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Target
Serine protease hepsin
Ligand
BDBM81467
Substrate
n/a
Meas. Tech.
High-Throughput Screening Assay
IC50
2020±370 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:
BDBM81467
Synonyms:
CAS_569-65-3 | CHEMBL1085765 | Meclizine | NSC_4034 | US9182402, 13
Type:
Small organic molecule
Emp. Form.:
C25H27ClN2
Mol. Mass.:
390.948
SMILES:
Cc1cccc(CN2CCN(CC2)C(c2ccccc2)c2ccc(Cl)cc2)c1
Structure:
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