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

General Information of Drug (ID: DMJLSX0)

• Drug Name: Ro4491533 Drug Info
• Synonyms: Ro 4491533; Ro-4491533

Indication

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

• Cross-matching ID:
  PubChem CID: 11158623
  CAS Number: CAS 579482-31-8
  TTD Drug ID: DMJLSX0

Molecule-Related Drug Atlas

Drug(s) Targeting Metabotropic glutamate receptor 3 (mGluR3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LY404039	DMWZIRJ	Schizophrenia	6A20	Phase 3	[4]
RO-4995819	DMNTC7O	Major depressive disorder	6A70.3	Phase 2	[5]
Oleoyl-estrone	DM0RA8F	Alzheimer disease	8A20	Phase 2	[6]
MP-101	DMYCITZ	Alzheimer disease	8A20	Phase 2	[7]
BCI-838	DMRXDN3	Major depressive disorder	6A70.3	Phase 1	[8]
Pomaglumetad	DMTOLI5	Schizophrenia	6A20	Phase 1	[9]
BCI-632	DMZYCWT	Alzheimer disease	8A20	Phase 1	[10]
PMID25435285-Compound-16	DMKFX2G	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-15	DMHBWNS	N. A.	N. A.	Patented	[11]
PMID25435285-Compound-20	DMG9FYH	N. A.	N. A.	Patented	[11]

Drug(s) Targeting Metabotropic glutamate receptor 2 (mGluR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
RO-4995819	DMNTC7O	Major depressive disorder	6A70.3	Phase 2	[5]
Oleoyl-estrone	DM0RA8F	Alzheimer disease	8A20	Phase 2	[6]
MP-101	DMYCITZ	Alzheimer disease	8A20	Phase 2	[7]
JNJ-64281802	DMNMSVX	Dengue	1D20-1D2Z	Phase 2	[12]
BCI-838	DMRXDN3	Major depressive disorder	6A70.3	Phase 1	[8]
Pomaglumetad	DMTOLI5	Schizophrenia	6A20	Phase 1	[9]
BCI-632	DMZYCWT	Alzheimer disease	8A20	Phase 1	[10]
LY-2979165	DM16IX2	Bipolar disorder	6A60	Phase 1	[13]
JNJ-42491293	DMOL9JR	Psychiatric disorder	6E8Z	Phase 1	[14]
ADX71149	DMBUOX4	Epilepsy	8A60-8A68	Phase 1	[15]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Metabotropic glutamate receptor 2 (mGluR2)	TTXJ47W	GRM2_HUMAN	Modulator (allosteric modulator)	[2]
Metabotropic glutamate receptor 3 (mGluR3)	TT8A9EF	GRM3_HUMAN	Modulator (allosteric modulator)	[3]

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: 6226).
• [2] Characterization of an mGluR2/3 negative allosteric modulator in rodent models of depression. J Neurogenet. 2011 Dec;25(4):152-66.
• [3] Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6969-74.
• [4] Positive allosteric modulators of the metabotropic glutamate receptor 2 for the treatment of schizophrenia. Expert Opin Ther Pat. 2009 Sep;19(9):1259-75.
• [5] Novel glutamatergic drugs for the treatment of mood disorders. Neuropsychiatr Dis Treat. 2013; 9: 1101-1112.
• [6] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [7] ClinicalTrials.gov (NCT03044249) A Study of MP-101 in Dementia-Related Psychosis and/or Agitation and Aggression. U.S. National Institutes of Health.
• [8] Metabotropic glutamate receptor subtype 2 (GRM2; MGLUR2); GRM3 (MGLUR3). SciBX 3(13); doi:10.1038/scibx.2010.413. April 1 2010
• [9] LY-2140023, a prodrug of the group II metabotropic glutamate receptor agonist LY-404039 for the potential treatment of schizophrenia. Curr Opin Investig Drugs. 2010 Jul;11(7):833-45.
• [10] Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists. J Med Chem. 2004 Aug 26;47(18):4570-87.
• [11] Novel metabotropic glutamate receptor 2/3 antagonists and their therapeutic applications: a patent review (2005 - present).Expert Opin Ther Pat. 2015 Jan;25(1):69-90.
• [12] Pharmacokinetic and pharmacodynamic characterisation of JNJ-40411813, a positive allosteric modulator of mGluR2, in two randomised, double-blind phase-I studies. J Psychopharmacol. 2015 Apr;29(4):414-25.
• [13] Annual Reports in Medicinal Chemistry. Volume 47, 2012, Page(78).
• [14] Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders. Nat Rev Drug Discov. 2014 Sep;13(9):692-708.
• [15] MGlu2 receptor-mediated modulation of conditioned avoidance behavior in rats. European journal of pharmacology. 01/2014; 727(1).