Target
Urokinase-type plasminogen activator
Ligand
BDBM16174
Substrate
BDBM13949
Meas. Tech.
Determination of Inhibition Constants
pH
8±n/a
Temperature
298.15±n/a K
Ki
640±n/a nM
Citation
 Zeslawska, ESchweinitz, AKarcher, ASondermann, PSperl, SSturzebecher, JJacob, U Crystals of the urokinase type plasminogen activator variant beta(c)-uPAin complex with small molecule inhibitors open the way towards structure-based drug design. J Mol Biol 301:465-75 (2000) [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:
BDBM16174
Synonyms:
3-[3-(4-beta-alanylpiperazin-1-yl)-3-oxo-2-({[2,4,6-tris(1-methylethyl)phenyl]sulfonyl}amino)propyl]benzenecarboximidamide | 3-{3-[4-(3-aminopropanoyl)piperazin-1-yl]-3-oxo-2-{[2,4,6-tris(propan-2-yl)benzene]sulfonamido}propyl}benzene-1-carboximidamide | UKI-1D
Type:
Small organic molecule
Emp. Form.:
C32H48N6O4S
Mol. Mass.:
612.826
SMILES:
CC(C)c1cc(C(C)C)c(c(c1)C(C)C)S(=O)(=O)NC(Cc1cccc(c1)C(N)=N)C(=O)N1CCN(CC1)C(=O)CCN
Structure:
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Substrate
Name:
BDBM13949
Synonyms:
(2S)-5-carbamimidamido-N-(4-nitrophenyl)-2-{2-[(2S)-2-(phenylformamido)propanamido]acetamido}pentanamide | Bz-Ala-Gly-Arg-pNA | uPA Chromogenic Substrate
Type:
Small organic molecule
Emp. Form.:
C24H30N8O6
Mol. Mass.:
526.545
SMILES:
[#6]-[#6@H](-[#7]-[#6](=O)-c1ccccc1)-[#6](=O)-[#7]-[#6]-[#6](=O)-[#7]-[#6@@H](-[#6]-[#6]-[#6]\[#7]=[#6](\[#7])-[#7])-[#6](=O)-[#7]-c1ccc(cc1)-[#7+](-[#8-])=O |r|
Structure:
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