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Target
Tissue-type plasminogen activator
Ligand
BDBM50301989
Substrate
n/a
Meas. Tech.
ChEMBL_599100 (CHEMBL1047155)
IC50
3900±n/a nM
Citation
 West, CW; Adler, M; Arnaiz, D; Chen, D; Chu, K; Gualtieri, G; Ho, E; Huwe, C; Light, D; Phillips, G; Pulk, R; Sukovich, D; Whitlow, M; Yuan, S; Bryant, J Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA). Bioorg Med Chem Lett 19:5712-5 (2009) [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:
BDBM50301989
Synonyms:
2-(6-(3'-carbamimidoylbiphenyl-3-yloxy)-3,5-difluoro-4-methylpyridin-2-yloxy)-4-(dimethylamino)benzoic acid | CHEMBL571392
Type:
Small organic molecule
Emp. Form.:
C28H24F2N4O4
Mol. Mass.:
518.5114
SMILES:
CN(C)c1ccc(C(O)=O)c(Oc2nc(Oc3cccc(c3)-c3cccc(c3)C(N)=N)c(F)c(C)c2F)c1
Structure:
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