Target
Urokinase-type plasminogen activator
Ligand
BDBM16133
Substrate
BDBM14716
Meas. Tech.
Determination of Inhibitor Potency and Selectivity
pH
8.1±n/a
Temperature
310.15±n/a K
Ki
71±n/a nM
Km
90000±n/a nM
Citation
 Fish, PVBarber, CGBrown, DGButt, RCollis, MGDickinson, RPHenry, BTHorne, VAHuggins, JPKing, EO'gara, MMcCleverty, DMcIntosh, FPhillips, CWebster, R Selective Urokinase-Type Plasminogen Activator Inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines. J Med Chem 50:2341-51 (2007) [PubMed]  Article 
Target
Name:
Urokinase-type plasminogen activator
Synonyms:
PLAU | U-plasminogen activator | UROK_HUMAN | Urokinase | Urokinase-type plasminogen activator (uPA) | Urokinase-type plasminogen activator/surface receptor
Type:
Enzyme
Mol. Mass.:
48528.62
Organism:
Homo sapiens (Human)
Description:
P00749
Residue:
431
Sequence:
MRALLARLLLCVLVVSDSKGSNELHQVPSNCDCLNGGTCVSNKYFSNIHWCNCPKKFGGQHCEIDKSKTCYEGNGHFYRGKASTDTMGRPCLPWNSATVLQQTYHAHRSDALQLGLGKHNYCRNPDNRRRPWCYVQVGLKPLVQECMVHDCADGKKPSSPPEELKFQCGQKTLRPRFKIIGGEFTTIENQPWFAAIYRRHRGGSVTYVCGGSLISPCWVISATHCFIDYPKKEDYIVYLGRSRLNSNTQGEMKFEVENLILHKDYSADTLAHHNDIALLKIRSKEGRCAQPSRTIQTICLPSMYNDPQFGTSCEITGFGKENSTDYLYPEQLKMTVVKLISHRECQQPHYYGSEVTTKMLCAADPQWKTDSCQGDSGGPLVCSLQGRMTLTGIVSWGRGCALKDKPGVYTRVSHFLPWIRSHTKEENGLAL
  
Inhibitor
Name:
BDBM16133
Synonyms:
1-guanidino-7-sulfonamidoisoquinoline 7 | 2-[4-chloro-7-(cyclopentylsulfamoyl)isoquinolin-1-yl]guanidine
Type:
Small organic molecule
Emp. Form.:
C15H18ClN5O2S
Mol. Mass.:
367.854
SMILES:
[#7]\[#6](-[#7])=[#7]/c1ncc(Cl)c2ccc(cc12)S(=O)(=O)[#7]-[#6]-1-[#6]-[#6]-[#6]-[#6]-1
Structure:
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Substrate
Name:
BDBM14716
Synonyms:
(2S)-5-carbamimidamido-N-(4-nitrophenyl)-2-(2-{[(2S)-5-oxopyrrolidin-2-yl]formamido}acetamido)pentanamide hydrochloride | Chromogenic Substrate S-2444 | L-Pyroglutamyl-glycyl-L-argininep-Nitroaniline hydrochloride
Type:
Small organic molecule
Emp. Form.:
C19H26N8O6
Mol. Mass.:
462.4597
SMILES:
[#7]\[#6](-[#7])=[#7]/[#6]-[#6]-[#6]-[#6@H](-[#7]-[#6](=O)-[#6]-[#7]-[#6](=O)-[#6@@H]-1-[#6]-[#6]-[#6](=O)-[#7]-1)-[#6](=O)-[#7]-c1ccc(cc1)-[#7+](-[#8-])=O |r|
Structure:
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