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

General Information of Drug (ID: DMLNKX7)

• Drug Name: STX-107 Drug Info
• Synonyms: 2-Methyl-4-(pyridin-3-ylethynyl)thiazole; MTEP; mGluR5 Antagonist, MTEP; 329205-68-7; 2-methyl-4-(pyridin-3-ylethynyl)thiazole; CHEMBL292065; 3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine; 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine; 3-[2-(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine; 3-(2-(2-methylthiazol-4-yl)ethynyl)pyridine; 3-[2-(2-Methylthiazol-4-yl)ethynyl]pyridine; 3-(2-Methyl-thiazol-4-ylethynyl)-pyridine; SCHEMBL187254; GTPL3336; CTK1B8867; DTXSID30430775; ZINC1489321; IN1238; BDBM50122758; FCH3417361; API0006876; ACN-027361; KB-274670

Indication

Disease Entry	ICD 11	Status	REF
Autism spectrum disorder	6A02	Phase 2	[1] , [2]

• Cross-matching ID:
  PubChem CID: 16662948
  CAS Number: CAS 935685-90-8
  TTD Drug ID: DMLNKX7

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	[5]
ADX-48621	DM6GTMD	Parkinson disease	8A00.0	Phase 2/3	[6]
RG-7090	DMX8JYN	Fragile X syndrome	LD55	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]
Tetra-hydro-oxazolopyridine derivative 2	DMP65Z4	N. A.	N. A.	Patented	[13]
Tetra-hydro-oxazolopyridine derivative 1	DM72MDA	N. A.	N. A.	Patented	[13]

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	Antagonist	[3] , [4]

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: 3336).
• [2] ClinicalTrials.gov (NCT01325740) A Study to Assess the Tolerability of a Single Dose of STX107 in Adults With Fragile X Syndrome. U.S. National Institutes of Health.
• [3] 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.
• [4] Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic gluta... Bioorg Med Chem. 2010 May 1;18(9):3026-35.
• [5] 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.
• [6] Pipeline of Addex Pharma. Addex Pharma. 2009.
• [7] The challenges of clinical trials in fragile X syndrome. Psychopharmacology (Berl) 2014; 231(6): 1237-1250.
• [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] mGlu5 negative allosteric modulators: a patent review (2013 - 2016).Expert Opin Ther Pat. 2017 Jun;27(6):691-706.