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

General Information of Drug (ID: DM3KARJ)

• Drug Name: GSK2647544 Drug Info
• Synonyms: GSK-2647544

Indication

Disease Entry	ICD 11	Status	REF
Alzheimer disease	8A20	Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 57336782
  TTD Drug ID: DM3KARJ

Molecule-Related Drug Atlas

Drug(s) Targeting Platelet-activating factor acetylhydrolase (PLA2G7)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Rilapladib	DMB9861	Arteriosclerosis	BD40	Phase 1	[3]
Indolizine derivative 1	DM4GZBI	N. A.	N. A.	Patented	[4]
Bicyclic pyrimidine derivative 2	DMJP16K	N. A.	N. A.	Patented	[4]
RPAF-AH	DMOVJ60	Sepsis	1G40-1G41	Discontinued in Phase 3	[5]
GSK568859	DM6E84O	Arteriosclerosis	BD40	Discontinued in Phase 1	[2]
Goxalapladib	DMSGUY9	Arteriosclerosis	BD40	Discontinued in Phase 1	[6]
(1r)-1,2,2-trimethylpropyl (r)-methylphosphinate	DMVE34H	Discovery agent	N.A.	Investigative	[7]
Benzaldehyde O-benzoyloxime	DMB7DFT	Discovery agent	N.A.	Investigative	[8]
(E)-(thiophen-2-ylmethylidene)amino benzoate	DMHSJAT	Discovery agent	N.A.	Investigative	[9]
3,4-difluorobenzaldehyde O-benzoyloxime	DMFV3Y9	Discovery agent	N.A.	Investigative	[8]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Platelet-activating factor acetylhydrolase (PLA2G7)	TTDNFMT	PAFA_HUMAN	Modulator	[2]

References

• [1] ClinicalTrials.gov (NCT01924858) A Positron Emission Tomography (PET) Study to Investigate the Brain Biodistribution of 18F GSK2647544 in Healthy Subjects to Determine Its Ability to Cross the Blood-brain-barrier.. U.S. National Institutes of Health.
• [2] 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: 1432).
• [3] Phospholipase A2 inhibitors. Curr Opin Lipidol. 2009 Aug;20(4):327-32.
• [4] Inhibitors of phospholipase A2 and their therapeutic potential: an update on patents (2012-2016).Expert Opin Ther Pat. 2017 Feb;27(2):217-225.
• [5] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006777)
• [6] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020582)
• [7] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [8] Potent inhibitors of lipoprotein-associated phospholipase A(2): benzaldehyde O-heterocycle-4-carbonyloxime. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5576-9.
• [9] (E)-Phenyl- and -heteroaryl-substituted O-benzoyl-(or acyl)oximes as lipoprotein-associated phospholipase A2 inhibitors. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1525-7.