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Target
Plasminogen activator inhibitor 1/Tissue-type plasminogen activator
Ligand
BDBM264627
Substrate
n/a
Meas. Tech.
Fluorometric PAI-1/tPA IC50 Plate Assay at pH 7.8
Temperature
298.15±n/a K
IC50
58160±n/a nM
Comments
extracted
Citation
 Lawrence, DA; Emal, C; Reinke, A; Li, S; Warnock, M; Abernathy, 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/Tissue-type plasminogen activator
Synonyms:
PAI-1/tPA
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:
Tissue-type plasminogen activator
Synonyms:
Alteplase | PLAT | Reteplase | TPA_HUMAN | Thrombin receptor protein | Tissue-type plasminogen activator | Tissue-type plasminogen activator (tPA) | Tissue-type plasminogen activator precursor | t-PA | t-Plasminogen Activator (tPA) | t-plasminogen activator
Type:
Enzyme
Mol. Mass.:
62931.08
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
562
Sequence:
MDAMKRGLCCVLLLCGAVFVSPSQEIHARFRRGARSYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGGTCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGTWSTAESGAECTNWNSSALAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDCYFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAKPWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAKHRRSPGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVHKEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEALSPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGGPLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP
  
Inhibitor
Name:
BDBM264627
Synonyms:
US9718760, C160
Type:
Small organic molecule
Emp. Form.:
C13H13NO4S
Mol. Mass.:
279.312
SMILES:
Oc1ccc(cc1O)S(=O)(=O)NCc1ccccc1
Structure:
Search PDB for entries with ligand similarity: