Target
Plasminogen activator inhibitor 1/Urokinase-type plasminogen activator
Ligand
BDBM264597
Substrate
n/a
Meas. Tech.
Fluorometric PAI-1/uPA IC50 Plate Assay
pH
7.4±n/a
Temperature
298.15±n/a K
IC50
1570±n/a nM
Comments
extracted
Citation
 Lawrence, DAEmal, CReinke, ALi, SWarnock, MAbernathy, G Plasminogen activator inhibitor-1 inhibitors and methods of use thereof US Patent  US9718760 Publication Date 8/1/2017 
Target
Name:
Plasminogen activator inhibitor 1/Urokinase-type plasminogen activator
Synonyms:
PAI-1/uPA
Type:
Enzyme
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Plasminogen activator inhibitor 1
Synonyms:
Endothelial plasminogen activator inhibitor | PAI | PAI-1 | PAI1 | PAI1_HUMAN | PLANH1 | Plasminogen activator inhibitor 1 | Plasminogen activator inhibitor 1 (PAI-1) | Plasminogen activator inhibitor-1 | Plasminogen activator-1 (PAI-1) | SERPINE1
Type:
Enzyme
Mol. Mass.:
45064.00
Organism:
Homo sapiens (Human)
Description:
P05121
Residue:
402
Sequence:
MQMSPALTCLVLGLALVFGEGSAVHHPPSYVAHLASDFGVRVFQQVAQASKDRNVVFSPYGVASVLAMLQLTTGGETQQQIQAAMGFKIDDKGMAPALRHLYKELMGPWNKDEISTTDAIFVQRDLKLVQGFMPHFFRLFRSTVKQVDFSEVERARFIINDWVKTHTKGMISNLLGKGAVDQLTRLVLVNALYFNGQWKTPFPDSSTHRRLFHKSDGSTVSVPMMAQTNKFNYTEFTTPDGHYYDILELPYHGDTLSMFIAAPYEKEVPLSALTNILSAQLISHWKGNMTRLPRLLVLPKFSLETEVDLRKPLENLGMTDMFRQFQADFTSLSDQEPLHVAQALQKVKIEVNESGTVASSSTAVIVSARMAPEEIIMDRPFLFVVRHNPTGTVLFMGQVMEP
  
Component 2
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:
BDBM264597
Synonyms:
US9718760, C152
Type:
Small organic molecule
Emp. Form.:
C20H25F2NO7S2
Mol. Mass.:
493.542
SMILES:
CCCCCCCCN(S(=O)(=O)c1ccc(O)c(O)c1)S(=O)(=O)c1cc(F)c(O)c(F)c1
Structure:
Search PDB for entries with ligand similarity: