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

General Information of Drug (ID: DMWVTS3)

• Drug Name: LSN2463359 Drug Info
• Synonyms: LSN 2463359

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 72551298
  CAS Number: CAS 1401031-52-4
  TTD Drug ID: DMWVTS3

Molecule-Related Drug Atlas

Drug(s) Targeting Metabotropic glutamate receptor 5 (mGluR5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AFQ056	DMMHSLC	Fragile X syndrome	LD55	Phase 2/3	[3]
ADX-48621	DM6GTMD	Parkinson disease	8A00.0	Phase 2/3	[4]
RG-7090	DMX8JYN	Fragile X syndrome	LD55	Phase 2	[5]
STX-107	DMLNKX7	Autism spectrum disorder	6A02	Phase 2	[6]
ADX10059	DMGVKHQ	Anxiety disorder	6B00-6B0Z	Phase 2	[7]
McN3377	DMTCADJ	Fragile X syndrome	LD55	Phase 1/2	[8]
MK-3328	DMW2O5D	Alzheimer disease	8A20	Phase 1	[9]
[3H]fenobam	DMBOXA1	Allodynia	MB40.1	Phase 1	[10]
RG7342	DMIW5NG	Schizophrenia	6A20	Phase 1	[11]
BMS-984923	DMFNDUL	Alzheimer disease	8A20	Phase 1	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Metabotropic glutamate receptor 5 (mGluR5)	TTHS256	GRM5_HUMAN	Modulator (allosteric modulator)	[2]

References

• [1] 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: 6394).
• [2] In vitro characterisation of the novel positive allosteric modulators of the mGlu receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat. Neuropharmacology. 2013 Jan;64:224-39.
• [3] Metabolism and disposition of the metabotropic glutamate receptor 5 antagonist (mGluR5) mavoglurant (AFQ056) in healthy subjects. Drug Metab Dispos. 2013 Sep;41(9):1626-41.
• [4] Pipeline of Addex Pharma. Addex Pharma. 2009.
• [5] The challenges of clinical trials in fragile X syndrome. Psychopharmacology (Berl) 2014; 231(6): 1237-1250.
• [6] Social Communication is an Emerging Target for Pharmacotherapy in Autism Spectrum Disorder - A Review of the Literature on Potential Agents. J Can Acad Child Adolesc Psychiatry. 2014 February; 23(1):20-30.
• [7] A proof-of-concept study evaluating the effect of ADX10059, a metabotropic glutamate receptor-5 negative allosteric modulator, on acid exposure and... Gut. 2009 Sep;58(9):1192-9.
• [8] Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
• [9] 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: 293).
• [10] Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agon... J Pharmacol Exp Ther. 2005 Nov;315(2):711-21.
• [11] Clinical pipeline report, company report or official report of Roche.
• [12] Silent Allosteric Modulation of mGluR5 Maintains Glutamate Signaling while Rescuing Alzheimer's Mouse Phenotypes. Cell Rep. 2017 Jul 5;20(1):76-88.