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Target
Tissue-type plasminogen activator
Ligand
BDBM16173
Substrate
n/a
Meas. Tech.
ChEMBL_1908157 (CHEMBL4410515)
IC50
>20000±n/a nM
Citation
 Buckley, BJ; Majed, H; Aboelela, A; Minaei, E; Jiang, L; Fildes, K; Cheung, CY; Johnson, D; Bachovchin, D; Cook, GM; Huang, M; Ranson, M; Kelso, MJ 6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease. Bioorg Med Chem Lett 29:0 (2019) [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:
BDBM16173
Synonyms:
3,5-diamino-6-chloro-N-(diaminomethylene)pyrazinamide;hydrochloride | 3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide | Amiloride | Amipramidin | CHEMBL945
Type:
Small organic molecule
Emp. Form.:
C6H8ClN7O
Mol. Mass.:
229.627
SMILES:
NC(=N)NC(=O)c1nc(Cl)c(N)nc1N
Structure:
Search PDB for entries with ligand similarity: