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-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
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]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histamine H3 receptor (H3R) TT9JNIC HRH3_HUMAN Antagonist [2]

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.