Page last updated: 2024-08-05 15:23:07

EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor

Any EC 3.1.3.* (phosphoric monoester hydrolase) inhibitor that interferes with the action of phosphoprotein phosphatase (EC 3.1.3.16).

ChEBI ID: 37153

Members (10)

MemberDefinitionClass
cantharidinA monoterpenoid with an epoxy-bridged cyclic dicarboxylic anhydride structure secreted by many species of blister beetle, and most notably by the Spanish fly, Lytta vesicatoria. Natural toxin inhibitor of protein phosphatases 1 and 2A.cantharidin
cyanoginosin lrA microcystin consisting of D-alanyl, L-leucyl, (3S)-3-methyl-D-beta-aspartyl,L-arginyl, 2S,3S,4E,6E,8S,9S)-3-amino-4,5,6,7-tetradehydro-9-methoxy-2,6,8-trimethyl-10-phenyldecanoyl, D-gamma-glutamyl, and 2,3-didehydro-N-methylalanyl residues joined into a 25-membered macrocycle. Produced by the cyanobacterium Microcystis aeruginosa, it is the most studied of the microcystins.microcystin-LR
cyclosporineA cyclic nonribosomal peptide of eleven amino acids; an immunosuppressant drug widely used in post-allogeneic organ transplant to reduce the activity of the patient's immune system, and therefore the risk of organ rejection. Also causes reversible inhibition of immunocompetent lymphocytes in the G0- and G1-phase of the cell cycle.cyclosporin A
decamethrinA cyclopropanecarboxylate ester obtained by formal condensation between 3-(2,2-dibromovinyl)-2,2-dimethylcyclopropanecarboxylic acid and cyano(3-phenoxyphenyl)methanol. It is the active insecticide of the proinsecticide tralomethrin.deltamethrin
dinophysistoxin 1A ketal that is a marine toxin structurally related to okadaic acid. Produced by dinoflagellates it is known to accumulate in shellfish and cause diarrhoeic shellfish poisoning. It is an inhibitor of serine/threonine protein phosphatases 1 (PP1) and PP2A and has been shown to promote cancer cell growth in tumour cell lines and animal models.dinophysistoxin 1
dinophysistoxin 2A ketal that is a rare marine toxin structurally related to okadaic acid. Found yearly along with okadaic acid in Portuguese shellfish, its presence has been correlated with the occurrence of Dinophysis acta.dinophysistoxin 2
fostriecinA structurally unique, naturally-occurring phosphate monoester isolated from the soil bacterium Streptomyces pulveraceus. It inhibits DNA topoisomerase II as well as several protein phosphatase including PP2A and PPA4, and exhibits potent antitumor activity against several cancer cell lines.fostriecin
leflunomideA monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-methyl-1,2-oxazole-4-carboxylic acid with the anilino group of 4-(trifluoromethyl)aniline. The prodrug of teriflunomide.leflunomide
okadaic acidA polycyclic ether that is produced by several species of dinoflagellates, and is known to accumulate in both marine sponges and shellfish. A polyketide, polyether derivative of a C38 fatty acid, it is one of the primary causes of diarrhetic shellfish poisoning (DSP). It is a potent inhibitor of specific protein phosphatases and is known to have a variety of negative effects on cells.okadaic acid
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 (11,591)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19901,343 (11.59)18.7374
1990's2,625 (22.65)18.2507
2000's3,239 (27.94)29.6817
2010's3,345 (28.86)24.3611
2020's1,039 (8.96)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials265 (2.17%)5.53%
Reviews548 (4.48%)6.00%
Case Studies360 (2.95%)4.05%
Observational22 (0.18%)0.25%
Other11,026 (90.22%)84.16%

Protein Targets (186)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
67.9K proteinVaccinia virusPotency1.619422
acetylcholinesteraseHomo sapiens (human)Potency48.508812
activating transcription factor 6Homo sapiens (human)Potency44.307125
AR proteinHomo sapiens (human)Potency13.94981130
aryl hydrocarbon receptorHomo sapiens (human)Potency7.609724
arylsulfatase AHomo sapiens (human)Potency37.933011
ATAD5 protein, partialHomo sapiens (human)Potency8.566345
Ataxin-2Homo sapiens (human)Potency3.902212
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency3.902224
Bloom syndrome protein isoform 1Homo sapiens (human)Potency28.183822
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency1.805812
caspase-3Homo sapiens (human)Potency1.805812
Cellular tumor antigen p53Homo sapiens (human)Potency48.208625
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency10.000024
Chain A, Beta-lactamaseEscherichia coli K-12Potency2.818411
cytochrome P450 2C19 precursorHomo sapiens (human)Potency15.848911
cytochrome P450 2C9 precursorHomo sapiens (human)Potency31.622811
cytochrome P450 2C9, partialHomo sapiens (human)Potency13.802911
cytochrome P450 2D6Homo sapiens (human)Potency12.708212
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency2.821424
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency3.467112
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency5.590613
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency57.122012
Endothelin receptor type BRattus norvegicus (Norway rat)Potency17.782811
Endothelin-1 receptorRattus norvegicus (Norway rat)Potency17.782811
estrogen nuclear receptor alphaHomo sapiens (human)Potency13.32381028
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency11.564612
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency16.76261037
EWS/FLI fusion proteinHomo sapiens (human)Potency16.136244
farnesoid X nuclear receptorHomo sapiens (human)Potency27.211838
Fumarate hydrataseHomo sapiens (human)Potency11.770411
GVesicular stomatitis virusPotency13.802911
GABA theta subunitRattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency2.821412
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency2.821412
gemininHomo sapiens (human)Potency1.319334
GLI family zinc finger 3Homo sapiens (human)Potency9.6655310
glp-1 receptor, partialHomo sapiens (human)Potency8.318612
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency30.3164510
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency13.561313
heat shock protein beta-1Homo sapiens (human)Potency49.000926
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency31.622813
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency27.829812
histone deacetylase 9 isoform 3Homo sapiens (human)Potency1.756124
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency13.802911
huntingtin isoform 2Homo sapiens (human)Potency2.969822
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency46.635414
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency2.511922
IDH1Homo sapiens (human)Potency14.581011
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency13.802912
Integrin alpha-IIbHomo sapiens (human)Potency10.000012
Integrin beta-3Homo sapiens (human)Potency10.000012
Interferon betaHomo sapiens (human)Potency13.510738
lamin isoform A-delta10Homo sapiens (human)Potency5.083513
LuciferasePhotinus pyralis (common eastern firefly)Potency22.367034
mitogen-activated protein kinase 1Homo sapiens (human)Potency10.430422
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency17.015722
neuropeptide S receptor isoform AHomo sapiens (human)Potency0.079411
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency18.044812
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency2.288213
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency19.3323310
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency8.310923
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency39.810711
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency48.655713
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency20.246622
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency3.981111
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency10.4965311
P53Homo sapiens (human)Potency56.234111
ParkinHomo sapiens (human)Potency1.636011
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency1.689624
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency37.933011
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency25.8009510
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency26.017234
phosphopantetheinyl transferaseBacillus subtilisPotency39.810711
plasminogen precursorMus musculus (house mouse)Potency5.712212
polyproteinZika virusPotency11.770411
PPM1D proteinHomo sapiens (human)Potency12.212614
pregnane X nuclear receptorHomo sapiens (human)Potency8.009838
pregnane X receptorRattus norvegicus (Norway rat)Potency25.118911
progesterone receptorHomo sapiens (human)Potency34.563113
pyruvate kinaseLeishmania mexicana mexicanaPotency17.782822
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency2.511911
RAR-related orphan receptor gammaMus musculus (house mouse)Potency19.9728210
ras-related protein Rab-9AHomo sapiens (human)Potency1.071612
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency8.8588311
retinoid X nuclear receptor alphaHomo sapiens (human)Potency21.658849
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810711
survival motor neuron protein isoform dHomo sapiens (human)Potency12.468127
TDP1 proteinHomo sapiens (human)Potency4.282528
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.631011
ThrombopoietinHomo sapiens (human)Potency7.943322
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency23.257329
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency22.339222
thyroid stimulating hormone receptorHomo sapiens (human)Potency17.228911
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency5.712212
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency5.712212
USP1 protein, partialHomo sapiens (human)Potency193.217922
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency43.286324
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency13.803446
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency13.561313

