General Information of the Protein
Protein ID
PT03634
Protein Name
Transmembrane protease serine 6
Secondarily
Protein Name
Matriptase-2
Gene Name
TMPRSS6
Secondarily
Gene Name
UNQ354/PRO618
Sequence
MLLLFHSKRMPVAEAPQVAGGQGDGGDGEEAEPEGMFKACEDSKRKARGYLRLVPLFVLLALLVLASAGVLLWYFLGYKAEVMVSQVYSGSLRVLNRHFSQDLTRRESSAFRSETAKAQKMLKELITSTRLGTYYNSSSVYSFGEGPLTCFFWFILQIPEHRRLMLSPEVVQALLVEELLSTVNSSAAVPYRAEYEVDPEGLVILEASVKDIAALNSTLGCYRYSYVGQGQVLRLKGPDHLASSCLWHLQGPKDLMLKLRLEWTLAECRDRLAMYDVAGPLEKRLITSVYGCSRQEPVVEVLASGAIMAVVWKKGLHSYYDPFVLSVQPVVFQACEVNLTLDNRLDSQGVLSTPYFPSYYSPQTHCSWHLTVPSLDYGLALWFDAYALRRQKYDLPCTQGQWTIQNRRLCGLRILQPYAERIPVVATAGITINFTSQISLTGPGVRVHYGLYNQSDPCPGEFLCSVNGLCVPACDGVKDCPNGLDERNCVCRATFQCKEDSTCISLPKVCDGQPDCLNGSDEEQCQEGVPCGTFTFQCEDRSCVKKPNPQCDGRPDCRDGSDEEHCDCGLQGPSSRIVGGAVSSEGEWPWQASLQVRGRHICGGALIADRWVITAAHCFQEDSMASTVLWTVFLGKVWQNSRWPGEVSFKVSRLLLHPYHEEDSHDYDVALLQLDHPVVRSAAVRPVCLPARSHFFEPGLHCWITGWGALREGGPISNALQKVDVQLIPQDLCSEVYRYQVTPRMLCAGYRKGKKDACQGDSGGPLVCKALSGRWFLAGLVSWGLGCGRPNYFGVYTRITGVISWIQQVVT
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Serine protease
Function
Membrane-bound serine protease (PubMed:18976966, PubMed:20518742, PubMed:25156943, PubMed:25588876). Through the cleavage of cell surface HJV, a regulator of the expression of the iron absorption-regulating hormone hepicidin/HAMP, plays a role in iron homeostasis (PubMed:25156943, PubMed:18408718, PubMed:18976966).
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Uniprot ID
Primary ID:
Q8IU80

Secondarily ID:
B0QYB4
B0QYB7
B0QYB8
Q5TI06
Q6ICC2
Q6UXD8
Q8IUE2
Q8IXV8
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HGNC ID
HGNC:16517
Subcellular Location
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: CL000006 , HEK293
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0157988
 Compound Info 
1-[2-[1-[(2S)-3-(3-carbamimidoylphenyl)-2-[[3-(2,4-dichlorophenyl)phenyl]sulfonylamino]propanoyl]piperidin-4-yl]ethyl]-3-methylurea
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C31H36Cl2N6O4S
  1
1
Ki = 73 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0059524
 Compound Info 
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[3-(2,4-dichlorophenyl)phenyl]sulfonylamino]-3-oxopropyl]benzenecarboximidamide
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C29H33Cl2N5O3S
  1
1
Ki = 110 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0086496
 Compound Info 
1-[2-[1-[(2S)-3-(3-carbamimidoylphenyl)-2-[[3-(2,4-dimethoxyphenyl)phenyl]sulfonylamino]propanoyl]piperidin-4-yl]ethyl]-3-methylurea
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C33H42N6O6S
  1
1
Ki = 180 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0807142
 Compound Info 
Benzylsulfonyl-D-argininyl-proline-(4-amidinobenzyl)amide Bis-(trifluoroacetate)
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C28H37F3N8O6S
  1
1
Ki = 190 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0767385
 Compound Info 
(S)-3-(3-(4-(2-aminoethyl)piperidin-1-yl)-2-(2',3'-dichlorobiphenyl-3-ylsulfonamido)-3-oxopropyl)benzimidamide
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C29H33Cl2N5O3S
  1
1
Ki = 210 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0704349
 Compound Info 
Benzylsulfonyl-D-cyclohexylalanyl-proline-(4-amidinobenzyl)-amide Trifluoroacetate
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C31H40F3N5O6S
  1
1
Ki = 290 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0086492
 Compound Info 
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[3-(2,4-dimethoxyphenyl)phenyl]sulfonylamino]-3-oxopropyl]benzenecarboximidamide
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C31H39N5O5S
  1
1
Ki = 310 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0174302
 Compound Info 
4-[1-[(2S)-3-(3-carbamimidoylphenyl)-2-[[3-(2,4-dichlorophenyl)phenyl]sulfonylamino]propanoyl]piperidin-4-yl]-N-methylbutanamide
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C32H37Cl2N5O4S
  1
1
Ki = 350 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0709768
 Compound Info 
(S)-3-(3-(4-(2-aminoethyl)piperidin-1-yl)-2-(2'-chloro-4'-ethoxybiphenyl-3-ylsulfonamido)-3-oxopropyl)benzimidamide
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C31H38ClN5O4S
  1
1
Ki = 400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0709778
 Compound Info 
(S)-3-amino-N-(3-(N-(3-(3-carbamimidoylphenyl)-1-(4-(2-(3-ethylureido)ethyl)piperidin-1-yl)-1-oxopropan-2-yl)sulfamoyl)phenyl)propanamide
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C29H42N8O5S
  1
1
Ki = 460 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0673482
 Compound Info 
(S)-3-(3-(4-(2-aminoethyl)piperidin-1-yl)-2-(3',4'-dichlorobiphenyl-3-ylsulfonamido)-3-oxopropyl)benzimidamide
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C29H33Cl2N5O3S
  1
1
Ki = 580 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0659824
 Compound Info 
(S)-4-(1-(3-(3-carbamimidoylphenyl)-2-(2',3'-dichlorobiphenyl-3-ylsulfonamido)propanoyl)piperidin-4-yl)-N-methylbutanamide
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C32H37Cl2N5O4S
  1
1
Ki = 750 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0677568
 Compound Info 
(S)-4-(1-(3-(3-carbamimidoylphenyl)-2-(2',4'-dimethoxybiphenyl-3-ylsulfonamido)propanoyl)piperidin-4-yl)-N-methylbutanamide
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C34H43N5O6S
  1
1
Ki = 770 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0709780
 Compound Info 
(S)-3-amino-N-(3-(N-(3-(3-carbamimidoylphenyl)-1-(4-(3-cyclohexylureido)piperidin-1-yl)-1-oxopropan-2-yl)sulfamoyl)phenyl)propanamide
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C31H44N8O5S
  1
1
Ki = 790 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0086494
 Compound Info 
1-[1-[(2S)-3-(3-carbamimidoylphenyl)-2-[[3-(2,4-dichlorophenyl)phenyl]sulfonylamino]propanoyl]piperidin-4-yl]-3-cyclohexylurea
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C34H40Cl2N6O4S
  1
1
Ki = 940 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0761783
 Compound Info 
(S)-3-amino-N-(3-(N-(1-(4-(3-benzylureido)piperidin-1-yl)-3-(3-carbamimidoylphenyl)-1-oxopropan-2-yl)sulfamoyl)phenyl)propanamide
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C32H40N8O5S
  1
1
Ki = 1100 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0214602
 Compound Info 
4-[4-(4-carbamimidoylphenyl)piperazin-1-yl]benzenecarboximidamide
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C18H22N6
  1
1
Ki = 1160 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0709774
 Compound Info 
(S)-3-amino-N-(3-(N-(3-(3-carbamimidoylphenyl)-1-(4-(2-(3-methylureido)ethyl)piperidin-1-yl)-1-oxopropan-2-yl)sulfamoyl)phenyl)propanamide
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C28H40N8O5S
  1
1
Ki = 1200 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0659825
 Compound Info 
(S)-3-amino-N-(3-(N-(1-(4-(2-(3-benzylureido)ethyl)piperidin-1-yl)-3-(3-carbamimidoylphenyl)-1-oxopropan-2-yl)sulfamoyl)phenyl)propanamide
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C34H44N8O5S
  1
1
Ki = 1300 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0673480
 Compound Info 
(S)-3-amino-N-(3-(N-(3-(3-carbamimidoylphenyl)-1-(4-(3-methylureido)piperidin-1-yl)-1-oxopropan-2-yl)sulfamoyl)phenyl)propanamide
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C26H36N8O5S
  1
1
Ki = 1300 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0709771
 Compound Info 
(S)-3-amino-N-(3-(N-(3-(3-carbamimidoylphenyl)-1-oxo-1-(4-(3-phenylureido)piperidin-1-yl)propan-2-yl)sulfamoyl)phenyl)propanamide
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C31H38N8O5S
  1
1
Ki = 1300 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0709773
 Compound Info 
(S)-4-(1-(3-(3-carbamimidoylphenyl)-2-(2'-chloro-4'-ethoxybiphenyl-3-ylsulfonamido)propanoyl)piperidin-4-yl)-N-methylbutanamide
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C34H42ClN5O5S
  1
1
Ki = 1300 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0059527
 Compound Info 
1-[1-[(2S)-3-(3-carbamimidoylphenyl)-2-[[3-(2,4-dimethoxyphenyl)phenyl]sulfonylamino]propanoyl]piperidin-4-yl]-3-cyclohexylurea
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C36H46N6O6S
  1
1
Ki = 1420 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0769761
 Compound Info 
(S)-4-(1-(3-(3-carbamimidoylphenyl)-2-(3',4'-dichlorobiphenyl-3-ylsulfonamido)propanoyl)piperidin-4-yl)-N-methylbutanamide
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C32H37Cl2N5O4S
  1
1
Ki = 1600 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0226194
 Compound Info 
4-[8-(4-carbamimidoylanilino)octylamino]benzenecarboximidamide
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C22H32N6
  1
1
Ki = 1640 nM
 Bioactivity Info 
   TI
   LI
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CP0659826
 Compound Info 
(S)-3-amino-N-(3-(N-(3-(3-carbamimidoylphenyl)-1-(4-(2-(3-cyclohexylureido)ethyl)piperidin-1-yl)-1-oxopropan-2-yl)sulfamoyl)phenyl)propanamide
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C33H48N8O5S
  1
1
Ki = 1800 nM
 Bioactivity Info 
   TI
   LI
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CP0780495
 Compound Info 
(S)-3-amino-N-(3-(N-(3-(3-carbamimidoylphenyl)-1-oxo-1-(4-(2-(3-phenylureido)ethyl)piperidin-1-yl)propan-2-yl)sulfamoyl)phenyl)propanamide
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C33H42N8O5S
  1
1
Ki = 1900 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0692378
 Compound Info 
(S)-3-(3-(4-(2-aminoethyl)piperidin-1-yl)-2-(2'-fluorobiphenyl-3-ylsulfonamido)-3-oxopropyl)benzimidamide
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C29H34FN5O3S
  1
1
Ki = 2100 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0038011
 Compound Info 
CHEBI:6426
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C20H38N6O4
  1
1
Ki = 2400 nM
 Bioactivity Info 
   TI
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   LO
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CP0709779
 Compound Info 
(S)-3-amino-N-(3-(N-(3-(3-carbamimidoylphenyl)-1-(4-(3-ethylureido)piperidin-1-yl)-1-oxopropan-2-yl)sulfamoyl)phenyl)propanamide
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C27H38N8O5S
  1
1
Ki = 2400 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0677566
 Compound Info 
(S)-4-(1-(3-(3-carbamimidoylphenyl)-2-(2'-fluorobiphenyl-3-ylsulfonamido)propanoyl)piperidin-4-yl)-N-methylbutanamide
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C32H38FN5O4S
  1
1
Ki = 3000 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0659822
 Compound Info 
(S)-3-(3-(4-(2-aminoethyl)piperidin-1-yl)-2-(4'-fluorobiphenyl-3-ylsulfonamido)-3-oxopropyl)benzimidamide
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C29H34FN5O3S
