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

Ligand: gastric inhibitory polypeptide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKd
Reference (Journal): GLP-1/GIP chimeric peptides define the structural requirements for specific ligand-receptor interaction of GLP-1.
Published in: Regul Pept

Ligand: GIP-(10-30) (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.2 pIC50
Reference (Journal): GIP(6-30amide) contains the high affinity binding region of GIP and is a potent inhibitor of GIP1-42 action in vitro.
Published in: Regul Pept

Ligand: GIP-(6-30)-amide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): GIP(6-30amide) contains the high affinity binding region of GIP and is a potent inhibitor of GIP1-42 action in vitro.
Published in: Regul Pept

Ligand: GIP-(7-30) (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.8 pIC50
Reference (Journal): GIP(6-30amide) contains the high affinity binding region of GIP and is a potent inhibitor of GIP1-42 action in vitro.
Published in: Regul Pept

Ligand: human GIP(1-30)NH2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.050000190734863 pKi
Reference (Journal): N-terminally and C-terminally truncated forms of glucose-dependent insulinotropic polypeptide are high-affinity competitive antagonists of the human GIP receptor.
Published in: Br J Pharmacol

Ligand: human GIP(3-30)NH2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.640000343322754 pKi
Reference (Journal): N-terminally and C-terminally truncated forms of glucose-dependent insulinotropic polypeptide are high-affinity competitive antagonists of the human GIP receptor.
Published in: Br J Pharmacol

Ligand: human GIP(3-42)NH2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): GIP-(3-42) does not antagonize insulinotropic effects of GIP at physiological concentrations.
Published in: Am J Physiol Endocrinol Metab

Ligand: human GIP(3-42)NH2 (Peptide)
Interaction type: Antagonist
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.659999847412109 pIC50
Reference (Journal): GIP-(3-42) does not antagonize insulinotropic effects of GIP at physiological concentrations.
Published in: Am J Physiol Endocrinol Metab

Ligand: human GIP(5-30)NH2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.229999542236328 pKi
Reference (Journal): N-terminally and C-terminally truncated forms of glucose-dependent insulinotropic polypeptide are high-affinity competitive antagonists of the human GIP receptor.
Published in: Br J Pharmacol

Ligand: maridebart cafraglutide (Antibody)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.369999885559082 pIC50
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: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.079999923706055 pIC50
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: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.579999923706055 pIC50
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: mGIPAnt-1 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Glucose-dependent insulinotropic polypeptide receptor antagonist treatment causes a reduction in weight gain in ovariectomised high fat diet-fed mice.
Published in: Br J Pharmacol

Ligand: mGIPAnt-1 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.570000171661377 pIC50
Reference (Journal): Glucose-dependent insulinotropic polypeptide receptor antagonist treatment causes a reduction in weight gain in ovariectomised high fat diet-fed mice.
Published in: Br J Pharmacol

Ligand: MK-0893 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.989999771118164 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: [Pro3]GIP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Effects of the novel (Pro3)GIP antagonist and exendin(9-39)amide on GIP- and GLP-1-induced cyclic AMP generation, insulin secretion and postprandial insulin release in obese diabetic (ob/ob) mice: evidence that GIP is the major physiological incretin.
Published in: Diabetologia

Ligand: [125I]GIP (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKd
Reference (Journal): GLP-1/GIP chimeric peptides define the structural requirements for specific ligand-receptor interaction of GLP-1.
Published in: Regul Pept

Ligand: tirzepatide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: EMA & FDA (2022)
Primary target: no
Median affinity: 9.869999885559082 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