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Target
Tissue-type plasminogen activator
Ligand
BDBM16142
Substrate
BDBM14715
Meas. Tech.
Determination of Inhibitor Potency and Selectivity
Ki
>100000±n/a nM
Citation
 Fish, PV; Barber, CG; Brown, DG; Butt, R; Collis, MG; Dickinson, RP; Henry, BT; Horne, VA; Huggins, JP; King, E; O'gara, M; McCleverty, D; McIntosh, F; Phillips, C; Webster, R Selective Urokinase-Type Plasminogen Activator Inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines. J Med Chem 50:2341-51 (2007) [PubMed]  Article 
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:
BDBM16142
Synonyms:
2-({4-chloro-1-[(diaminomethylidene)amino]isoquinoline-7-}(methyl)sulfonamido)acetic acid | substituted glycine deriv. 16
Type:
Small organic molecule
Emp. Form.:
C13H14ClN5O4S
Mol. Mass.:
371.799
SMILES:
[#6]-[#7](-[#6]-[#6](-[#8])=O)S(=O)(=O)c1ccc2c(Cl)cnc(\[#7]=[#6](/[#7])-[#7])c2c1
Structure:
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Substrate
Name:
BDBM14715
Synonyms:
(2S)-2-{[(2S)-1-[(2R,3R)-2-amino-3-methylpentanoyl]pyrrolidin-2-yl]formamido}-5-carbamimidamido-N-(4-nitrophenyl)pentanamide dihydrochloride | Chromogenic Substrate S-2288 | H-D-Isoleucyl-L-prolyl-L-arginine-pnitroaniline dihydrochloride
Type:
Small organic molecule
Emp. Form.:
C23H36N8O5
Mol. Mass.:
504.5825
SMILES:
CC[C@@H](C)[C@@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(N)=N)C(=O)Nc1ccc(cc1)[N+]([O-])=O |r|
Structure:
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