Target family: Motilin receptor (type: gpcr)
Target: motilin receptor

Ligand: GM-109 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Design and synthesis of motilin antagonists derived from the [1-4] fragment of porcine motilin.
Published in: J Med Chem

Ligand: GM-109 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pA2
Reference (Journal): GM-109: a novel, selective motilin receptor antagonist in the smooth muscle of the rabbit small intestine.
Published in: J Pharmacol Exp Ther

Ligand: KOS1326 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.2 pIC50
Reference (Journal): Desensitization of the human motilin receptor by motilides.
Published in: J Pharmacol Exp Ther

Ligand: [Leu13]motilin (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pIC50
Reference (Journal): Receptor for motilin identified in the human gastrointestinal system.
Published in: Science

Ligand: MA-2029 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pA2
Reference (Journal): Oral administration of MA-2029, a novel selective and competitive motilin receptor antagonist, inhibits motilin-induced intestinal contractions and visceral pain in rabbits.
Published in: Eur J Pharmacol

Ligand: ME36 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.7 pIC50
Reference (Journal): Desensitization of the human motilin receptor by motilides.
Published in: J Pharmacol Exp Ther

Ligand: ME4 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.3 pIC50
Reference (Journal): Desensitization of the human motilin receptor by motilides.
Published in: J Pharmacol Exp Ther

Ligand: ME67 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.5 pIC50
Reference (Journal): Desensitization of the human motilin receptor by motilides.
Published in: J Pharmacol Exp Ther

Ligand: mitemcinal (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Erythromycin derivatives ABT 229 and GM 611 act on motilin receptors in the rabbit duodenum.
Published in: Clin Exp Pharmacol Physiol

Ligand: mitemcinal (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): In vitro pharmacological characterization of mitemcinal (GM-611), the first acid-resistant non-peptide motilin receptor agonist, in smooth muscle of rabbit small intestine.
Published in: Pharmacology

Ligand: mitemcinal (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Potent, acid-stable and orally active macrolide-type motilin receptor agonists, GM-611 and the derivatives.
Published in: Bioorg Med Chem Lett

Ligand: motilin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Differential contributions of motilin receptor extracellular domains for peptide and non-peptidyl agonist binding and activity.
Published in: J Biol Chem

Ligand: motilin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Differential determinants for peptide and non-peptidyl ligand binding to the motilin receptor. Critical role of second extracellular loop for peptide binding and action.
Published in: J Biol Chem

Ligand: motilin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Demonstration of a specific site of covalent labeling of the human motilin receptor using a biologically active photolabile motilin analog.
Published in: J Pharmacol Exp Ther

Ligand: motilin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Identification of peptide ligand-binding domains within the human motilin receptor using photoaffinity labeling.
Published in: J Biol Chem

Ligand: motilin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pIC50
Reference (Journal): Receptor for motilin identified in the human gastrointestinal system.
Published in: Science

Ligand: motilin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.7 pIC50
Reference (Journal): Receptor for motilin identified in the human gastrointestinal system.
Published in: Science

Ligand: motilin-(1-11) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.8 pIC50
Reference (Journal): Receptor for motilin identified in the human gastrointestinal system.
Published in: Science

Ligand: [Phe3,Leu13]motilin (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.9 pIC50
Reference (Journal): Receptor for motilin identified in the human gastrointestinal system.
Published in: Science

Ligand: roxithromycin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Median affinity: 6.2 pIC50
Reference (Journal): Receptor for motilin identified in the human gastrointestinal system.
Published in: Science

Ligand: [D-Bpa5,Ile13]motilin (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): Demonstration of a specific site of covalent labeling of the human motilin receptor using a biologically active photolabile motilin analog.
Published in: J Pharmacol Exp Ther

Ligand: [L-Bpa5,Ile13]motilin (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Demonstration of a specific site of covalent labeling of the human motilin receptor using a biologically active photolabile motilin analog.
Published in: J Pharmacol Exp Ther

Ligand: [125I]motilin (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pKd
Reference (Journal): Receptor for motilin identified in the human gastrointestinal system.
Published in: Science

Ligand: motilin-(1-12) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pIC50
Reference (Journal): Receptor for motilin identified in the human gastrointestinal system.
Published in: Science

Ligand: motilin-(1-13) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pIC50
Reference (Journal): Receptor for motilin identified in the human gastrointestinal system.
Published in: Science

Ligand: motilin-(1-19) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pIC50
Reference (Journal): Receptor for motilin identified in the human gastrointestinal system.
Published in: Science

Ligand: motilin-(2-22) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.5 pIC50
Reference (Journal): Receptor for motilin identified in the human gastrointestinal system.
Published in: Science

Ligand: [nLeu13,Glu14]motilin (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pIC50
Reference (Journal): Receptor for motilin identified in the human gastrointestinal system.
Published in: Science

Ligand: OHM-11526 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Motilin and OHM-11526 activate a calcium current in human and canine jejunal circular smooth muscle.
Published in: Am J Physiol

Ligand: alemcinal (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pIC50
Reference (Journal): Desensitization of the human motilin receptor by motilides.
Published in: J Pharmacol Exp Ther

Ligand: azithromycin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA & UK (1991)
Primary target: no
Median affinity: 5.5 pEC50
Reference (Journal): The antibiotic azithromycin is a motilin receptor agonist in human stomach: comparison with erythromycin.
Published in: Br J Pharmacol

Ligand: [Bpa1,Ile13]motilin (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Identification of peptide ligand-binding domains within the human motilin receptor using photoaffinity labeling.
Published in: J Biol Chem

Ligand: camicinal (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.900000095367432 pEC50
Reference (Journal): GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of human and rabbit gastrointestinal motility.
Published in: Neurogastroenterol Motil

Ligand: camicinal (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.900000095367432 pEC50
Reference (Journal): The investigational drug camicinal for the treatment of gastroparesis.
Published in: Expert Opin Investig Drugs

Ligand: DS-3801b free base (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.279999732971191 pEC50
Reference (Journal): Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure.
Published in: Bioorg Med Chem Lett

Ligand: EM-523 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.6 pIC50
Reference (Journal): Desensitization of the human motilin receptor by motilides.
Published in: J Pharmacol Exp Ther

Ligand: erythromycin (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1964)
Median affinity:  pIC50
Reference (Journal): Desensitization of the human motilin receptor by motilides.
Published in: J Pharmacol Exp Ther

Ligand: erythromycin (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1964)
Median affinity:  pIC50
Reference (Journal): Receptor for motilin identified in the human gastrointestinal system.
Published in: Science

Ligand: GM-109 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pA2
Reference (Journal): Erythromycin derivatives ABT 229 and GM 611 act on motilin receptors in the rabbit duodenum.
Published in: Clin Exp Pharmacol Physiol