MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC50=4.9 nM). MA-2029 is selective for the motilin receptor over various other receptors and ion channels. MA-2029 may be useful for gastrointestinal disorders associated with disturbed gastrointestinal motility.

ANQ-11125 is a potent and selective antagonist of motilin, with the pKd of 8.24. ANQ-11125 blocks motilide-induced contractions in vitro in the rabbit.

ANQ-11125 TFA is a potent and selective antagonist of motilin, with the pKd of 8.24. ANQ-11125 TFA blocks motilide-induced contractions in vitro in the rabbit.