR antagonist (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pIC50
Reference (Journal): Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.
Published in: Bioorg Med Chem Lett

Ligand: glucagon-(1-6) (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 4 pEC50
Reference (Journal): Glucagon1-6 binds to the glucagon receptor and activates hepatic adenylate cyclase.
Published in: J Biol Chem

Ligand: glucagon-(1-21) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6 pEC50
Reference (Journal): A reassessment of structure-function relationships in glucagon. Glucagon1-21 is a full agonist.
Published in: J Biol Chem

Ligand: glucagon (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1960)
Primary target: yes
Median affinity: 9 pEC50
Reference (Journal): Glucagon-sensitive adenyl cylase in plasma membrane of hepatic parenchymal cells.
Published in: Science

Ligand: des-His1-[Leu4-Glu9]glucagon-NH2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Development of potent glucagon antagonists: structure-activity relationship study of glycine at position 4.
Published in: J Pept Res

Ligand: des-His1-[Glu9]glucagon-NH2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pA2
Reference (Journal): Biological activities of des-His1[Glu9]glucagon amide, a glucagon antagonist.
Published in: Peptides

Ligand: des-His1-[Glu9]glucagon-NH2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pA2
Reference (Journal): Synthetic peptide antagonists of glucagon.
Published in: Proc Natl Acad Sci USA

Ligand: crotedumab (Antibody)
Interaction type: Antibody
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Glucagon Receptor Blockade With a Human Antibody Normalizes Blood Glucose in Diabetic Mice and Monkeys.
Published in: Endocrinology

Ligand: crotedumab (Antibody)
Interaction type: Antibody
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.819999694824219 pKd
Reference (Journal): Glucagon Receptor Blockade With a Human Antibody Normalizes Blood Glucose in Diabetic Mice and Monkeys.
Published in: Endocrinology

Ligand: crotedumab (Antibody)
Interaction type: Antibody
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Glucagon Receptor Blockade With a Human Antibody Normalizes Blood Glucose in Diabetic Mice and Monkeys.
Published in: Endocrinology

Ligand: crotedumab (Antibody)
Interaction type: Antibody
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pKd
Reference (Journal): Glucagon Receptor Blockade With a Human Antibody Normalizes Blood Glucose in Diabetic Mice and Monkeys.
Published in: Endocrinology

Ligand: BAY27-9955 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Effects of a novel glucagon receptor antagonist (Bay 27-9955) on glucagon-stimulated glucose production in humans.
Published in: Diabetologia

Ligand: adomeglivant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.180000305175781 pKi
Reference (Journal): Evaluation of Efficacy and Safety of the Glucagon Receptor Antagonist LY2409021 in Patients With Type 2 Diabetes: 12- and 24-Week Phase 2 Studies.
Published in: Diabetes Care

Ligand: adomeglivant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.180000305175781 pKi
Reference (Journal): Short-term administration of the glucagon receptor antagonist LY2409021 lowers blood glucose in healthy people and in those with type 2 diabetes.
Published in: Diabetes Obes Metab