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TargetSerine protease hepsin
LigandBDBM50069109
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1466699 (CHEMBL3404297)
Ki 2600±n/a nM
Citation Franco, FMJones, DEHarris, PKHan, ZWildman, SAJarvis, CMJanetka, JW Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets. Bioorg Med Chem23:2328-43 (2015) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Serine protease hepsin
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:
MAQKEGGRTVPCCSRPKVAALTAGTLLLLTAIGAASWAIVAVLLRSDQEPLYPVQVSSAD
ARLMVFDKTEGTWRLLCSSRSNARVAGLSCEEMGFLRALTHSELDVRTAGANGTSGFFCV
DEGRLPHTQRLLEVISVCDCPRGRFLAAICQDCGRRKLPVDRIVGGRDTSLGRWPWQVSL
RYDGAHLCGGSLLSGDWVLTAAHCFPERNRVLSRWRVFAGAVAQASPHGLQLGVQAVVYH
GGYLPFRDPNSEENSNDIALVHLSSPLPLTEYIQPVCLPAAGQALVDGKICTVTGWGNTQ
YYGQQAGVLQEARVPIISNDVCNGADFYGNQIKPKMFCAGYPEGGIDACQGDSGGPFVCE
DSISRTPRWRLCGIVSWGTGCALAQKPGVYTKVSDFREWIFQAIKTHSEASGMVTQL
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50069109
n/a
NameBDBM50069109
Synonyms:CHEMBL3402438
TypeSmall organic molecule
Emp. Form.C33H35N5O5S
Mol. Mass.613.727
SMILESNC(=N)c1cccc(C[C@H](NS(=O)(=O)c2ccc3ccccc3c2)C(=O)N2CCC[C@H](C2)NC(=O)OCc2ccccc2)c1 |r|
Structure
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