Page last updated: 2024-08-05 15:13:20

EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor

An EC 3.1.3.* (phosphoric monoester hydrolase) inhibitor which interferes with the activity of the enzyme protein tyrosine phosphatases (PTPs), EC 3.1.3.48, involved in the removal of phosphate groups from phosphorylated tyrosine residues on proteins.

ChEBI ID: 35608

Members (8)

MemberDefinitionClass
bay 11-7082A nitrile that is acrylonitrile in which the hydrogen located beta,trans to the cyano group is replaced by a tosyl group. It is an inhibitor of cytokine-induced IkappaB-alpha phosphorylation in cells.(E)-3-tosylacrylonitrile
berberineberberine
gsk2656157A pyrrolopyrimidine that is 7-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine which has been substituted at position 5 by a 4-fluoro-2,3-dihydro-1H-indol-5-yl group, the nitrogen of which has been acylated by a (6-methylpyridin-2-yl)acetyl group. An orally bioavailable PERK inhibitor.GSK2656157
o-iodoxybenzoic acidA benziodoxole compound having hydroxy and oxo substituents at the 1-position and an oxo substituent at the 3-position. It is a mild and efficient hypervalent iodine synthetic reagent used to carry out several selective oxidation reactions.1-hydroxy-1,3-dioxobenziodoxole
oltiprazA 1,2-dithiole that is 3H-1,2-dithiole-3-thione substituted at positions 4 and 5 by methyl and pyrazin-2-yl groups respectively.oltipraz
oxophenylarsineAn arsine oxide derived from phenylarsine.phenylarsine oxide
sodium selenateAn inorganic sodium salt having selenate as the counterion.sodium selenate
vanadatesA vanadium oxoanion that is a trianion with formula VO4 in which the vanadium is in the +5 oxidation state and is attached to four oxygen atoms.vanadate(3-)

Research

Studies (10,515)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19901,228 (11.68)18.7374
1990's2,396 (22.79)18.2507
2000's2,498 (23.76)29.6817
2010's3,106 (29.54)24.3611
2020's1,287 (12.24)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials138 (1.27%)5.53%
Reviews449 (4.12%)6.00%
Case Studies15 (0.14%)4.05%
Observational2 (0.02%)0.25%
Other10,293 (94.46%)84.16%

Protein Targets (142)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
activating transcription factor 6Homo sapiens (human)Potency2.329022
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency14.929223
Alpha-synucleinHomo sapiens (human)Potency11.582111
Amyloid-beta precursor proteinHomo sapiens (human)Potency2.310911
AR proteinHomo sapiens (human)Potency0.466688
ATAD5 protein, partialHomo sapiens (human)Potency24.834422
Ataxin-2Homo sapiens (human)Potency5.038522
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency3.013111
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency0.077022
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency9.268311
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency0.685911
caspase-3Homo sapiens (human)Potency0.685911
Cellular tumor antigen p53Homo sapiens (human)Potency4.686722
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency9.647513
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency22.196912
chromobox protein homolog 1Homo sapiens (human)Potency39.810711
cytochrome P450 2C9, partialHomo sapiens (human)Potency10.684011
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency2.511911
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency12.589322
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency8.486611
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency0.306411
D(1A) dopamine receptorHomo sapiens (human)Potency12.589311
estrogen nuclear receptor alphaHomo sapiens (human)Potency1.93651010
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency1.852222
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency6.36181011
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency1.353412
EWS/FLI fusion proteinHomo sapiens (human)Potency8.357244
farnesoid X nuclear receptorHomo sapiens (human)Potency3.722333
Fumarate hydrataseHomo sapiens (human)Potency34.327312
GVesicular stomatitis virusPotency10.684011
GABA theta subunitRattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency12.589311
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency12.589311
GLI family zinc finger 3Homo sapiens (human)Potency0.101822
GLS proteinHomo sapiens (human)Potency12.589311
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency3.151533
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency0.544811
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency2.930911
heat shock protein beta-1Homo sapiens (human)Potency0.577722
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency23.930913
histone deacetylase 9 isoform 3Homo sapiens (human)Potency0.172311
Histone H2A.xCricetulus griseus (Chinese hamster)Potency1.791011
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency10.684011
hypothetical protein, conservedTrypanosoma bruceiPotency16.944111
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency2.095822
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency2.511922
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency10.684012
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency10.430422
Interferon betaHomo sapiens (human)Potency10.497524
LuciferasePhotinus pyralis (common eastern firefly)Potency31.705511
Microtubule-associated protein tauHomo sapiens (human)Potency9.834412
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency115.821011
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency0.485611
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency16.150922
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency0.842222
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency0.638433
ParkinHomo sapiens (human)Potency29.092911
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency6.242622
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency0.787333
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency1.832522
phosphopantetheinyl transferaseBacillus subtilisPotency2.528612
polyproteinZika virusPotency34.327312
PPM1D proteinHomo sapiens (human)Potency10.435312
pregnane X nuclear receptorHomo sapiens (human)Potency0.611311
progesterone receptorHomo sapiens (human)Potency3.108922
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.225622
ras-related protein Rab-9AHomo sapiens (human)Potency58.047911
regulator of G-protein signaling 4Homo sapiens (human)Potency2.990612
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency0.451933
retinoid X nuclear receptor alphaHomo sapiens (human)Potency0.054922
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency0.521211
SMAD family member 2Homo sapiens (human)Potency0.870811
SMAD family member 3Homo sapiens (human)Potency0.870811
survival motor neuron protein isoform dHomo sapiens (human)Potency7.079511
TDP1 proteinHomo sapiens (human)Potency0.975422
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.543733
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency0.134233
thyroid stimulating hormone receptorHomo sapiens (human)Potency13.699944
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency14.394622
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency0.245411
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency6.668613
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency0.544811

