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Target
Urokinase-type plasminogen activator
Ligand
BDBM14714
Substrate
BDBM14716
Meas. Tech.
Serine Protease Inhibition Assay
pH
7.8±n/a
Temperature
295.15±n/a K
Ki
>3400±n/a nM
Citation
 Olivero, AG; Eigenbrot, C; Goldsmith, R; Robarge, K; Artis, DR; Flygare, J; Rawson, T; Sutherlin, DP; Kadkhodayan, S; Beresini, M; Elliott, LO; DeGuzman, GG; Banner, DW; Ultsch, M; Marzec, U; Hanson, SR; Refino, C; Bunting, S; Kirchhofer, D A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo. J Biol Chem 280:9160-9 (2005) [PubMed]  Article 
Target
Name:
Urokinase-type plasminogen activator
Synonyms:
3.4.21.73 | PLAU | U-plasminogen activator | UROK_HUMAN | Urokinase | Urokinase-type plasminogen activator (uPA) | Urokinase-type plasminogen activator chain B | Urokinase-type plasminogen activator long chain A | Urokinase-type plasminogen activator short chain A | Urokinase-type plasminogen activator/surface receptor | uPA
Type:
Enzyme
Mol. Mass.:
48528.62
Organism:
Homo sapiens (Human)
Description:
P00749
Residue:
431
Sequence:
MRALLARLLLCVLVVSDSKGSNELHQVPSNCDCLNGGTCVSNKYFSNIHWCNCPKKFGGQHCEIDKSKTCYEGNGHFYRGKASTDTMGRPCLPWNSATVLQQTYHAHRSDALQLGLGKHNYCRNPDNRRRPWCYVQVGLKLLVQECMVHDCADGKKPSSPPEELKFQCGQKTLRPRFKIIGGEFTTIENQPWFAAIYRRHRGGSVTYVCGGSLISPCWVISATHCFIDYPKKEDYIVYLGRSRLNSNTQGEMKFEVENLILHKDYSADTLAHHNDIALLKIRSKEGRCAQPSRTIQTICLPSMYNDPQFGTSCEITGFGKENSTDYLYPEQLKMTVVKLISHRECQQPHYYGSEVTTKMLCAADPQWKTDSCQGDSGGPLVCSLQGRMTLTGIVSWGRGCALKDKPGVYTRVSHFLPWIRSHTKEENGLAL
  
Inhibitor
Name:
BDBM14714
Synonyms:
(2R)-N-[(3-aminobenzene)sulfonyl]-2-[(4-carbamimidoyl-3-hydroxyphenyl)amino]-2-(3,5-diethoxy-2-fluorophenyl)acetamide | G17905 | R-4-[2-(3-aminobenzenesulfonylamino)-1-(3,5-diethoxy-2-fluorophenyl)-2-oxoethylamino]-2-hydroxy-benzamidine.TFA
Type:
Small organic molecule
Emp. Form.:
C25H28FN5O6S
Mol. Mass.:
545.583
SMILES:
CCOc1cc(OCC)c(F)c(c1)[C@@H](Nc1ccc(C(N)=N)c(O)c1)C(=O)NS(=O)(=O)c1cccc(N)c1 |r|
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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