Target Validation Information
TTD ID	T62306
Target Name	Motilin receptor (MLNR)
Type of Target	Clinical trial
Drug Potency against Target	MOTILIN	Drug Info	Ki = 0.36 nM	[1]
Action against Disease Model	Camicinal	Drug Info	GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of h uMan and rabbit gastrointestinal motility. In rabbit gastric antr uM, GSK962040 300 nmol L(-1)-10 micromol L(-1) caused a prolonged facilitation of the amplitude of cholinergically mediated contractions, to a maxim uM of 248 +/- 47% at 3 micromol L(-1). In h uMan-isolated stomach, GSK962040 10 micromol L(-1), erythromycin 10 micromol L(-1) and [Nle13]-motilin 100 nmol L(-1), each caused muscle contraction of similar amplitude. In conscious rabbits, intravenous doses of 5 mg kg(-1) GSK962040 or 10 mg kg(-1) erythromycin significantly increased faecal output over a 2-h period.	[2]
References
REF 1	Discovery of a new class of macrocyclic antagonists to the human motilin receptor. J Med Chem. 2006 Nov 30;49(24):7190-7.
REF 2	GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of human and rabbit gastrointestinal motility. Neurogastroenterol Motil. 2009 Jun;21(6):657-64, e30-1.

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