Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMKAGLV)

• Drug Name: GR-131663 Drug Info
• Synonyms: AH-002; AH-017; GR-131665

Indication

Disease Entry	ICD 11	Status	REF
Anxiety disorder	6B00-6B0Z	Terminated	[1]

• Cross-matching ID: TTD Drug ID: DMKAGLV

Molecule-Related Drug Atlas

Drug(s) Targeting Melatonin receptor type 1A (MTNR1A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Melatonin	DMKWFBT	Insomnia	7A00-7A0Z	Approved	[3]
Ramelteon	DM7IW9J	Insomnia	7A00-7A0Z	Approved	[4]
Tasimelteon	DMLOQ1V	Insomnia	7A00-7A0Z	Approved	[5]
Neu-P11	DMIQDFW	Alzheimer disease	8A20	Phase 2	[6]
LY-156735	DM5IX9M	Anxiety disorder	6B00-6B0Z	Phase 2	[7]
Agomelatine	DMXYA5K	Major depressive disorder	6A70.3	Withdrawn from market	[8]
Luzindole	DMXRJQV	Sleep-wake disorder	7A00-7B2Z	Terminated	[9]
S-20928	DMQDWMJ	Sleep-wake disorder	7A00-7B2Z	Terminated	[10]
GR-133347	DMNRJA0	Anxiety disorder	6B00-6B0Z	Terminated	[11]
SL-18.1616	DMI1WNF	Insomnia	7A00-7A0Z	Terminated	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Melatonin receptor type 1A (MTNR1A)	TT0WAIE	MTR1A_HUMAN	Modulator	[2]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003455)
• [2] Novel non-indolic melatonin receptor agonists differentially entrain endogenous melatonin rhythm and increase its amplitude. Eur J Pharmacol. 1999 Oct 15;382(3):157-66.
• [3] The human MT1 melatonin receptor stimulates cAMP production in the human neuroblastoma cell line SH-SY5Y cells via a calcium-calmodulin signal transduction pathway. J Neuroendocrinol. 2005 Mar;17(3):170-8.
• [4] MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential. J Med Chem. 2014 Apr 24;57(8):3161-85.
• [5] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7393).
• [6] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 288).
• [7] Melatonin and sleep in aging population. Exp Gerontol. 2005 Dec;40(12):911-25.
• [8] Melatonin receptor agonists: SAR and applications to the treatment of sleep-wake disorders. Curr Top Med Chem. 2008;8(11):954-68.
• [9] Luzindole (N-0774): a novel melatonin receptor antagonist. J Pharmacol Exp Ther. 1988 Sep;246(3):902-10.
• [10] Effects of two melatonin analogues, S-20098 and S-20928, on melatonin receptors in the pars tuberalis of the rat. J Pineal Res. 1998 Oct;25(3):172-6.
• [11] US patent application no. 5,151,446, Substituted 2-amidotetralins as melatonin agonists and antagonists.
• [12] US patent application no. 2005,016,4987, Melatonin combination therapy for improving sleep quality.