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

General Information of Drug (ID: DMFXKN1)

• Drug Name: 2-nas-phe(3-am)-4-(2-guanidinoethyl)piperidine Drug Info
• Synonyms: (S)-3-(3-(4-(2-GUANIDINOETHYL)PIPERIDIN-1-YL)-2-(NAPHTHALENE-2-SULFONAMIDO)-3-OXOPROPYL)BENZIMIDAMIDE; 2gv6; AC1OA9XW; CHEMBL210771; SCHEMBL12960819; BDBM23902; 3-amidinophenylalanine deriv., 8; 3-[(2S)-3-[4-(2-carbamimidamidoethyl)piperidin-1-yl]-2-(naphthalene-2-sulfonamido)-3-oxopropyl]benzene-1-carboximidamide; 3-{(2S)-3-[4-(2-carbamimidamidoethyl)piperidin-1-yl]-2-[(naphthalen-2-ylsulfonyl)amino]-3-oxopropyl}benzenecarboximidamide

Indication

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

• Cross-matching ID:
  PubChem CID: 6852210
  TTD Drug ID: DMFXKN1

Molecule-Related Drug Atlas

Drug(s) Targeting Urokinase-type plasminogen activator (PLAU)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pro-urokinase	DMGKT2L	Thrombin deficiency	3B14.Z	Approved	[2]
Urokinase	DM0GOUD	Myocardial infarction	BA41-BA43	Approved	[3]
PAI-1	DMY2AEF	N. A.	N. A.	Phase 4	[4]
Amediplase	DM4FPM3	Myocardial infarction	BA41-BA43	Phase 3	[5]
Upamostat	DMFZULI	Breast cancer	2C60-2C65	Phase 2	[6]
Saruplase	DM1M0PR	Thrombosis	DB61-GB90	Phase 2	[7]
HTU-PA	DMNHE43	Cerebrovascular ischaemia	8B1Z	Phase 1/2	[8]
PMID18163548C4	DMHPME3	Myocardial ischemia	BA6Z	Clinical trial	[9]
UK-356202	DMSRK2A	Myocardial hypertrophy	BC45	Clinical trial	[10]
PAI-2	DMRSMW8	N. A.	N. A.	Discontinued in Phase 2	[11]

Drug(s) Targeting Suppressor of tumorigenicity 14 protein (ST14)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
US8569313, Inhibitor 18	DMXTCGM	N. A.	N. A.	Patented	[12]
US8569313, Inhibitor 14	DMZV6YT	N. A.	N. A.	Patented	[12]
US8569313, Inhibitor 19	DMLXG43	N. A.	N. A.	Patented	[12]
US8569313, Inhibitor 15	DMTMG02	N. A.	N. A.	Patented	[12]
PMID23849879C3	DMUW3MT	Discovery agent	N.A.	Investigative	[13]
PMID25489658C4d	DMWZJT0	Discovery agent	N.A.	Investigative	[14]
Benzamidine	DM37GWL	Discovery agent	N.A.	Investigative	[15]
Inhibitor 1 [Colombo et al., 2012]	DMUQHMP	Discovery agent	N.A.	Investigative	[16]
3-tapap	DMKSUV9	Discovery agent	N.A.	Investigative	[1]

Drug(s) Targeting Coagulation factor IIa (F2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Argatroban	DMFI46A	Thrombosis	DB61-GB90	Approved	[17]
Pyridoxal Phosphate	DMO2K0J	Malnutrition	5B50-5B71	Approved	[18]
Bivalirudin	DMECRX1	Thrombocytopenia	3B64	Approved	[19]
Ximelegatran	DMU8ANS	Myocardial infarction	BA41-BA43	Approved	[5]
Dabigatran	DMDI6R4	Stroke	8B20	Approved	[20]
Desirudin Recombinant	DM2BTFN	Coagulation defect	3B10.0	Approved	[3]
Human prothrombin complex concentrate	DMPHVQ1	Bleeding disorder	GA20-GA21	Approved	[21]
Lepirudin	DM1I3D5	Thrombocytopenia	3B64	Approved	[22]
Anisindione	DM2C48U	Coagulation defect	3B10.0	Approved	[23]
ATryn antithrombin	DM79Y2T	Multiple sclerosis	8A40	Approved	[24]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Coagulation factor IIa (F2)	TT6L509	THRB_HUMAN	Inhibitor	[1]
Suppressor of tumorigenicity 14 protein (ST14)	TTPRO7W	ST14_HUMAN	Inhibitor	[1]
Urokinase-type plasminogen activator (PLAU)	TTGY7WI	UROK_HUMAN	Inhibitor	[1]

References

• [1] Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase. J Med Chem. 2006 Jul 13;49(14):4116-26.
• [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: 2393).
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [4] Urokinase-type plasminogen activator and its inhibitor PAI-1: predictors of poor response to tamoxifen therapy in recurrent breast cancer. J Natl Cancer Inst. 1995 May 17;87(10):751-6.
• [5] Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
• [6] Phase II randomised proof-of-concept study of the urokinase inhibitor upamostat (WX-671) in combination with gemcitabine compared with gemcitabine alone in patients with non-resectable, locally advanced pancreatic cancer. Br J Cancer. 2013 Mar 5;108(4):766-70.
• [7] Pharmacokinetics and pharmacodynamics of saruplase, an unglycosylated single-chain urokinase-type plasminogen activator, in patients with acute myocardial infarction. Thromb Haemost. 1994 Nov;72(5):740-4.
• [8] Characterization of the dexamethasone-induced inhibitor of plasminogen activator in HTC hepatoma cells. J Biol Chem. 1986 Mar 25;261(9):4352-7.
• [9] Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator. J Med Chem. 2008 Jan 24;51(2):183-6.
• [10] Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.
• [11] Topological localization of plasminogen activator inhibitor type 2. Cytometry. 2000 May 1;40(1):32-41.
• [12] Meta-substituted phenyl sulfonyl amides of secondary amino acid amides, the production thereof, and use thereof as matriptase inhibitors. US8569313.
• [13] 1,2,4-Triazole derivatives as transient inactivators of kallikreins involved in skin diseases. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4547-51.
• [14] Toward the first class of suicide inhibitors of kallikreins involved in skin diseases. J Med Chem. 2015 Jan 22;58(2):598-612.
• [15] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [16] 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: 2418).
• [17] Studies on the different modes of action of the anticoagulant protease inhibitors DX-9065a and Argatroban. I. Effects on thrombin generation. J Biol Chem. 2002 Dec 27;277(52):50439-44.
• [18] New antithrombotic drugs (excluding plasminogen activators. Arch Mal Coeur Vaiss. 2001 Nov;94(11 Suppl):1225-32.
• [19] New anticoagulants. Am Heart J. 2001 Aug;142(2 Suppl):S3-8.
• [20] Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
• [21] 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: 2362).
• [22] Recombinant hirudin (lepirudin) as anticoagulant in intensive care patients treated with continuous hemodialysis. Kidney Int Suppl. 1999 Nov;(72):S46-50.
• [23] Anticoagulation with anisindione in a patient with a warfarin-induced skin eruption. Pharmacotherapy. 2003 Apr;23(4):533-6.
• [24] Antithrombin III Utilization in a Large Teaching Hospital. P T. 2013 December; 38(12): 764-767, 779.