General Information of the Protein
Protein ID
PT01387
Protein Name
Furin
Secondarily
Protein Name
Dibasic-processing enzyme
Paired basic amino acid residue-cleaving enzyme
Gene Name
FURIN
Secondarily
Gene Name
FUR
PACE
PCSK3
Sequence
MELRPWLLWVVAATGTLVLLAADAQGQKVFTNTWAVRIPGGPAVANSVARKHGFLNLGQIFGDYYHFWHRGVTKRSLSPHRPRHSRLQREPQVQWLEQQVAKRRTKRDVYQEPTDPKFPQQWYLSGVTQRDLNVKAAWAQGYTGHGIVVSILDDGIEKNHPDLAGNYDPGASFDVNDQDPDPQPRYTQMNDNRHGTRCAGEVAAVANNGVCGVGVAYNARIGGVRMLDGEVTDAVEARSLGLNPNHIHIYSASWGPEDDGKTVDGPARLAEEAFFRGVSQGRGGLGSIFVWASGNGGREHDSCNCDGYTNSIYTLSISSATQFGNVPWYSEACSSTLATTYSSGNQNEKQIVTTDLRQKCTESHTGTSASAPLAAGIIALTLEANKNLTWRDMQHLVVQTSKPAHLNANDWATNGVGRKVSHSYGYGLLDAGAMVALAQNWTTVAPQRKCIIDILTEPKDIGKRLEVRKTVTACLGEPNHITRLEHAQARLTLSYNRRGDLAIHLVSPMGTRSTLLAARPHDYSADGFNDWAFMTTHSWDEDPSGEWVLEIENTSEANNYGTLTKFTLVLYGTAPEGLPVPPESSGCKTLTSSQACVVCEEGFSLHQKSCVQHCPPGFAPQVLDTHYSTENDVETIRASVCAPCHASCATCQGPALTDCLSCPSHASLDPVEQTCSRQSQSSRESPPQQQPPRLPPEVEAGQRLRAGLLPSHLPEVVAGLSCAFIVLVFVTVFLVLQLRSGFSFRGVKVYTMDRGLISYKGLPPEAWQEECPSDSEEDEGRGERTAFIKDQSAL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Serine protease
>
Serine protease SB clan
>
Serine protease S8B subfamily
Function
Ubiquitous endoprotease within constitutive secretory pathways capable of cleavage at the RX(K/R)R consensus motif (PubMed:11799113, PubMed:1629222, PubMed:1713771, PubMed:2251280, PubMed:24666235, PubMed:25974265, PubMed:7592877, PubMed:7690548, PubMed:9130696). Mediates processing of TGFB1, an essential step in TGF-beta-1 activation (PubMed:7737999). Converts through proteolytic cleavage the non-functional Brain natriuretic factor prohormone into its active hormone BNP(1-32) (PubMed:20489134, PubMed:21763278). By mediating processing of accessory subunit ATP6AP1/Ac45 of the V-ATPase, regulates the acidification of dense-core secretory granules in islets of Langerhans cells (By similarity).
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Uniprot ID
Primary ID:
P09958

Secondarily ID:
Q14336
Q6LBS3
Q9UCZ5
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Ensembl ID
ENSG00000140564
HGNC ID
HGNC:8568
Subcellular Location
Golgi apparatus
Trans-Golgi network membrane
Cell membrane
Secreted
Endosome 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: CL000011 , CHO
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0130814
 Compound Info 
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C33H50N12O4
  1
1
Ki = 0.81 nM
 Bioactivity Info 
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CP0512633
 Compound Info 
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-(diaminomethylideneamino)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C32H49N15O4
  1
1
Ki = 0.83 nM
 Bioactivity Info 
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CP0528191
 Compound Info 
(2S,3S)-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanoyl]amino]-3-methylpentanamide
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C34H52N12O4
  1
1
Ki = 0.84 nM
 Bioactivity Info 
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CP0457399
 Compound Info 
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C37H50N12O4
  1
1
Ki = 1.4 nM
 Bioactivity Info 
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CP0506636
 Compound Info 
(2S)-6-amino-N-[(4-carbamimidoylphenyl)methyl]-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanoyl]amino]-3-methylbutanoyl]amino]hexanamide
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C33H50N10O4
  1
1
Ki = 1.5 nM
 Bioactivity Info 
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CP0428275
 Compound Info 
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C37H50N12O5
  1
1
Ki = 1.9 nM
 Bioactivity Info 
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CP0375110
 Compound Info 
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C34H53N15O4
  1
1
Ki = 3 nM
 Bioactivity Info 
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CP0507962
 Compound Info 
(2S)-N-[(2S)-3-amino-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C31H47N13O4
  1
1
Ki = 3 nM
 Bioactivity Info 
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CP0527378
 Compound Info 
(2S)-6-amino-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanoyl]amino]hexanamide
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C34H53N13O4
  1
1
Ki = 3.6 nM
 Bioactivity Info 
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CP0473546
 Compound Info 
(2S)-6-amino-2-[[(2S)-3-amino-2-[[(2S)-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanoyl]amino]propanoyl]amino]-N-[(4-carbamimidoylphenyl)methyl]hexanamide
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C31H47N11O4
  1
1
Ki = 3.7 nM
 Bioactivity Info 
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CP0528900
 Compound Info 
(2S)-N-[(2R)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C31H46N12O4S
  1
1
Ki = 5.9 nM
 Bioactivity Info 
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CP0376045
 Compound Info 
(2S)-N-[(2S,3R)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C32H48N12O5
  1
1
Ki = 6 nM
 Bioactivity Info 
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CP0512634
 Compound Info 
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C34H48N14O4
  1
1
Ki = 6.3 nM
 Bioactivity Info 
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CP0513820
 Compound Info 
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C39H51N13O4
  1
1
Ki = 6.3 nM
 Bioactivity Info 
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CP0501244
 Compound Info 
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C33H50N12O4S
  1
1
Ki = 9.7 nM
 Bioactivity Info 
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CP0425432
 Compound Info 
(2S)-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanoyl]amino]-4-methylpentanamide
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C34H52N12O4
  1
1
Ki = 12 nM
 Bioactivity Info 
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CP0505324
 Compound Info 
(2S)-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanoyl]amino]pentanediamide
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C33H49N13O5
  1
1
Ki = 13 nM
 Bioactivity Info 
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CP0471604
 Compound Info 
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C31H46N12O4
  1
1
Ki = 19 nM
