General Information of the Protein
Protein ID
PT03005
Protein Name
Serine protease hepsin
Secondarily
Protein Name
Transmembrane protease serine 1
Gene Name
HPN
Secondarily
Gene Name
TMPRSS1
Sequence
MAQKEGGRTVPCCSRPKVAALTAGTLLLLTAIGAASWAIVAVLLRSDQEPLYPVQVSSADARLMVFDKTEGTWRLLCSSRSNARVAGLSCEEMGFLRALTHSELDVRTAGANGTSGFFCVDEGRLPHTQRLLEVISVCDCPRGRFLAAICQDCGRRKLPVDRIVGGRDTSLGRWPWQVSLRYDGAHLCGGSLLSGDWVLTAAHCFPERNRVLSRWRVFAGAVAQASPHGLQLGVQAVVYHGGYLPFRDPNSEENSNDIALVHLSSPLPLTEYIQPVCLPAAGQALVDGKICTVTGWGNTQYYGQQAGVLQEARVPIISNDVCNGADFYGNQIKPKMFCAGYPEGGIDACQGDSGGPFVCEDSISRTPRWRLCGIVSWGTGCALAQKPGVYTKVSDFREWIFQAIKTHSEASGMVTQL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Serine protease
Function
Serine protease that cleaves extracellular substrates, and contributes to the proteolytic processing of growth factors, such as HGF and MST1/HGFL (PubMed:21875933, PubMed:15839837). Plays a role in cell growth and maintenance of cell morphology (PubMed:8346233, PubMed:21875933). Plays a role in the proteolytic processing of ACE2 (PubMed:24227843). Mediates the proteolytic cleavage of urinary UMOD that is required for UMOD polymerization (PubMed:26673890).
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Uniprot ID
Primary ID:
P05981

Secondarily ID:
B2RDS4
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Ensembl ID
ENSG00000105707
HGNC ID
HGNC:5155
Subcellular Location
Cell membrane
Apical cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000243 , MCF-10A
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0065004
 Compound Info 
(2R)-N-(4-carbamimidoylphenyl)-2-[(4-methylphenyl)sulfonylamino]-2-phenylacetamide
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C22H22N4O3S
  1
1
IC50 = 100 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0064994
 Compound Info 
(2R)-N-(4-carbamimidoylphenyl)-2-cyclohexyl-2-[(4-methylphenyl)sulfonylamino]acetamide
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C22H28N4O3S
  1
1
IC50 = 990 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0099151
 Compound Info 
(2R)-N-(4-carbamimidoylphenyl)-2-cyclohexyl-2-[(4-fluorophenyl)sulfonylamino]acetamide
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C21H25FN4O3S
  1
1
IC50 = 1290 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0521056
 Compound Info 
(2R)-N-(4-carbamimidoylphenyl)-2-cyclohexyl-2-[[4-(trifluoromethyl)phenyl]sulfonylamino]acetamide
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C22H25F3N4O3S
  1
1
IC50 = 3150 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0384876
 Compound Info 
ethyl 4-[(2R)-3-(3-carbamimidoylphenyl)-2-[[2,4,6-tri(propan-2-yl)phenyl]sulfonylamino]propanoyl]piperazine-1-carboxylate
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C32H47N5O5S
  1
1
IC50 = 6490 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000265 , NS0
 Cell Line Info 
Cell Line ID: CL000090 , Schneider 2
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0384876
 Compound Info 
ethyl 4-[(2R)-3-(3-carbamimidoylphenyl)-2-[[2,4,6-tri(propan-2-yl)phenyl]sulfonylamino]propanoyl]piperazine-1-carboxylate
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C32H47N5O5S
  1
1 IC50 = 3000 nM
CP0082712
 Compound Info 
4-Guanidino-benzoic acid 6-carbamimidoyl-naphthalen-2-yl ester
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C19H17N5O2
  1
1 Ki = 0.53 nM
CP0098764
 Compound Info 
9H-fluoren-9-ylmethyl N-[(2S)-4-amino-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamate
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C32H33N7O5S
  1
1 Ki = 1.7 nM
CP0225577
 Compound Info 
9H-fluoren-9-ylmethyl N-[2-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]carbamate
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C30H30N6O4S
  1
1 Ki = 831 nM
Clinical Information about the Protein
Target 1 ( Serine protease hepsin (HPN) )
Target Type Patented-recorded Target