Target
Serine protease hepsin
Ligand
BDBM191630
Substrate
n/a
Meas. Tech.
High-Throughput Screening Assay
IC50
1930±390 nM
Citation
 Vasioukhin, VIChevillet, JR Hepsin inhibitors US Patent  US9182402 Publication Date 11/10/2015 
Target
Name:
Serine protease hepsin
Synonyms:
HEPS_HUMAN | HPN | Hepsin | Serine protease hepsin | TMPRSS1 | Transmembrane protease serine 11E | Transmembrane protease, serine 1
Type:
Enzyme
Mol. Mass.:
45016.98
Organism:
Homo sapiens (Human)
Description:
Human deglycosylated hepsin was expressed in Pichia pastoris.
Residue:
417
Sequence:
MAQKEGGRTVPCCSRPKVAALTAGTLLLLTAIGAASWAIVAVLLRSDQEPLYPVQVSSADARLMVFDKTEGTWRLLCSSRSNARVAGLSCEEMGFLRALTHSELDVRTAGANGTSGFFCVDEGRLPHTQRLLEVISVCDCPRGRFLAAICQDCGRRKLPVDRIVGGRDTSLGRWPWQVSLRYDGAHLCGGSLLSGDWVLTAAHCFPERNRVLSRWRVFAGAVAQASPHGLQLGVQAVVYHGGYLPFRDPNSEENSNDIALVHLSSPLPLTEYIQPVCLPAAGQALVDGKICTVTGWGNTQYYGQQAGVLQEARVPIISNDVCNGADFYGNQIKPKMFCAGYPEGGIDACQGDSGGPFVCEDSISRTPRWRLCGIVSWGTGCALAQKPGVYTKVSDFREWIFQAIKTHSEASGMVTQL
  
Inhibitor
Name:
BDBM191630
Synonyms:
US9182402, 3
Type:
Small organic molecule
Emp. Form.:
C19H12BrN3O3
Mol. Mass.:
410.221
SMILES:
Brc1cccc(c1)N1C(=O)NC(=O)\C(=C/c2c[nH]c3ccccc23)C1=O
Structure:
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