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TargetSerine protease hepsin
LigandBDBM50130871
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1525565 (CHEMBL3637191)
Ki 400±n/a nM
Citation Goswami, RWohlfahrt, GTörmäkangas, OMoilanen, ALakshminarasimhan, ANagaraj, JArumugam, KNMukherjee, SChacko, ARKrishnamurthy, NRJaleel, MPalakurthy, RKSamiulla, DSRamachandra, M Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors. Bioorg Med Chem Lett25:5309-14 (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:
BDBM50130871
n/a
NameBDBM50130871
Synonyms:CHEMBL3632760
TypeSmall organic molecule
Emp. Form.C20H21FN4
Mol. Mass.336.4059
SMILESNC(=N)c1ccc2[nH]c(cc2c1)-c1cccc(n1)C1(F)CCCCC1
Structure
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