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

General Information of Drug (ID: DMVE34H)

• Drug Name: (1r)-1,2,2-trimethylpropyl (r)-methylphosphinate Drug Info
• Synonyms: GD7

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 52947808
  TTD Drug ID: DMVE34H

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	[2]
GSK2647544	DM3KARJ	Alzheimer disease	8A20	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	[3]
Goxalapladib	DMSGUY9	Arteriosclerosis	BD40	Discontinued in Phase 1	[6]
Benzaldehyde O-benzoyloxime	DMB7DFT	Discovery agent	N.A.	Investigative	[7]
(E)-(thiophen-2-ylmethylidene)amino benzoate	DMHSJAT	Discovery agent	N.A.	Investigative	[8]
3,4-difluorobenzaldehyde O-benzoyloxime	DMFV3Y9	Discovery agent	N.A.	Investigative	[7]

Drug(s) Targeting Liver carboxylesterase (CES1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cholic Acid	DM7OKQV	Cholelithiasis	DC11	Approved	[9]
PACTIMIBE	DM0NZDT	Arteriosclerosis	BD40	Phase 2/3	[10]
K-604	DMQVN6P	Arteriosclerosis	BD40	Phase 2	[11]
Eldacimibe	DML7WP0	Hyperlipidaemia	5C80	Phase 2	[12]
GR148672X	DM7W6YN	Acute lymphoblastic leukaemia	2A85	Clinical trial	[13]
Avasimibe	DMFG4OM	Peripheral vascular disease	BD4Z	Discontinued in Phase 3	[14]
E-5324	DM562BM	Hyperlipidaemia	5C80	Discontinued in Phase 2	[15]
RP-64477	DMTQ3BS	Hyperlipidaemia	5C80	Discontinued in Phase 2	[16]
CI-976	DMBO28J	Hyperlipidaemia	5C80	Discontinued in Phase 2	[17]
CL-283796	DM7LIDT	Hyperlipidaemia	5C80	Discontinued in Phase 2	[18]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Liver carboxylesterase (CES1)	TTMF541	EST1_HUMAN	Inhibitor	[1]
Platelet-activating factor acetylhydrolase (PLA2G7)	TTDNFMT	PAFA_HUMAN	Inhibitor	[1]

References

• [1] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [2] Phospholipase A2 inhibitors. Curr Opin Lipidol. 2009 Aug;20(4):327-32.
• [3] 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).
• [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] Potent inhibitors of lipoprotein-associated phospholipase A(2): benzaldehyde O-heterocycle-4-carbonyloxime. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5576-9.
• [8] (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.
• [9] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [10] Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and b... J Med Chem. 2008 Aug 14;51(15):4823-33.
• [11] A selective ACAT-1 inhibitor, K-604, suppresses fatty streak lesions in fat-fed hamsters without affecting plasma cholesterol levels. Atherosclerosis. 2007 Apr;191(2):290-7.
• [12] Prospects for drug therapy for hyperlipoproteinaemia. Diabete Metab. 1995 Apr;21(2):139-46.
• [13] 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: 2592).
• [14] New advances in lipid-modifying therapies for reducing cardiovascular risk. Cardiology. 2002;97(2):59-66.
• [15] Effect of the acyl-CoA:cholesterol acyltransferase inhibitor, E5324, on experimental atherosclerosis in rabbits. Atherosclerosis. 1994 Jun;107(2):187-201.
• [16] RP 64477: a potent inhibitor of acyl-coenzyme A:cholesterol O-acyltransferase with low systemic bioavailability. Biochem Pharmacol. 1996 Feb 23;51(4):413-21.
• [17] Acyl-coenzyme A:cholesterol-acyltransferase (ACAT) inhibitors modulate monocyte adhesion to aortic endothelial cells. Atherosclerosis. 1995 Jan 6;112(1):7-17.
• [18] ACAT inhibitors CL 283,546 and CL 283,796 reduce LDL cholesterol without affecting cholesterol absorption in African green monkeys. J Lipid Res. 1995 Jun;36(6):1199-210.