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AcetylcholinesteraseElectrophorus electricus (electric eel)IC500.782733
AcetylcholinesteraseHomo sapiens (human)IC500.400022
Aldo-keto reductase family 1 member C2 Homo sapiens (human)IC506.710011
Aldo-keto reductase family 1 member C3Homo sapiens (human)IC504.990022
Carbonic anhydrase Astrosclera willeyanaKi880.000011
Carbonic anhydrase Pseudomonas aeruginosa PAO1Ki23,500.000011
Carbonic anhydrase 1Homo sapiens (human)Ki103,321.250088
Carbonic anhydrase 13Mus musculus (house mouse)Ki484,000.000011
Carbonic anhydrase 2Homo sapiens (human)Ki112,000.00001717
Carbonic anhydrase 4Homo sapiens (human)Ki138,000.000011
Carbonic anhydrase 7Homo sapiens (human)Ki215,000.000011
CholinesteraseEquus caballus (horse)IC5015.266733
CholinesteraseHomo sapiens (human)IC5015.895022
Class A sortase SrtA Staphylococcus aureusIC50129.000011
Cytochrome P450 1A2Homo sapiens (human)Ki9.000011
Cytochrome P450 1B1Homo sapiens (human)IC500.974733
Cytochrome P450 1B1Homo sapiens (human)Ki0.044011
Cytochrome P450 3A4Homo sapiens (human)IC500.245022
eIF-2-alpha kinase GCN2Homo sapiens (human)IC503.388011
Eukaryotic translation initiation factor 2-alpha kinase 1Homo sapiens (human)IC500.460011
Eukaryotic translation initiation factor 2-alpha kinase 3Homo sapiens (human)IC500.015422
Histone-lysine N-methyltransferase EHMT1Homo sapiens (human)IC50100.000011
Histone-lysine N-methyltransferase EHMT2Homo sapiens (human)IC50100.000011
Interferon-induced, double-stranded RNA-activated protein kinaseHomo sapiens (human)IC500.905011
Lysine-specific histone demethylase 1AHomo sapiens (human)IC506.970011
Mu-type opioid receptorRattus norvegicus (Norway rat)Ki112,000.000011
NACHT, LRR and PYD domains-containing protein 3 Mus musculus (house mouse)IC5012.000011
NeuraminidaseInfluenza A virus (A/USSR/90/1977(H1N1))IC5035.350022
NeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))Ki14.300011
Nuclear factor NF-kappa-B p100 subunit Homo sapiens (human)IC502.000011
Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)IC502.000011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC5066.069311
Prolyl endopeptidaseHomo sapiens (human)IC50143.500022
Receptor-interacting serine/threonine-protein kinase 1Homo sapiens (human)IC500.069111
Receptor-type tyrosine-protein phosphatase FHomo sapiens (human)IC5022.563313
Replicase polyprotein 1abBetacoronavirus England 1IC5010.000013
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC500.550013
Telomerase reverse transcriptaseHomo sapiens (human)IC5037.000011
Transcription factor p65Homo sapiens (human)IC502.500022
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)IC50215.785946
Tyrosine-protein phosphatase non-receptor type 11Homo sapiens (human)IC5022.563313
Tyrosine-protein phosphatase non-receptor type 2Homo sapiens (human)IC5022.563313
Tyrosine-protein phosphatase non-receptor type 6Homo sapiens (human)IC5022.563313

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Carbonic anhydrase 12Homo sapiens (human)Kinact138,000.000011
Carbonic anhydrase 14Homo sapiens (human)Kinact49,600.000011
Carbonic anhydrase 9Homo sapiens (human)Kinact183,000.000011
Nuclear factor erythroid 2-related factor 2Mus musculus (house mouse)CD10.200011