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Target
Urokinase-type plasminogen activator
Ligand
BDBM13945
Substrate
BDBM13949
Meas. Tech.
Enzyme Assay and Determination of the Inhibition Constants
Ki
3800±n/a nM
Citation
 Katz, BA; Elrod, K; Luong, C; Rice, MJ; Mackman, RL; Sprengeler, PA; Spencer, J; Hataye, J; Janc, J; Link, J; Litvak, J; Rai, R; Rice, K; Sideris, S; Verner, E; Young, W A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site. J Mol Biol 307:1451-86 (2001) [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:
BDBM13945
Synonyms:
APC-13140 | [amino(2-{hydroxy[(3-phenoxyphenyl)methyl]carbamoyl}-1H-1,3-benzodiazol-5-yl)methylidene]azanium
Type:
Small organic molecule
Emp. Form.:
C22H20N5O3
Mol. Mass.:
402.4254
SMILES:
NC(=[NH2+])c1ccc2nc([nH]c2c1)C(=O)N(O)Cc1cccc(Oc2ccccc2)c1
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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