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Target
Serine protease hepsin
Ligand
BDBM191634
Substrate
n/a
Meas. Tech.
High-Throughput Screening Assay
IC50
2310±530 nM
Citation
 Vasioukhin, VI; Chevillet, 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:
BDBM191634
Synonyms:
US9182402, 7
Type:
Small organic molecule
Emp. Form.:
C29H16F2N2O4
Mol. Mass.:
494.4451
SMILES:
Fc1cccc(c1)-c1nc2ccc(Cc3ccc4nc(oc(=O)c4c3)-c3cccc(F)c3)cc2c(=O)o1
Structure:
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