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

General Information of Drug (ID: DM6VQZ7)

• Drug Name: SP203 Drug Info
• Synonyms: SP 203; SP-203

Indication

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

• Cross-matching ID:
  PubChem CID: 16737207
  CAS Number: CAS 945933-41-5
  TTD Drug ID: DM6VQZ7

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	[4]
ADX-48621	DM6GTMD	Parkinson disease	8A00.0	Phase 2/3	[5]
RG-7090	DMX8JYN	Fragile X syndrome	LD55	Phase 2	[6]
STX-107	DMLNKX7	Autism spectrum disorder	6A02	Phase 2	[7]
ADX10059	DMGVKHQ	Anxiety disorder	6B00-6B0Z	Phase 2	[8]
McN3377	DMTCADJ	Fragile X syndrome	LD55	Phase 1/2	[9]
MK-3328	DMW2O5D	Alzheimer disease	8A20	Phase 1	[10]
[3H]fenobam	DMBOXA1	Allodynia	MB40.1	Phase 1	[11]
RG7342	DMIW5NG	Schizophrenia	6A20	Phase 1	[12]
BMS-984923	DMFNDUL	Alzheimer disease	8A20	Phase 1	[13]

Drug(s) Affected By Metabotropic glutamate receptor 5 (GRM5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[14]
Benzo(a)pyrene	DMN7J43	N. A.	N. A.	Phase 1	[15]
bisphenol A	DM2ZLD7	Discovery agent	N.A.	Investigative	[16]

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]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Metabotropic glutamate receptor 5 (GRM5)	OTRYQ7PP	GRM5_HUMAN	Protein Interaction/Cellular Processes	[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: 6434).
• [2] Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging mo... J Med Chem. 2007 Jul 12;50(14):3256-66.
• [3] Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging. J Med Chem. 2011 Feb 10;54(3):901-8. doi: 10.1021/jm101430m. Epub 2011 Jan 5.
• [4] 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.
• [5] Pipeline of Addex Pharma. Addex Pharma. 2009.
• [6] The challenges of clinical trials in fragile X syndrome. Psychopharmacology (Berl) 2014; 231(6): 1237-1250.
• [7] 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.
• [8] 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.
• [9] Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
• [10] 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).
• [11] 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.
• [12] Clinical pipeline report, company report or official report of Roche.
• [13] Silent Allosteric Modulation of mGluR5 Maintains Glutamate Signaling while Rescuing Alzheimer's Mouse Phenotypes. Cell Rep. 2017 Jul 5;20(1):76-88.
• [14] Predictive toxicology using systemic biology and liver microfluidic "on chip" approaches: application to acetaminophen injury. Toxicol Appl Pharmacol. 2012 Mar 15;259(3):270-80.
• [15] Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.
• [16] DNA methylome-wide alterations associated with estrogen receptor-dependent effects of bisphenols in breast cancer. Clin Epigenetics. 2019 Oct 10;11(1):138. doi: 10.1186/s13148-019-0725-y.