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plasminogen activator, urokinase

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Target not currently curated in GtoImmuPdb

Target id: 2393

Nomenclature: plasminogen activator, urokinase

Family: S1: Chymotrypsin

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 431 10q22.2 PLAU plasminogen activator, urokinase
Mouse - 433 14 11.53 cM Plau plasminogen activator, urokinase
Rat - 432 15p16 Plau plasminogen activator, urokinase
Previous and Unofficial Names Click here for help
uPA | UPAM | U-plasminogen activator | URK | plasminogen activator
Database Links Click here for help
Specialist databases
MEROPS S01.231 (Hs)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction Click here for help
EC Number:

Download all structure-activity data for this target as a CSV file go icon to follow link

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
WX-UK1 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.2 pKi 3
pKi 6.2 (Ki 6.5x10-7 M) [3]
compound 4 [PMID: 18163548] Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.7 pIC50 2
pIC50 7.7 (IC50 2x10-8 M) [2]
UK-356202 Small molecule or natural product Hs Inhibition 7.4 pIC50 1
pIC50 7.4 (IC50 3.7x10-8 M) [1]
WX-UK1 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pIC50 4
pIC50 6.4 (IC50 4.1x10-7 M) [4]
upamostat Small molecule or natural product Hs Inhibition - -
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Cellular signalling
Immuno Process:  Tissue repair
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Quebec platelet disorder
OMIM: 601709
Orphanet: ORPHA220436


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1. Barber CG, Dickinson RP, Fish PV. (2004) Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. Bioorg Med Chem Lett, 14 (12): 3227-30. [PMID:15149680]

2. Frederickson M, Callaghan O, Chessari G, Congreve M, Cowan SR, Matthews JE, McMenamin R, Smith DM, Vinković M, Wallis NG. (2008) Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator. J Med Chem, 51 (2): 183-6. [PMID:18163548]

3. Setyono-Han B, Stürzebecher J, Schmalix WA, Muehlenweg B, Sieuwerts AM, Timmermans M, Magdolen V, Schmitt M, Klijn JG, Foekens JA. (2005) Suppression of rat breast cancer metastasis and reduction of primary tumour growth by the small synthetic urokinase inhibitor WX-UK1. Thromb Haemost, 93 (4): 779-86. [PMID:15841327]

4. Stürzebecher J, Vieweg H, Steinmetzer T, Schweinitz A, Stubbs MT, Renatus M, Wikström P. (1999) 3-Amidinophenylalanine-based inhibitors of urokinase. Bioorg Med Chem Lett, 9 (21): 3147-52. [PMID:10560742]

How to cite this page

S1: Chymotrypsin: plasminogen activator, urokinase. Last modified on 17/05/2022. Accessed on 04/03/2024. IUPHAR/BPS Guide to PHARMACOLOGY,