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

General Information of Drug (ID: DM8Q2ZR)

• Drug Name: WX-UK1 Drug Info
• Synonyms: UKI-1; UNII-00LOF6890B; CHEMBL107955; WX-UK1; 00LOF6890B; 220355-63-5; Wx-uk1 free base; compound 2r-L; GTPL6498; BDBM23891; 3-amidinophenylalanine deriv., 35; ZINC4426028; AKOS030526723; CS-5726; HY-100415; 1-Piperazinecarboxylic acid, 4-((2S)-3-(3-(aminoiminomethyl)phenyl)-1-oxo-2-(((2,4,6-tris(1-methylethyl)phenyl)sulfonyl)amino)propyl)-, ethyl ester; ethyl 4-[(2S)-3-(3-carbamimidoylphenyl)-2-[[2,4,6-tri(propan-2-yl)phenyl]sulfonylamino]propanoyl]piperazine-1-carboxylate; ethyl 4-[(2S)-3-(3-carbamimidoylphenyl)-2-{[2,4,6

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1/2	[1]

• Cross-matching ID:
  PubChem CID: 9895194
  TTD Drug ID: DM8Q2ZR

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	[3]
Urokinase	DM0GOUD	Myocardial infarction	BA41-BA43	Approved	[4]
PAI-1	DMY2AEF	N. A.	N. A.	Phase 4	[5]
Amediplase	DM4FPM3	Myocardial infarction	BA41-BA43	Phase 3	[6]
Upamostat	DMFZULI	Breast cancer	2C60-2C65	Phase 2	[7]
Saruplase	DM1M0PR	Thrombosis	DB61-GB90	Phase 2	[8]
HTU-PA	DMNHE43	Cerebrovascular ischaemia	8B1Z	Phase 1/2	[9]
PMID18163548C4	DMHPME3	Myocardial ischemia	BA6Z	Clinical trial	[10]
UK-356202	DMSRK2A	Myocardial hypertrophy	BC45	Clinical trial	[11]
PAI-2	DMRSMW8	N. A.	N. A.	Discontinued in Phase 2	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Urokinase-type plasminogen activator (PLAU)	TTGY7WI	UROK_HUMAN	Inhibitor	[2]

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: 6498).
• [2] Inhibition of the invasion capacity of carcinoma cells by WX-UK1, a novel synthetic inhibitor of the urokinase-type plasminogen activator system. Int J Cancer. 2004 Jul 20;110(6):815-24.
• [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: 2393).
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [5] 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.
• [6] Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
• [7] 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.
• [8] 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.
• [9] Characterization of the dexamethasone-induced inhibitor of plasminogen activator in HTC hepatoma cells. J Biol Chem. 1986 Mar 25;261(9):4352-7.
• [10] 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.
• [11] Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.
• [12] Topological localization of plasminogen activator inhibitor type 2. Cytometry. 2000 May 1;40(1):32-41.