 Bioactivity Info 
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CP0534797
 Compound Info 
(2S)-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[[(2S)-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanoyl]amino]butanediamide
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C32H47N13O5
  1
1
Ki = 23 nM
 Bioactivity Info 
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CP0527379
 Compound Info 
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C31H46N12O5
  1
1
Ki = 24 nM
 Bioactivity Info 
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CP0506633
 Compound Info 
(2S)-N-[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(2S)-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanoyl]pyrrolidine-2-carboxamide
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C33H48N12O4
  1
1
Ki = 37 nM
 Bioactivity Info 
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CP0457400
 Compound Info 
(2S)-N-[2-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C30H44N12O4
  1
1
Ki = 40 nM
 Bioactivity Info 
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CP0457404
 Compound Info 
(4S)-5-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-[[(2S)-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanoyl]amino]-5-oxopentanoic acid
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C33H48N12O6
  1
1
Ki = 102 nM
 Bioactivity Info 
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CP0506634
 Compound Info 
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C34H52N12O4
  1
1
Ki = 142 nM
 Bioactivity Info 
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CP0431722
 Compound Info 
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-5-(carbamoylamino)-2-[(2-phenylacetyl)amino]pentanamide
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C33H49N11O5
  1
1
Ki = 238 nM
 Bioactivity Info 
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CP0527185
 Compound Info 
(2S)-6-amino-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-2-[(2-phenylacetyl)amino]hexanamide
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C33H50N10O4
  1
1
Ki = 285 nM
 Bioactivity Info 
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CP0428276
 Compound Info 
(3S)-4-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[(2S)-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanoyl]amino]-4-oxobutanoic acid
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C32H46N12O6
  1
1
Ki = 405 nM
 Bioactivity Info 
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CP0512635
 Compound Info 
benzyl N-[(5S)-6-[[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-6-oxo-5-[(2-phenylacetyl)amino]hexyl]carbamate
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C41H56N10O6
  1
1
Ki = 702 nM
 Bioactivity Info 
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CP0512638
 Compound Info 
(2R)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C33H50N12O4
  1
1
Ki = 970 nM
 Bioactivity Info 
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CP0457406
 Compound Info 
(2S)-N-[(2R)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C33H50N12O4
  1
1
Ki = 1110 nM
 Bioactivity Info 
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CP0512636
 Compound Info 
(2S)-N-[(2R)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C31H46N12O4
  1
1
Ki = 1385 nM
 Bioactivity Info 
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CP0501245
 Compound Info 
(2S)-2-[[(2S)-2-acetamido-3-methylbutanoyl]amino]-N-[(4-carbamimidoylphenyl)methyl]-5-(diaminomethylideneamino)pentanamide
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C21H34N8O3
  1
1
Ki = 2390 nM
 Bioactivity Info 
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CP0528192
 Compound Info 
(2S)-5-(diaminomethylideneamino)-2-[[(2R)-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanoyl]amino]pentanoic acid
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C20H32N8O4
  1
1
Ki = 3200 nM
 Bioactivity Info 
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CP0468839
 Compound Info 
(2S)-N-[(4-carbamimidoylphenyl)methyl]-5-(diaminomethylideneamino)-2-[[(2R)-5-(diaminomethylideneamino)-2-[[(2S)-3-methyl-2-[(2-phenylacetyl)amino]butanoyl]amino]pentanoyl]amino]pentanamide
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C33H50N12O4
  1
1
Ki = 7340 nM
 Bioactivity Info 
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Cell Line ID: CL000090 , Schneider 2
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0393429
 Compound Info 
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylbutanoyl]amino]-6-amino-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]hexanamide
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C49H94N16O9
  1
1 IC50 = 20 nM
CP0130814
 Compound Info 
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-5-(diaminomethylideneamino)-2-[(2-phenylacetyl)amino]pentanamide
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C33H50N12O4
  1
1 Ki = 0.81 nM
CP0247982
 Compound Info 
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-acetamido-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylbutanoyl]amino]-6-amino-N-[(4-carbamimidoylphenyl)methyl]hexanamide
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C51H90N14O8
  1
1 Ki = 9.8 nM
CP0431722
 Compound Info 
(2S)-N-[(2S)-1-[[(2S)-1-[(4-carbamimidoylphenyl)methylamino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-5-(carbamoylamino)-2-[(2-phenylacetyl)amino]pentanamide
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C33H49N11O5
  1
1 Ki = 238 nM
CP0365035
 Compound Info 
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-acetamido-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylbutanoyl]amino]-6-amino-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]hexanamide
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C49H94N16O9
  1
1 Ki = 760 nM
CP0146918
 Compound Info 
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylbutanoyl]amino]-6-amino-N-[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]hexanamide
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C37H72N14O7
  1
1 Ki = 1400 nM
Clinical Information about the Protein
Target 1 ( Dibasic-processing enzyme (Furin) )
Target Type Preclinical Target
Target 2 ( HUMAN dibasic-processing enzyme (Furin) )
Target Type Unknown Type Target