plasminogen activator, urokinase

Target id: 2393

Nomenclature: plasminogen activator, urokinase

Family: S1: Chymotrypsin

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for plasminogen activator, urokinase in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 431 10q24 PLAU plasminogen activator, urokinase
Mouse - 433 14 A3 Plau plasminogen activator
Rat - 432 15p16 Plau plasminogen activator
Previous and Unofficial Names
uPA | UPAM | U-plasminogen activator | URK | plasminogen activator
Database Links
Specialist databases
MEROPS S01.231 (Hs)
Other databases
BRENDA
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.21.73

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
compound 4 [PMID: 18163548] Hs Inhibition 7.7 pIC50 2
pIC50 7.7 (IC50 2x10-8 M) [2]
UK-356202 Hs Inhibition 7.4 pIC50 1
pIC50 7.4 (IC50 3.7x10-8 M) [1]
WX-UK1 Hs Inhibition 6.4 pIC50 3
pIC50 6.4 (IC50 4.1x10-7 M) [3]
upamostat Hs Inhibition - -
Clinically-Relevant Mutations and Pathophysiology
Disease:  Quebec platelet disorder
OMIM: 601709
Orphanet: ORPHA220436

References

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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. 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 10/03/2014. Accessed on 18/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2393.