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

General Information of Drug (ID: DMBJMZC)

Drug Name

GSK239512 Drug Info

Synonyms

720691-69-0; GSK-239512; 1-(6-((3-CYCLOBUTYL-2,3,4,5-TETRAHYDRO-1H-BENZO[D]AZEPIN-7-YL)OXY)PYRIDIN-3-YL)PYRROLIDIN-2-ONE; GSK239512; UNII-4I7U5C459M; CHEMBL3092650; 4I7U5C459M; YFRBKEVUUCQYOW-UHFFFAOYSA-N; SCHEMBL167578; MolPort-035-776-189; ZINC3961802; BDBM50444496; AKOS025291102; SB16754; KS-0000063Q; AS-42474; AK171368; 2-Pyrrolidinone, 1-(6-((3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy)-3-pyridinyl)-; J3.497.402K

Indication

Disease Entry	ICD 11	Status	REF
Alzheimer disease	8A20	Phase 2	[1]
Dementia	6D80-6D86	Phase 2	[1]

Cross-matching ID

PubChem CID: 9976892
CAS Number: CAS 720691-69-0
TTD Drug ID: DMBJMZC
VARIDT Drug ID: DR00805

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

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Drug(s) Targeting Histamine H3 receptor (H3R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pitolisant	DM8RFNJ	Excessive daytime sleepiness	MG42	Approved	[3]
SUVN-G3031	DM3BO8G	Cognitive impairment	6D71	Phase 3	[4]
JNJ-17216498	DM1GRCU	Narcolepsy	7A20	Phase 2	[5]
JNJ-39220675	DM0WY3H	Alcohol dependence	6C40.2	Phase 2	[6]
AZD-5213	DMOZ04X	Alzheimer disease	8A20	Phase 2	[7]
Bavisant	DM6CVZ5	Attention deficit hyperactivity disorder	6A05.Z	Phase 2	[8]
ABT-288	DM7X54F	Alzheimer disease	8A20	Phase 2	[9]
SAR-110894	DMCLEXM	Alzheimer disease	8A20	Phase 2	[7]
ABT-652	DMLEO2Z	Diabetic neuropathy	8C0Z	Phase 2	[10]
S-38093	DMD8XOY	Alzheimer disease	8A20	Phase 2	[11]
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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
Histamine H3 receptor (H3R)	TT9JNIC	HRH3_HUMAN	Antagonist	[2]

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References

1	ClinicalTrials.gov (NCT01772199) Study to Assess Whether GSK239512 Can Remyelinate Lesions in Subjects With Relapsing Remitting Multiple Sclerosis. U.S. National Institutes of Health.
2	Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
3	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
4	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5	Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61.
6	JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats. Psychopharmacology (Berl). 2011 Apr;214(4):829-41.
7	SAR110894, a potent histamine H receptor antagonist, displays procognitive effects in rodents. Pharmacol Biochem Behav. 2012 Aug;102(2):203-14.
8	Randomized clinical study of a histamine H3 receptor antagonist for the treatment of adults with attention-deficit hyperactivity disorder. CNS Drugs. 2012 May 1;26(5):421-34.
9	A randomized study of H3 antagonist ABT-288 in mild-to-moderate Alzheimer's dementia.J Alzheimers Dis.2014;42(3):959-71.
10	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032225)
11	Histamine H3 Receptors and Sleep-Wake Regulation. JPET January 2011 vol. 336 no. 1 17-23.