Target
Tissue-type plasminogen activator
Ligand
BDBM298246
Substrate
n/a
Meas. Tech.
Plasma-based Clot Lysis Assay
IC50
10.00±n/a nM
Citation
 Ellermann, MValot, GCancho Grande, YHaßfeld, JKinzel, TKöbberling, JBeyer, KRöhrig, SSperzel, MStampfuß, JMeyer, IKöllnberger, MBurkhardt, NSchlemmer, KStegmann, CSchuhmacher, JWerner, MHeiermann, JHengeveld, WJ Piperidinylpyrazolopyrimidinones and their use US Patent  US10118930 Publication Date 11/6/2018 
Target
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:
BDBM298246
Synonyms:
3-[3-(4-hydroxybenzyl)-1,2,4-oxadiazol-5-yl]-2-methyl-7-(piperidin-4-yl)pyrazolo[1,5-a]pyrimidin-5(4H)-one hydrochloride | US10118930, Example 446
Type:
Small organic molecule
Emp. Form.:
C21H22N6O3
Mol. Mass.:
406.4378
SMILES:
Cc1nn2c(cc(=O)[nH]c2c1-c1nc(Cc2ccc(O)cc2)no1)C1CCNCC1
Structure:
Search PDB for entries with ligand similarity: