General Information of the Protein
Protein ID
PT01158
Protein Name
Tyrosine-protein phosphatase non-receptor type 1
Secondarily
Protein Name
Protein-tyrosine phosphatase 1B
Gene Name
PTPN1
Secondarily
Gene Name
PTP1B
Sequence
MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLHQEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLKCAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWPDFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKDPSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLEPPPEHIPPPPRPPKRILEPHNGKCREFFPNHQWVKEETQEDKDCPIKEEKGSPLNAAPYGIESMSQDTEVRSRVVGGSLRGAQAASPAKGEPSLPEKDEDHALSYWKPFLVNMCVATVLTAGAYLCYRFLFNSNT
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Phosphatase
>
Protein Phosphatase
>
Tyrosine protein phosphatase
Function
Tyrosine-protein phosphatase which acts as a regulator of endoplasmic reticulum unfolded protein response. Mediates dephosphorylation of EIF2AK3/PERK; inactivating the protein kinase activity of EIF2AK3/PERK. May play an important role in CKII- and p60c-src-induced signal transduction cascades. May regulate the EFNA5-EPHA3 signaling pathway which modulates cell reorganization and cell-cell repulsion. May also regulate the hepatocyte growth factor receptor signaling pathway through dephosphorylation of MET.
    Show/Hide
Uniprot ID
Primary ID:
P18031

Secondarily ID:
Q5TGD8
Q9BQV9
Q9NQQ4
    Show/Hide
Ensembl ID
ENSG00000196396
HGNC ID
HGNC:9642
Subcellular Location
Endoplasmic reticulum 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
CP0218985
 Compound Info 
2-hydroxy-5-[5-[4-[[(2R,3R,4S,5R,6S)-3,4,5-tribenzoyloxy-6-methoxyoxan-2-yl]methoxymethyl]triazol-1-yl]pentoxy]benzoic acid
   Show/Hide
C43H43N3O13
  1
1
IC50 = 6700 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0198921
 Compound Info 
2-hydroxy-5-[4-[4-[[(2R,3R,4S,5R,6S)-3,4,5-tribenzoyloxy-6-methoxyoxan-2-yl]methoxymethyl]triazol-1-yl]butoxy]benzoic acid
   Show/Hide
C42H41N3O13
  1
1
IC50 = 8700 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0399056
 Compound Info 
3-hydroxy-5-[5-[4-[[(2R,3R,4S,5R,6S)-3,4,5-tribenzoyloxy-6-methoxyoxan-2-yl]methoxymethyl]triazol-1-yl]pentoxy]benzoic acid
   Show/Hide
C43H43N3O13
  1
1
IC50 = 16600 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0509388
 Compound Info 
3-hydroxy-5-[4-[4-[[(2R,3R,4S,5R,6S)-3,4,5-tribenzoyloxy-6-methoxyoxan-2-yl]methoxymethyl]triazol-1-yl]butoxy]benzoic acid
   Show/Hide
C42H41N3O13
  1
1
IC50 = 19300 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0528096
 Compound Info 
3-hydroxy-5-[3-[4-[[(2R,3R,4S,5R,6S)-3,4,5-tribenzoyloxy-6-methoxyoxan-2-yl]methoxymethyl]triazol-1-yl]propoxy]benzoic acid
   Show/Hide
C41H39N3O13
  1
1
IC50 = 19700 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0456067
 Compound Info 
2-hydroxy-5-[3-[4-[[(2R,3R,4S,5R,6S)-3,4,5-tribenzoyloxy-6-methoxyoxan-2-yl]methoxymethyl]triazol-1-yl]propoxy]benzoic acid
   Show/Hide
C41H39N3O13
  1
1
IC50 = 28900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0484959
 Compound Info 
3-[5-[4-[[(2R,3R,4S,5R,6S)-3,4,5-tribenzoyloxy-6-methoxyoxan-2-yl]methoxymethyl]triazol-1-yl]pentoxy]benzoic acid
   Show/Hide
C43H43N3O12
  1
1
IC50 = 38700 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0509387
 Compound Info 
3-[4-[4-[[(2R,3R,4S,5R,6S)-3,4,5-tribenzoyloxy-6-methoxyoxan-2-yl]methoxymethyl]triazol-1-yl]butoxy]benzoic acid
   Show/Hide
C42H41N3O12
  1
1
IC50 = 60100 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0474698
 Compound Info 
3-[3-[4-[[(2R,3R,4S,5R,6S)-3,4,5-tribenzoyloxy-6-methoxyoxan-2-yl]methoxymethyl]triazol-1-yl]propoxy]benzoic acid
   Show/Hide
C41H39N3O12
  1
1
IC50 = 64600 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0039361
 Compound Info 
3,5-DIHYDROXYBENZOATE
   Show/Hide
C7H6O4
  1
1
IC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0057570
 Compound Info 
2,5-Dihydroxybenzoate, VI
   Show/Hide
C7H6O4
  1
1
IC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0198720
 Compound Info 
3-Hydroxy-benzoic acid
   Show/Hide
C7H6O3
  1
1
IC50 > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0054352
 Compound Info 
(3S)-3-{[(1S)-1-carbamoyl-2-{4-[difluoro(phosphono)methyl]phenyl}ethyl]carbamoyl}-3-(2-{4-[difluoro(phosphono)methyl]phenyl}acetamido)propanoic acid
   Show/Hide
C23H25F4N3O11P2
  2
1 IC50 = 2.4 nM
2 Ki = 2.4 nM
CP0166681
 Compound Info 
3-{4-[2-(1H-1,2,3-benzotriazol-1-yl)-3-{4-[difluoro(phosphono)methyl]phenyl}-2-phenylpropyl]phenyl}benzene-1-phosphonic acid
   Show/Hide
C34H29F2N3O6P2
  1
1 IC50 = 3 nM
CP0267727
 Compound Info 
[[4-[2-(benzotriazol-1-yl)-3-[3-bromo-4-[difluoro(phosphono)methyl]phenyl]-2-phenylpropyl]phenyl]-difluoromethyl]phosphonic acid
   Show/Hide
C29H24BrF4N3O6P2
  1
1 IC50 = 5 nM
CP0152540
 Compound Info 
4-{1-Benzotriazol-1-yl-1-[4-(difluoro-phosphono-methyl)-benzyl]-2-[4-(difluoro-phosphono-methyl)-phenyl]-ethyl}-benzoic acid methyl ester
   Show/Hide
C31H27F4N3O8P2
  1
1 IC50 = 11 nM
CP0112045
 Compound Info 
({4-[2-(1H-1,2,3-benzotriazol-1-yl)-3-{4-[difluoro(phosphono)methyl]phenyl}-2-(3,4-difluorophenyl)propyl]phenyl}difluoromethyl)phosphonic acid
   Show/Hide
C29H23F6N3O6P2
  1
1 IC50 = 12 nM
CP0194946
 Compound Info 
6-{4-[2-(1H-1,2,3-benzotriazol-1-yl)-3-{4-[difluoro(phosphono)methyl]phenyl}-2-phenylpropyl]phenyl}-2-methylquinoline-8-phosphonic acid
   Show/Hide
C38H32F2N4O6P2
  1
1 IC50 = 12 nM
CP0151508
 Compound Info 
[[4-[(E)-2-(benzotriazol-1-yl)-5-[4-[difluoro(phosphono)methyl]phenyl]-2-phenylpent-4-enyl]phenyl]-difluoromethyl]phosphonic acid
   Show/Hide
C31H27F4N3O6P2
  1
1 IC50 = 16 nM
CP0321165
 Compound Info 
({4-[2-(1H-1,2,3-benzotriazol-1-yl)-3-{4-[difluoro(phosphono)methyl]phenyl}-2-phenylpropyl]phenyl}difluoromethyl)phosphonic acid
   Show/Hide
C29H25F4N3O6P2
  1
1 IC50 = 16 nM
CP0245304
 Compound Info 
[[4-[2-(1,3-benzothiazol-2-yl)-2-(benzotriazol-1-yl)-3-[4-[difluoro(phosphono)methyl]phenyl]propyl]phenyl]-difluoromethyl]phosphonic acid
   Show/Hide
C30H24F4N4O6P2S
  1
1 IC50 = 18 nM
CP0078105
 Compound Info 
({4-[2-Benzotriazol-1-yl-3-[4-(difluoro-phosphono-methyl)-phenyl]-2-(4-phenyl-thiazol-2-yl)-propyl]-phenyl}-difluoro-methyl)-phosphonic acid
   Show/Hide
C32H26F4N4O6P2S
  1
1 IC50 = 19 nM
CP0080110
 Compound Info 
[[4-[2-(benzotriazol-1-yl)-3-[4-[difluoro(phosphono)methyl]phenyl]-2-quinolin-2-ylpropyl]phenyl]-difluoromethyl]phosphonic acid
   Show/Hide
C32H26F4N4O6P2
  1
1 IC50 = 20 nM
CP0212665
 Compound Info 
({4-[2-Benzotriazol-1-yl-3-[4-(difluoro-phosphono-methyl)-phenyl]-2-(1H-tetrazol-5-yl)-propyl]-phenyl}-difluoro-methyl)-phosphonic acid
   Show/Hide
C24H21F4N7O6P2
  1
1 IC50 = 32 nM
CP0303831
 Compound Info 
({4-[2-(1H-1,2,3-benzotriazol-1-yl)-2-phenyl-3-(4-phenylphenyl)propyl]phenyl}difluoromethyl)phosphonic acid
   Show/Hide
C34H28F2N3O3P
  1
1 IC50 = 38 nM
CP0268538
 Compound Info 
2-[4-(Carboxy-difluoro-methyl)-benzyl]-2-[4-(difluoro-phosphono-methyl)-benzyl]-malonic acid dibenzyl ester
   Show/Hide
C34H29F4O9P
  1
1 IC50 = 40 nM
CP0267562
 Compound Info 
[[4-[2-(benzotriazol-1-yl)-2,5-diphenylpentyl]phenyl]-difluoromethyl]phosphonic acid
   Show/Hide
C30H28F2N3O3P
  1
1 IC50 = 46 nM
CP0302509
 Compound Info 
({4-[(4E)-2-(1H-1,2,3-benzotriazol-1-yl)-2,5-diphenylpent-4-en-1-yl]phenyl}difluoromethyl)phosphonic acid
   Show/Hide
C30H26F2N3O3P
  1
1 IC50 = 49 nM
CP0081269
 Compound Info 
2,2-Bis-[4-(difluoro-phosphono-methyl)-benzyl]-malonic acid dibenzyl ester
   Show/Hide
C33H30F4O10P2
  1
1 IC50 = 60 nM
CP0102074
 Compound Info 
({4-[2-Benzotriazol-1-yl-2-phenyl-3-(2'-sulfamoyl-biphenyl-4-yl)-propyl]-phenyl}-difluoro-methyl)-phosphonic acid
   Show/Hide
C34H29F2N4O5PS
  1
1 IC50 = 69 nM
CP0267643
 Compound Info 
[[4-[2-(benzotriazol-1-yl)-2-phenyl-1-[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]ethyl]phenyl]-difluoromethyl]phosphonic acid
   Show/Hide
C34H26F2N7O3P
  1
1 IC50 = 74 nM
CP0102048
 Compound Info 
({4-[2-Benzotriazol-1-yl-3-(4-bromo-phenyl)-2-phenyl-propyl]-phenyl}-difluoro-methyl)-phosphonic acid
   Show/Hide
C28H23BrF2N3O3P
  1
1 IC50 = 89 nM
CP0263427
 Compound Info 
2-(4-Acetylsulfamoyl-benzyl)-2-[4-(difluoro-phosphono-methyl)-benzyl]-malonic acid dibenzyl ester
   Show/Hide
C34H32F2NO10PS
  1
1 IC50 = 90 nM
CP0212664
 Compound Info 
({4-[2-Benzotriazol-1-yl-3-(4-benzyloxy-phenyl)-2-phenyl-propyl]-phenyl}-difluoro-methyl)-phosphonic acid
   Show/Hide
C35H30F2N3O4P
  1
1 IC50 = 98 nM
CP0245576
 Compound Info 
2,2-Bis-[4-(difluoro-phosphono-methyl)-benzyl]-malonic acid diisopropyl ester
   Show/Hide
C25H30F4O10P2
  1
1 IC50 = 110 nM
CP0105082
 Compound Info 
(2-bromo-4-(3-oxo-2,3-diphenylpropyl)phenyl)difluoromethylphosphonic acid
   Show/Hide
C22H18BrF2O4P
  1
1 IC50 = 120 nM
CP0275477
 Compound Info 
