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Target
Tissue-type plasminogen activator
Ligand
BDBM14714
Substrate
BDBM14715
Meas. Tech.
Serine Protease Inhibition Assay
pH
7.8±n/a
Temperature
295.15±n/a K
Ki
>3900±n/a nM
Citation
 Olivero, AG; Eigenbrot, C; Goldsmith, R; Robarge, K; Artis, DR; Flygare, J; Rawson, T; Sutherlin, DP; Kadkhodayan, S; Beresini, M; Elliott, LO; DeGuzman, GG; Banner, DW; Ultsch, M; Marzec, U; Hanson, SR; Refino, C; Bunting, S; Kirchhofer, D A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo. J Biol Chem 280:9160-9 (2005) [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:
BDBM14714
Synonyms:
(2R)-N-[(3-aminobenzene)sulfonyl]-2-[(4-carbamimidoyl-3-hydroxyphenyl)amino]-2-(3,5-diethoxy-2-fluorophenyl)acetamide | G17905 | R-4-[2-(3-aminobenzenesulfonylamino)-1-(3,5-diethoxy-2-fluorophenyl)-2-oxoethylamino]-2-hydroxy-benzamidine.TFA
Type:
Small organic molecule
Emp. Form.:
C25H28FN5O6S
Mol. Mass.:
545.583
SMILES:
CCOc1cc(OCC)c(F)c(c1)[C@@H](Nc1ccc(C(N)=N)c(O)c1)C(=O)NS(=O)(=O)c1cccc(N)c1 |r|
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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