  1
1
Ki = 3200 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0804353
 Compound Info 
(S)-3-(3-(4-(2-aminoethyl)piperidin-1-yl)-2-(3'-fluorobiphenyl-3-ylsulfonamido)-3-oxopropyl)benzimidamide
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C29H34FN5O3S
  1
1
Ki = 3200 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0767383
 Compound Info 
(S)-3-amino-N-(3-(N-(3-(3-carbamimidoylphenyl)-1-oxo-1-(4-(2-ureidoethyl)piperidin-1-yl)propan-2-yl)sulfamoyl)phenyl)propanamide
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C27H38N8O5S
  1
1
Ki = 3300 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0179945
 Compound Info 
4-[7-(4-carbamimidoylanilino)heptylamino]benzenecarboximidamide
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C21H30N6
  1
1
Ki = 3680 nM
 Bioactivity Info 
   TI
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CP0761784
 Compound Info 
(S)-3-amino-N-(3-(N-(3-(3-carbamimidoylphenyl)-1-oxo-1-(4-ureidopiperidin-1-yl)propan-2-yl)sulfamoyl)phenyl)propanamide
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C25H34N8O5S
  1
1
Ki = 3900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0231244
 Compound Info 
4-[4-(4-carbamimidoylphenyl)-1,4-diazepan-1-yl]benzenecarboximidamide
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C19H24N6
  1
1
Ki = 4390 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0804352
 Compound Info 
(S)-4-(1-(3-(3-carbamimidoylphenyl)-2-(4'-fluorobiphenyl-3-ylsulfonamido)propanoyl)piperidin-4-yl)-N-methylbutanamide
   Show/Hide
C32H38FN5O4S
  1
1
Ki = 4400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0342900
 Compound Info 
4,4''-(1,2-Phenylenebis(Methylene))Bis(Oxy)Dibenzimidamide
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C22H22N4O2
  1
1
Ki = 5200 nM
 Bioactivity Info 
   TI
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CP0054560
 Compound Info 
4,4''-(1,4-Phenylenebis(Methylene))Bis(Oxy)Dibenzimidamide
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C22H22N4O2
  1
1
Ki = 5700 nM
 Bioactivity Info 
   TI
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CP0214603
 Compound Info 
N,N'-bis(4-carbamimidoylphenyl)oxamide
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C16H16N6O2
  1
1
Ki = 6230 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0754265
 Compound Info 
Benzylsulfonyl-D-arginyl-proline-(2-aminomethyl-5-chlorobenzyl)-amide Bis(trifluoroacetate)
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C28H37ClF3N7O6S
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0844406
 Compound Info 
Benzylsulfonyl-D-cyclohexylalanyl-proline-(2-aminomethyl-5-chlorobenzyl)amide Trifluoroacetate
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C31H40ClF3N4O6S
  1
1
Ki > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0659823
 Compound Info 
(S)-4-(1-(3-(3-carbamimidoylphenyl)-2-(3'-fluorobiphenyl-3-ylsulfonamido)propanoyl)piperidin-4-yl)-N-methylbutanamide
   Show/Hide
C32H38FN5O4S
  1
1
Ki = 10000 nM
 Bioactivity Info 
   TI
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Cell Line ID: CL000262 , MT-2
 Cell Line Info 
Cell Line ID: CL000090 , Schneider 2
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0177130
 Compound Info 
(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-3-methylbutanamide
   Show/Hide
C36H44N8O6S
  1
1 Ki = 2.56 nM
Clinical Information about the Protein
Target 1 ( Transmembrane protease serine 6 (TMPRSS6) )
Target Type Literature-reported Target
Target 2 ( TMPRSS6 messenger RNA (TMPRSS6 mRNA) )
Target Type Clinical trial Target