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Target
Tissue-type plasminogen activator
Ligand
BDBM298180
Substrate
n/a
Meas. Tech.
Plasma-based Clot Lysis Assay
IC50
15.0±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:
BDBM298180
Synonyms:
3-[5-(2-Methylprop-1-en-1-yl)-1,2,4-oxadiazol-3-yl]-7-(piperidin-4-yl)pyrazolo[1,5-a]pyrimidin-5 (4H)-one hydrochloride | US10118930, Example 383
Type:
Small organic molecule
Emp. Form.:
C17H20N6O2
Mol. Mass.:
340.3797
SMILES:
CC(C)=Cc1nc(no1)-c1cnn2c(cc(=O)[nH]c12)C1CCNCC1 |(5.75,5.52,;4.26,5.12,;3.17,6.21,;3.86,3.64,;2.37,3.24,;1.9,1.77,;.36,1.77,;-.12,3.24,;1.13,4.14,;-.73,.68,;-2.26,.84,;-2.89,-.56,;-1.75,-1.59,;-1.75,-3.13,;-.41,-3.9,;.92,-3.13,;2.26,-3.9,;.92,-1.59,;-.41,-.82,;-3.08,-3.9,;-4.41,-3.13,;-5.75,-3.9,;-5.75,-5.44,;-4.41,-6.21,;-3.08,-5.44,)|
Structure:
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