[[4-[3-[4-[difluoro(phosphono)methyl]phenyl]-2,2-bis(phenylmethoxy)propyl]phenyl]-difluoromethyl]phosphonic acid
   Show/Hide
C31H30F4O8P2
  1
1 IC50 = 160 nM
CP0225529
 Compound Info 
[[4-[(E)-2-benzoyl-2,5-diphenylpent-4-enyl]phenyl]-difluoromethyl]phosphonic acid
   Show/Hide
C31H27F2O4P
  1
1 IC50 = 190 nM
CP0287450
 Compound Info 
2,2-Bis-[4-(difluoro-phosphono-methyl)-benzyl]-malonic acid benzyl ester methyl ester
   Show/Hide
C27H26F4O10P2
  1
1 IC50 = 190 nM
CP0211305
 Compound Info 
2-Benzotriazol-1-yl-3-[4-(difluoro-phosphono-methyl)-phenyl]-2-phenyl-propionic acid benzyl ester
   Show/Hide
C29H24F2N3O5P
  1
1 IC50 = 240 nM
CP0278748
 Compound Info 
[[2-chloro-4-(3-oxo-2,3-diphenylpropyl)phenyl]-difluoromethyl]phosphonic acid
   Show/Hide
C22H18ClF2O4P
  1
1 IC50 = 360 nM
CP0151233
 Compound Info 
2,2-Bis-[4-(difluoro-phosphono-methyl)-benzyl]-malonic acid monomethyl ester
   Show/Hide
C20H20F4O10P2
  1
1 IC50 = 390 nM
CP0292182
 Compound Info 
4-{2-[4-(Difluoro-phosphono-methyl)-benzyl]-3-oxo-2,3-diphenyl-propyl}-benzoic acid
   Show/Hide
C30H25F2O6P
  1
1 IC50 = 800 nM
CP0205894
 Compound Info 
2-[4-(Difluoro-phosphono-methyl)-benzyl]-2-(4-methanesulfonyl-benzyl)-malonic acid dibenzyl ester
   Show/Hide
C33H31F2O9PS
  1
1 IC50 = 940 nM
CP0289829
 Compound Info 
[difluoro-[4-(3-oxo-2,3-diphenylpropyl)phenyl]methyl]phosphonic acid
   Show/Hide
C22H19F2O4P
  1
1 IC50 = 2000 nM
CP0336775
 Compound Info 
2-(4-(benzyloxy)-3-(2-(2-(4-chlorophenyl)-4-methylthiazol-5-yl)ethoxy)phenyl)-3,3,3-trifluoro-2-hydroxypropanoic acid
   Show/Hide
C28H23ClF3NO5S
  1
1 IC50 = 3000 nM
CP0036444
 Compound Info 
5-{2-fluoro-5-[(1E)-3-[3-hydroxy-2-(methoxycarbonyl)phenoxy]prop-1-en-1-yl]phenyl}-1,2-oxazole-3-carboxylic acid
   Show/Hide
C21H16FNO7
  3
1 Ki = 6309.57 nM
2 Ki = 6900 nM
3 Ki = 7000 nM
Clinical Information about the Protein
Target 1 ( PTPN1 messenger RNA (PTPN1 mRNA) )
Target Type Successful Target
Disease 3 Target-related Diseases  3
1 Infectious disease [ICD-11: 1A00-CA43.1]
2 Metabolic syndrome x [ICD-11: 5C50-5D2Z]
3 Type-2 diabetes [ICD-11: 5A11]
Approved Drug(s) 1 Approved Drug  1
1 Hydrogen peroxide
 Drug Info 
Approved
Infectious disease
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 URSOLIC ACID
 Drug Info 
Phase 2
Metabolic syndrome x
Discontinued Drug(s) 1 Discontinued Drug  1
1 ERTIPROTAFIB
 Drug Info 
Terminated
Type-2 diabetes
Target 2 ( Protein-tyrosine phosphatase 1B (PTP1B) )
Target Type Clinical trial Target
Disease 2 Target-related Diseases  2
1 Obesity [ICD-11: 5B81]
2 Type-2 diabetes [ICD-11: 5A11]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Trodusquemine
 Drug Info 
Phase 1
Obesity
Discontinued Drug(s) 1 Discontinued Drug  1
1 JTT-551
 Drug Info 
Terminated
Type-2 diabetes
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02225 Tyrosine-protein phosphatase non-receptor type 1 Mus musculus, Mouse
 Protein Info