Target
Urokinase-type plasminogen activator
Ligand
BDBM14144
Substrate
BDBM13949
Meas. Tech.
Enzyme Assay and Determination of the Inhibition Constants
pH
7.4±n/a
Temperature
295.15±n/a K
Ki
220±n/a nM
Citation
 Katz, BASprengeler, PALuong, CVerner, EElrod, KKirtley, MJanc, JSpencer, JRBreitenbucher, JGHui, HMcGee, DAllen, DMartelli, AMackman, RL Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets. Chem Biol 8:1107-21 (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:
BDBM14144
Synonyms:
2-{5-[amino(iminiumyl)methyl]-1H-1,3-benzodiazol-2-yl}-6-(cyclopentyloxy)benzen-1-olate | APC-10655 | CA-06
Type:
Small organic molecule
Emp. Form.:
C19H20N4O2
Mol. Mass.:
336.3877
SMILES:
NC(=[NH2+])c1ccc2nc([nH]c2c1)-c1cccc(OC2CCCC2)c1[O-]
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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