Reaction Details Report a problem with these data
Target
Tissue-type plasminogen activator
Ligand
BDBM297798
Substrate
n/a
Meas. Tech.
Plasma-based Clot Lysis Assay
IC50
14.0±n/a nM
Citation
 Ellermann, M; Valot, G; Cancho Grande, Y; Haßfeld, J; Kinzel, T; Köbberling, J; Beyer, K; Röhrig, S; Sperzel, M; Stampfuß, J; Meyer, I; Köllnberger, M; Burkhardt, N; Schlemmer, K; Stegmann, C; Schuhmacher, J; Werner, M; Heiermann, J; Hengeveld, 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:
BDBM297798
Synonyms:
3-(Morpholin-4-ylcarbonyl)-7-(piperidin-4-yl)pyrazolo[1,5-a]pyrimidin-5(4H)-one hydrochloride | US10118930, Example 23
Type:
Small organic molecule
Emp. Form.:
C16H21N5O3
Mol. Mass.:
331.3696
SMILES:
O=C(N1CCOCC1)c1cnn2c(cc(=O)[nH]c12)C1CCNCC1
Structure:
Search PDB for entries with ligand similarity: