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Target
Urokinase-type plasminogen activator
Ligand
BDBM14479
Substrate
BDBM13949
Meas. Tech.
Enzyme Assay and Determination of the Inhibition Constants
Ki
100±n/a nM
Citation
 Katz, BA; Luong, C; Ho, JD; Somoza, JR; Gjerstad, E; Tang, J; Williams, SR; Verner, E; Mackman, RL; Young, WB; Sprengeler, PA; Chan, H; Mortara, K; Janc, JW; McGrath, ME Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA). J Mol Biol 344:527-47 (2004) [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:
BDBM14479
Synonyms:
CA-21 | [amino({5-[(3-hydroxynaphthalene-2-)amido]pyridin-2-yl}amino)methylidene]azanium
Type:
Small organic molecule
Emp. Form.:
C17H16N5O2
Mol. Mass.:
322.3407
SMILES:
[#7]\[#6](-[#7])=[#7+]/c1ccc(-[#7]-[#6](=O)-c2cc3ccccc3cc2-[#8])cn1
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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