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC504.630011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki4.591011
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC509.340011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC509.340011
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC509.340011
Amine oxidase [flavin-containing] AHomo sapiens (human)IC5020.696011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC5052.210523
ATP-dependent translocase ABCB1Homo sapiens (human)IC503.04644142
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC502.750044
ATP-dependent translocase ABCB1Homo sapiens (human)Ki1.718366
ATP-dependent translocase ABCB1Mus musculus (house mouse)Ki3.575022
Bile salt export pumpHomo sapiens (human)IC5040.7636811
Bile salt export pumpRattus norvegicus (Norway rat)IC5056.100012
Bile salt export pumpHomo sapiens (human)Ki9.500011
Bile salt export pumpRattus norvegicus (Norway rat)Ki0.300011
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC5024.654633
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)Ki0.500011
Calcineurin subunit B type 1Homo sapiens (human)IC5034.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC5037.161756
Canalicular multispecific organic anion transporter 1Homo sapiens (human)Ki11.270033
Canalicular multispecific organic anion transporter 1Rattus norvegicus (Norway rat)Ki5.980022
Chain A, Serine/threonine protein phosphatase PP1-gamma catalytic subunitHomo sapiens (human)IC500.097011
Cytochrome P450 1A2Homo sapiens (human)IC5050.250022
Cytochrome P450 2C19Homo sapiens (human)IC507.000011
Cytochrome P450 2C9 Homo sapiens (human)IC5038.800011
Cytochrome P450 2D6Homo sapiens (human)IC50100.000011
Cytochrome P450 3A4Homo sapiens (human)IC503.734045
Cytochrome P450 3A4Homo sapiens (human)Ki6.055024
Cytochrome P450 3A43 Homo sapiens (human)IC502.060011
Cytochrome P450 3A43 Homo sapiens (human)Ki7.600012
Cytochrome P450 3A5Homo sapiens (human)IC502.060011
Cytochrome P450 3A5Homo sapiens (human)Ki7.600012
Cytochrome P450 3A7Homo sapiens (human)IC502.060011
Cytochrome P450 3A7Homo sapiens (human)Ki7.600012
Dihydroorotate dehydrogenase (quinone), mitochondrialHomo sapiens (human)IC5018.450034
Dihydroorotate dehydrogenase (quinone), mitochondrialMus musculus (house mouse)IC500.030011
Dihydroorotate dehydrogenase (quinone), mitochondrialRattus norvegicus (Norway rat)IC500.009011
fMet-Leu-Phe receptorHomo sapiens (human)IC5010.000011
Ileal sodium/bile acid cotransporterHomo sapiens (human)Ki24.000011
Interleukin-2Mus musculus (house mouse)IC500.005011
Multidrug resistance-associated protein 1 Homo sapiens (human)IC503.50821010
Multidrug resistance-associated protein 1 Homo sapiens (human)Ki5.000011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000012
Peptidyl-prolyl cis-trans isomerase A Homo sapiens (human)IC500.02521212
Peptidyl-prolyl cis-trans isomerase A Homo sapiens (human)Ki0.064588
Peptidyl-prolyl cis-trans isomerase BHomo sapiens (human)IC500.008811
Peptidyl-prolyl cis-trans isomerase DHomo sapiens (human)IC500.003611
Peptidyl-prolyl cis-trans isomerase DHomo sapiens (human)Ki0.012944
Peptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)Ki0.020011
Peptidyl-prolyl cis-trans isomerase FKBP1BHomo sapiens (human)Ki0.006011
Peptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)IC500.016011
Peptidylglycine alpha-amidating monooxygenaseRattus norvegicus (Norway rat)Ki0.006011
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Mus musculus (house mouse)IC500.570011
Protein phosphatase 1AHomo sapiens (human)IC500.003011
Protein phosphatase 1BHomo sapiens (human)IC501.780011
Protein-arginine deiminase type-4Homo sapiens (human)IC502,400.000011
Receptor-type tyrosine-protein phosphatase FHomo sapiens (human)IC5022.563313
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC505.820011
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC500.455011
Sarcoplasmic/endoplasmic reticulum calcium ATPase 1Oryctolagus cuniculus (rabbit)IC5062.000011
Serine/threonine-protein phosphatase 2A 55 kDa regulatory subunit B Gallus gallus (chicken)IC500.2527810
Serine/threonine-protein phosphatase 2A 55 kDa regulatory subunit B alpha isoformHomo sapiens (human)IC500.000111
Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoformHomo sapiens (human)IC500.007011
Serine/threonine-protein phosphatase 2B catalytic subunit alpha isoformHomo sapiens (human)IC500.183011
Serine/threonine-protein phosphatase PP1-gamma catalytic subunitHomo sapiens (human)IC501.07782122
Sodium-dependent dopamine transporter Homo sapiens (human)IC502.884011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki2.291011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC504.630011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki4.591011
Sodium/bile acid cotransporterHomo sapiens (human)IC501.000011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC500.950055
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Ki0.484544
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC501.300011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Ki1.200011
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)IC5037.000011
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)Ki36.000011
Substance-K receptorHomo sapiens (human)IC504.139011
Substance-K receptorHomo sapiens (human)Ki1.380011
TransthyretinHomo sapiens (human)Ki0.002611
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)IC508.075379
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
UDP-glucuronosyltransferase 1-6Homo sapiens (human)IC50211.833316
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50211.833316
UDP-glucuronosyltransferase 1A4Homo sapiens (human)IC50211.833316
UDP-glucuronosyltransferase 2B10 Homo sapiens (human)IC50211.833316
UDP-glucuronosyltransferase 2B7Homo sapiens (human)IC50211.833316

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
ATP-dependent translocase ABCB1Homo sapiens (human)EC5025.779988
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)EC501.750011
Cytochrome P450 3A4Homo sapiens (human)Kd0.013011
matrix metalloproteinase 1, partialHomo sapiens (human)EC505.650011
Multidrug resistance-associated protein 1 Homo sapiens (human)EC501.700011
Peptidyl-prolyl cis-trans isomerase A Homo sapiens (human)Kd0.62251111
Peptidyl-prolyl cis-trans isomerase BHomo sapiens (human)Kd0.009811
Peptidyl-prolyl cis-trans isomerase DHomo sapiens (human)Kd0.021522

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
ATP-dependent translocase ABCB1Homo sapiens (human)Activity9.033333
ATP-dependent translocase ABCB1Homo sapiens (human)Km4.123333
fMet-Leu-Phe receptorHomo sapiens (human)IC203.600011
Non-lysosomal glucosylceramidaseMus musculus (house mouse)Activity11.000011
scavenger receptor class B member 1 isoform 1Mus musculus (house mouse)AbsAC40_uM35.000011
Solute carrier organic anion transporter family member 1A2Homo sapiens (human)Km20.000011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Km12.400011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Km12.400011
UDP-glucuronosyltransferase 2B7Homo sapiens (human)Km202.000011