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Target
Urokinase-type plasminogen activator
Ligand
BDBM50231520
Substrate
n/a
Meas. Tech.
ChEMBL_460612 (CHEMBL927669)
IC50
20±n/a nM
Citation
 Frederickson, M; Callaghan, O; Chessari, G; Congreve, M; Cowan, SR; Matthews, JE; McMenamin, R; Smith, DM; Vinkovic, M; Wallis, NG Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator. J Med Chem 51:183-6 (2008) [PubMed]  Article 
Target
Name:
Urokinase-type plasminogen activator
Synonyms:
Urokinase-type plasminogen activator short chain A | U-plasminogen activator | UROK_HUMAN | Urokinase-type plasminogen activator/surface receptor | Urokinase | Urokinase-type plasminogen activator (uPA) | Urokinase-type plasminogen activator long chain A | 3.4.21.73 | Urokinase-type plasminogen activator chain B | PLAU | uPA
Type:
Enzyme
Mol. Mass.:
48528.62
Organism:
Human
Description:
P00749
Residue:
431
Sequence:
MRALLARLLLCVLVVSDSKGSNELHQVPSNCDCLNGGTCVSNKYFSNIHWCNCPKKFGGQHCEIDKSKTCYEGNGHFYRGKASTDTMGRPCLPWNSATVLQQTYHAHRSDALQLGLGKHNYCRNPDNRRRPWCYVQVGLKLLVQECMVHDCADGKKPSSPPEELKFQCGQKTLRPRFKIIGGEFTTIENQPWFAAIYRRHRGGSVTYVCGGSLISPCWVISATHCFIDYPKKEDYIVYLGRSRLNSNTQGEMKFEVENLILHKDYSADTLAHHNDIALLKIRSKEGRCAQPSRTIQTICLPSMYNDPQFGTSCEITGFGKENSTDYLYPEQLKMTVVKLISHRECQQPHYYGSEVTTKMLCAADPQWKTDSCQGDSGGPLVCSLQGRMTLTGIVSWGRGCALKDKPGVYTRVSHFLPWIRSHTKEENGLAL
  
Inhibitor
Name:
BDBM50231520
Synonyms:
CHEMBL252937 | US8476306, 6.12 | (R)-N-[(S)-1-(4-carbamimidoyl-benzylcarbamoyl)-2-hydroxy-ethyl]-3-hydroxy-2-phenylmethanesulfonylamino-propionamide | N-(BENZYLSULFONYL)SERYL-N~1~-{4-[(Z)-AMINO(IMINO)METHYL]BENZYL}SERINAMIDE
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
NC(=N)c1ccc(CNC(=O)[C@H](CO)NC(=O)[C@@H](CO)NS(=O)(=O)Cc2ccccc2)cc1
Structure:
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