Target
Tissue-type plasminogen activator
Ligand
BDBM50301980
Substrate
n/a
Meas. Tech.
ChEMBL_599100 (CHEMBL1047155)
IC50
22000±n/a nM
Citation
 West, CWAdler, MArnaiz, DChen, DChu, KGualtieri, GHo, EHuwe, CLight, DPhillips, GPulk, RSukovich, DWhitlow, MYuan, SBryant, 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:
BDBM50301980
Synonyms:
2-(6-(3'-(aminomethyl)biphenyl-3-yloxy)-3,5-difluoropyridin-2-yloxy)-4-methylbenzoic acid | CHEMBL572250
Type:
Small organic molecule
Emp. Form.:
C26H20F2N2O4
Mol. Mass.:
462.4448
SMILES:
Cc1ccc(C(O)=O)c(Oc2nc(Oc3cccc(c3)-c3cccc(CN)c3)c(F)cc2F)c1
Structure:
Search PDB for entries with ligand similarity: