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

General Information of Drug (ID: DMSCXB7)

Drug Name

UK-240455 Drug Info

Synonyms

UK-212189 (racemate); (aR)-N-(6,7-Dichloro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-N-(2-hydroxyethyl)methanesulfonamide

Indication

Disease Entry	ICD 11	Status	REF
Nerve injury	ND56.4	Phase 1	[1]

Cross-matching ID

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Discontinued Drug(s)

Investigative Drug(s)

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Drug(s) Targeting Glycine receptor (GlyR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
THIOCOLCHICOSIDE	DMEPWYA	Muscle spasm	MB47.3	Approved	[2]
ZD-9379	DM3KYO4	Cerebrovascular ischaemia	8B1Z	Phase 1	[3]
MDL-27531	DMC60S8	Epilepsy	8A60-8A68	Phase 1	[4]
Gavestinel	DM8IL1U	Nerve injury	ND56.4	Discontinued in Phase 2	[5]
GV-196771	DMFN21T	Migraine	8A80	Discontinued in Phase 2	[6]
GW 468816	DMQ92WF	Tobacco dependence	6C4A.2	Discontinued in Phase 2	[7]
M-241247	DMIY51U	Cerebrovascular ischaemia	8B1Z	Terminated	[8]
GINKOLIDE B	DMLIM7B	Sepsis	1G40-1G41	Terminated	[9]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine	DME8VPC	Discovery agent	N.A.	Investigative	[2]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine	DMXFVD1	Discovery agent	N.A.	Investigative	[2]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Glycine receptor (GlyR)	TTZ8EM9	GLRA1_HUMAN; GLRA2_HUMAN; GLRA3_HUMAN; GLRA4_HUMAN; GLRB_HUMAN	Modulator	[1]

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References

1	UK-315716/UK-240455. Pfizer. Curr Opin Investig Drugs. 2001 Dec;2(12):1737-9.
2	3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. J Med Chem. 2006 Sep 7;49(18):5571-7.
3	Neuroprotective potential of ionotropic glutamate receptor antagonists. Neurotox Res. 2002 Mar;4(2):119-26.
4	MDL 27,531 reduces spontaneous hindlimb contractions in rats with chronic transections of the spinal cord. Neurosci Lett. 1992 Nov 23;147(1):101-5.
5	Glycine antagonist (gavestinel) in neuroprotection (GAIN International) in patients with acute stroke: a randomised controlled trial.GAIN International Investigators.Lancet.2000 Jun 3;355(9219):1949-54.
6	First time in human for GV196771: interspecies scaling applied on dose selection. J Clin Pharmacol. 1999 Jun;39(6):560-6.
7	A double-blind, placebo-controlled trial of the NMDA glycine site antagonist, GW468816, for prevention of relapse to smoking in females.J Clin Psychopharmacol.2011 Oct;31(5):597-602.
8	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003415)
9	Probing the pharmacophore of ginkgolides as glycine receptor antagonists. J Med Chem. 2007 Apr 5;50(7):1610-7.