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

General Information of Drug (ID: DMN8TH1)

Drug Name

GR-144053 Drug Info

Synonyms

GR-144053; CHEMBL36326; GR-144053F; GR144053; 2-[4-[4-(4-carbamimidoylphenyl)piperazin-1-yl]piperidin-1-yl]acetic acid; {4-[4-(4-Carbamimidoyl-phenyl)-piperazin-1-yl]-piperidin-1-yl}-acetic acid; GR 144053; AC1L5AAD; GTPL6587; ZINC5719; SCHEMBL6839445; CHEBI:92207; BDBM50037970; BRD-K12120659-305-01-4; {4-[4-(4-Carbamimidoyl-phenyl)-piperazin-1-yl]-piperidin-1-yl}-acetic acid (GR 144053)

Indication

Disease Entry	ICD 11	Status	REF
Thrombosis	DB61-GB90	Terminated	[1]

Cross-matching ID

PubChem CID: 173614
ChEBI ID: CHEBI:92207
TTD Drug ID: DMN8TH1

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

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Drug(s) Targeting Glycoprotein IIb/IIIa receptor (GPIIb/IIIa)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydroquinone	DM6AVR4	Melasma	ED60.1	Approved	[3]
Eptifibatide	DMQXTJS	Acute cardiac ischemic events	BA40.Z	Approved	[4]
Tirofiban	DMQG17S	Acute coronary syndrome	BA41	Approved	[5]
Abciximab	DMJO6GV	Acute disease		Approved	[5]
DMP-444	DMO7BQS	Coronary artery disease	BA80	Phase 3	[6]
99mTc-rBitistatin	DMFAMNH	Pulmonary embolism	JB42	Phase 1/2	[7]
AjvW2	DM6PN4H	Thrombosis	DB61-GB90	Phase 1	[8]
SDZ-GPI-562	DMU9ZGN	Thrombosis	DB61-GB90	Phase 1	[9]
RGD-891	DMVJMF1	Thrombosis	DB61-GB90	Phase 1	[10]
Lefradafiban	DMKZVLH	Angina pectoris	BA40	Phase 1	[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
Glycoprotein IIb/IIIa receptor (GPIIb/IIIa)	TT38RM1	ITA2B_HUMAN; ITB3_HUMAN	Modulator	[2]

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References

1	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. (Ligand id: 6587).
2	GR144053, a fibrinogen receptor antagonist, enhances the suppression of neointima formation by losartan, an angiotensin II receptor antagonist, in ... Br J Pharmacol. 1997 Nov;122(6):1099-104.
3	Accutin, a new disintegrin, inhibits angiogenesis in vitro and in vivo by acting as integrin alphavbeta3 antagonist and inducing apoptosis. Blood. 1998 Nov 1;92(9):3268-76.
4	Barbourin. A GPIIb-IIIa-specific integrin antagonist from the venom of Sistrurus m. barbouri. J Biol Chem. 1991 May 25;266(15):9359-62.
5	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
6	Evaluation of Tc-99m-labeled glycoprotein IIb/IIIa receptor antagonist DMP444 SPECT in patients with infective endocarditis. Clin Nucl Med. 2003 Jun;28(6):480-4.
7	Platelet binding and biodistribution of [99mTc]rBitistatin in animal species and humans. Nucl Med Biol. 2007 Oct;34(7):855-63.
8	Novel approaches to the treatment of thrombosis. Trends Pharmacol Sci. 2002 Jan;23(1):25-32.
9	Heparin-induced thrombocytopenia: the role of platelet activation and therapeutic implications. Semin Thromb Hemost. 1999;25 Suppl 1:67-75.
10	Pharmacokinetics, pharmacodynamics, and safety of a platelet GPIIb/IIIa antagonist, RGD891, following intravenous administration in healthy male volunteers. J Clin Pharmacol. 2000 Nov;40(11):1245-56.
11	Pharmacodynamics and safety of lefradafiban, an oral platelet glycoprotein IIb/IIIa receptor antagonist, in patients with stable coronary artery disease undergoing elective angioplasty. Heart. 2001 Apr;85(4):444-50.