plasminogen activator, urokinase | S1: Chymotrypsin | IUPHAR/BPS Guide to PHARMACOLOGY

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plasminogen activator, urokinase

Target not currently curated in GtoImmuPdb

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

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, urokinase
Rat - 432 15p16 Plau plasminogen activator, urokinase
Previous and Unofficial Names
uPA | UPAM | U-plasminogen activator | URK | plasminogen activator
Database Links
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
EC Number:

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

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter 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 - -
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0043312 neutrophil degranulation TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0043312 neutrophil degranulation TAS
Immuno Process:  Tissue repair
GO Annotations:  Associated to 1 GO processes
GO:0043403 skeletal muscle tissue regeneration ISO
Clinically-Relevant Mutations and Pathophysiology
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. 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 11/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY,